Romidepsin
别名: FK228, Depsipeptide, FR 901228, NSC 630176, 中文名称：罗米地辛
Romidepsin (FK228, Depsipeptide, FR 901228, NSC 630176)是一种有效的HDAC1和HDAC2抑制剂，无细胞试验中IC50分别为36 nM和47 nM。Romidepsin (FK228/depsipeptide) 在神经母细胞瘤肿瘤细胞中可控制生长并诱导凋亡。
Romidepsin Chemical Structure
CAS: 128517-07-7
产品质控
批次：
纯度：
99.89%
99.89
Romidepsin 相关产品
相关信号通路图
细胞实验数据示例
| 细胞系 | 实验类型 | 给药浓度 | 孵育时间 | 活性描述 | 文献信息 |
|---|---|---|---|---|---|
| A549 | Growth Inhibition Assay | 5 nM | 24/48/72 h | inhibits cell growth time-dependently | 22106282 |
| LNCaP | Growth Inhibition Assay | 5 nM | 24/48/72 h | inhibits cell growth time-dependently | 22106282 |
| HFS | Growth Inhibition Assay | 5 nM | 24/48/72 h | inhibits cell growth time-dependently | 22106282 |
| CO115 | Growth Inhibition Assay | 5 nM-50 μM | 24 h | inhibits cell growth in a concentration-dependent manner | 22924958 |
| RKO | Growth Inhibition Assay | 5 nM-50 μM | 24 h | inhibits cell growth in a concentration-dependent manner | 22924958 |
| HCT116 | Growth Inhibition Assay | 5 nM-50 μM | 24 h | inhibits cell growth in a concentration-dependent manner | 22924958 |
| NCI/ADR-RES | Growth Inhibition Assay | 1–20nM | 72 h | reduces cell viability alone and combined with cisplatin | 23010348 |
| OVCAR-8 | Growth Inhibition Assay | 1–20nM | 72 h | reduces cell viability alone and combined with cisplatin | 23010348 |
| Brca1 Null | Growth Inhibition Assay | 1–20nM | 72 h | reduces cell viability alone and combined with cisplatin | 23010348 |
| Brca1 WT | Growth Inhibition Assay | 1–20nM | 72 h | reduces cell viability alone and combined with cisplatin | 23010348 |
| SKOV-3 | Growth Inhibition Assay | 1–20nM | 72 h | reduces cell viability alone and combined with cisplatin | 23010348 |
| DpP75 | Apoptosis Assay | 1/10/100 nM | 48 h | induces blunt apoptosis | 23532732 |
| DpVp50 | Apoptosis Assay | 1/10/100 nM | 48 h | induces blunt apoptosis | 23532732 |
| DpVp35 | Apoptosis Assay | 1/10/100 nM | 48 h | induces blunt apoptosis | 23532732 |
| HuT78 | Apoptosis Assay | 1/10/100 nM | 48 h | induces apoptosis at 1 nM | 23532732 |
| A549 | Growth Inhibition Assay | 10–100 nM | 24/36/48 h | inhibits cell growth in both concentration- and time-dependent manner | 24485799 |
| MS-275 | Growth Inhibition Assay | 0.625-10nM | 48 h | induces a significantly stronger inhibition of cell proliferation co-treated with bortezomib | 24771510 |
| HA | Growth Inhibition Assay | 0.625-10nM | 48 h | induces a significantly stronger inhibition of cell proliferation co-treated with bortezomib | 24771510 |
| ACH-2 | Function Assay | 1-9 nM | 24 h | induces HIV-1 Env expression | 25149467 |
| HCT116 | Growth Inhibition Assay | 5-5000 nM | 24 h | induces cell death in a concentration-dependent manner | 25492515 |
| U2932/EBV | Cell Viability Assay | 2.5-15 nM | 72 h | induces cytotoxicity in a concentration-dependent manner | 25790907 |
| LY7/EBV | Cell Viability Assay | 2.5-15 nM | 72 h | induces cytotoxicity in a concentration-dependent manner | 25790907 |
| Farage | Cell Viability Assay | 2.5-15 nM | 72 h | induces cytotoxicity in a concentration-dependent manner | 25790907 |
| OCI-LY7 | Cell Viability Assay | 2.5-15 nM | 72 h | induces cytotoxicity in a concentration-dependent manner | 25790907 |
| U2932 | Cell Viability Assay | 2.5-15 nM | 72 h | induces cytotoxicity in a concentration-dependent manner | 25790907 |
| SU-DHL4 | Cell Viability Assay | 2.5-15 nM | 72 h | induces cytotoxicity in a concentration-dependent manner | 25790907 |
| THJ-16T | Growth Inhibition Assay | 1 nM | 24 h | inhibits cell growth | 20810568 |
| HCT116 | Function Assay | 20 nM | 8 h | modulates transcript levels for hundreds of genes in either direction | 20739454 |
| B104 | Function Assay | 2 nM | 24/48/72 h | increases the surface expression of CD20 | 20686505 |
| HL-60 | Cytotoxicity Assay | 1-500 nM | 24 h | induces cytotoxicity in a concentration-dependent manner | 20624163 |
| HP100 | Cytotoxicity Assay | 1-500 nM | 24 h | induces cytotoxicity in a concentration-dependent manner | 20624163 |
| HL-60 | Function Assay | 10 nM | 4/6/16 h | induces the generation of hydrogen peroxide from 4h | 20624163 |
| HP100 | Function Assay | 10 nM | 4/6/16 h | induces the generation of hydrogen peroxide from 4h | 20624163 |
| HL-60 | Function Assay | 10-500 nM | 4 h | decreases the histone deacetylase (HDAC) activity | 20624163 |
| HP100 | Function Assay | 10-500 nM | 4 h | decreases the histone deacetylase (HDAC) activity | 20624163 |
| SKOV-3 | Growth Inhibition Assay | 4/8/16 nM | 48 h | inhibits cell growth in a concentration-dependent manner | 20404564 |
| OVCAR-3 | Growth Inhibition Assay | 4/8/16 nM | 48 h | inhibits cell growth in a concentration-dependent manner | 20404564 |
| HBL-2 | Growth Inhibition Assay | 2-10 nM | 24 h | IC50=4.3 nM | 20068080 |
| Jeko-1 | Growth Inhibition Assay | 2-50 nM | 24 h | IC50=11 nM | 20068080 |
| Granta-519 | Growth Inhibition Assay | 5-40 nM | 24 h | IC50=58.5 nM | 20068080 |
| L1236 | Cytotoxicity Assay | 1 nM-100 μM | 48 h | EC50=0.07 μM | 19233470 |
| L428 | Cytotoxicity Assay | 1 nM-100 μM | 48 h | EC50=0.43 μM | 19233470 |
| KM-H2 | Cytotoxicity Assay | 1 nM-100 μM | 48 h | EC50=0.58 μM | 19233470 |
| L540Cy | Cytotoxicity Assay | 1 nM-100 μM | 48 h | EC50=0.16 μM | 19233470 |
| G401 | Function Assay | 10 nM | 24/48/72 h | increases CDKN1C expression | 19221586 |
| STM91-01 | Function Assay | 10 nM | 24/48/72 h | increases CDKN1C expression | 19221586 |
| SJSC | Function Assay | 10 nM | 24/48/72 h | increases CDKN1C expression | 19221586 |
| BT16 | Function Assay | 10 nM | 24/48/72 h | increases CDKN1C expression | 19221586 |
| NCI-H23 | Antitumor assay | 1.6 to 2.4 mg/kg | up to 5 days | Antitumor activity against human NCI-H23 cells implanted intraperitoneally in mouse assessed as inhibition of tumor cell growth at 1.6 to 2.4 mg/kg, ip administered on day 1 to 4 measured on day 5 by hollow fiber assay | 21967146 |
| NCI-H522 | Antitumor assay | 1.6 to 2.4 mg/kg | up to 5 days | Antitumor activity against human NCI-H522 cells implanted intraperitoneally in mouse assessed as inhibition of tumor cell growth at 1.6 to 2.4 mg/kg, ip administered on day 1 to 4 measured on day 5 by hollow fiber assay | 21967146 |
| OVCAR5 | Antitumor assay | 1.6 to 2.4 mg/kg | up to 5 days | Antitumor activity against human OVCAR5 cells implanted intraperitoneally in mouse assessed as inhibition of tumor cell growth at 1.6 to 2.4 mg/kg, ip administered on day 1 to 4 measured on day 5 by hollow fiber assay | 21967146 |
| SW620 | Antitumor assay | 1.6 to 2.4 mg/kg | up to 5 days | Antitumor activity against human SW620 cells implanted intraperitoneally in mouse assessed as inhibition of tumor cell growth at 1.6 to 2.4 mg/kg, ip administered on day 1 to 4 measured on day 5 by hollow fiber assay | 21967146 |
| MDA-MB-435 | Antitumor assay | 1.6 to 2.4 mg/kg | up to 5 days | Antitumor activity against human MDA-MB-435 cells implanted intraperitoneally in mouse assessed as inhibition of tumor cell growth at 1.6 to 2.4 mg/kg, ip administered on day 1 to 4 measured on day 5 by hollow fiber assay | 21967146 |
| COLO205 | Antitumor assay | 1.6 to 2.4 mg/kg | up to 5 days | Antitumor activity against human COLO205 cells implanted intraperitoneally in mouse assessed as inhibition of tumor cell growth at 1.6 to 2.4 mg/kg, ip administered on day 1 to 4 measured on day 5 by hollow fiber assay | 21967146 |
| LOXIMVI | Antitumor assay | 1.6 to 2.4 mg/kg | up to 5 days | Antitumor activity against human LOXIMVI cells implanted intraperitoneally in mouse assessed as inhibition of tumor cell growth at 1.6 to 2.4 mg/kg, ip administered on day 1 to 4 measured on day 5 by hollow fiber assay | 21967146 |
| UACC62 | Antitumor assay | 1.6 to 2.4 mg/kg | up to 5 days | Antitumor activity against human UACC62 cells implanted intraperitoneally in mouse assessed as inhibition of tumor cell growth at 1.6 to 2.4 mg/kg, ip administered on day 1 to 4 measured on day 5 by hollow fiber assay | 21967146 |
| MDA-MB-231 | Antitumor assay | 1.6 to 2.4 mg/kg | up to 5 days | Antitumor activity against human MDA-MB-231 cells implanted intraperitoneally in mouse assessed as inhibition of tumor cell growth at 1.6 to 2.4 mg/kg, ip administered on day 1 to 4 measured on day 5 by hollow fiber assay | 21967146 |
| SF295 | Antitumor assay | 1.6 to 2.4 mg/kg | up to 5 days | Antitumor activity against human SF295 cells implanted intraperitoneally in mouse assessed as inhibition of tumor cell growth at 1.6 to 2.4 mg/kg, ip administered on day 1 to 4 measured on day 5 by hollow fiber assay | 21967146 |
| U251 | Antitumor assay | 1.6 to 2.4 mg/kg | up to 5 days | Antitumor activity against human U251 cells implanted intraperitoneally in mouse assessed as inhibition of tumor cell growth at 1.6 to 2.4 mg/kg, ip administered on day 1 to 4 measured on day 5 by hollow fiber assay | 21967146 |
| OVRAC3 | Antitumor assay | 1.6 to 2.4 mg/kg | up to 5 days | Antitumor activity against human OVRAC3 cells implanted intraperitoneally in mouse assessed as inhibition of tumor cell growth at 1.6 to 2.4 mg/kg, ip administered on day 1 to 4 measured on day 5 by hollow fiber assay | 21967146 |
| 11z | Kinase Assay | 3-100 nM | reduces HDAC enzymatic activity (IC50 = 6.5 ± 0.6 nmol/L) | 20605144 | |
| ST486 | Apoptosis Assay | 6 h | induces extensive apoptosis | 23966164 | |
| Ramos | Apoptosis Assay | 6 h | induces extensive apoptosis | 23966164 | |
| DG75 | Apoptosis Assay | 6 h | induces no apoptosis | 23966164 | |
| CA46 | Apoptosis Assay | 6 h | induces blunt apoptosis | 23966164 | |
| U266 | Growth Inhibition Assay | 24/48 h | EC50s=10 nM; 48 h | 24030150 | |
| RPMI-8226 | Growth Inhibition Assay | 24/48 h | EC50s=1.8 nM; 48 h | 24030150 | |
| OPM-2 | Growth Inhibition Assay | 24/48 h | EC50s=1 nM; 48 h | 24030150 | |
| JJN3 | Growth Inhibition Assay | 24/48 h | EC50<1 nM; 48 h | 24030150 | |
| CD4 T | Growth Inhibition Assay | 48 h | CC50=107±126 nM | 24722454 | |
| CD4 T | Growth Inhibition Assay | 48 h | EC50=4.5±1.0 nM | 24722454 | |
| A498 | Cytotoxicity assay | 6 days | Cytotoxicity against human A498 cells after 6 days by MTT assay, TGI = 0.028 μM. | 21967146 | |
| COLO205 | Cytotoxicity assay | 6 days | Cytotoxicity against human COLO205 cells after 6 days by MTT assay, TGI = 0.031 μM. | 21967146 | |
| U251 | Cytotoxicity assay | 6 days | Cytotoxicity against human U251 cells after 6 days by MTT assay, TGI = 0.031 μM. | 21967146 | |
| RXF393 | Cytotoxicity assay | 6 days | Cytotoxicity against human RXF393 cells after 6 days by MTT assay, TGI = 0.062 μM. | 21967146 | |
| MDA-MB-468 | Cytotoxicity assay | 6 days | Cytotoxicity against human MDA-MB-468 cells after 6 days by MTT assay, TGI = 0.09 μM. | 21967146 | |
| COLO205 | Cytotoxicity assay | 6 days | Cytotoxicity against human COLO205 cells after 6 days by MTT assay, LC50 = 0.092 μM. | 21967146 | |
| UACC257 | Cytotoxicity assay | 6 days | Cytotoxicity against human UACC257 cells after 6 days by MTT assay, TGI = 0.095 μM. | 21967146 | |
| U251 | Cytotoxicity assay | 6 days | Cytotoxicity against human U251 cells after 6 days by MTT assay, LC50 = 0.13 μM. | 21967146 | |
| A498 | Cytotoxicity assay | 6 days | Cytotoxicity against human A498 cells after 6 days by MTT assay, LC50 = 0.2 μM. | 21967146 | |
| NCI-H322M | Cytotoxicity assay | 6 days | Cytotoxicity against human NCI-H322M cells after 6 days by MTT assay, TGI = 0.23 μM. | 21967146 | |
| SF295 | Cytotoxicity assay | 6 days | Cytotoxicity against human SF295 cells after 6 days by MTT assay, TGI = 0.25 μM. | 21967146 | |
| RXF393 | Cytotoxicity assay | 6 days | Cytotoxicity against human RXF393 cells after 6 days by MTT assay, LC50 = 0.3 μM. | 21967146 | |
| NCI60 | Cytotoxicity assay | 6 days | Cytotoxicity against human NCI60 cells after 6 days by MTT assay, TGI = 0.33 μM. | 21967146 | |
| SN12C | Cytotoxicity assay | 6 days | Cytotoxicity against human SN12C cells after 6 days by MTT assay, TGI = 0.34 μM. | 21967146 | |
| MDA-MB-231 | Cytotoxicity assay | 6 days | Cytotoxicity against human MDA-MB-231 cells after 6 days by MTT assay, TGI = 0.35 μM. | 21967146 | |
| ACHN | Cytotoxicity assay | 6 days | Cytotoxicity against human ACHN cells after 6 days by MTT assay, TGI = 0.73 μM. | 21967146 | |
| SN12C | Cytotoxicity assay | 6 days | Cytotoxicity against human SN12C cells after 6 days by MTT assay, LC50 = 1.5 μM. | 21967146 | |
| UO31 | Cytotoxicity assay | 6 days | Cytotoxicity against human UO31 cells after 6 days by MTT assay, TGI = 1.55 μM. | 21967146 | |
| Caki1 | Cytotoxicity assay | 6 days | Cytotoxicity against human Caki1 cells after 6 days by MTT assay, TGI = 1.89 μM. | 21967146 | |
| NCI60 | Cytotoxicity assay | 6 days | Cytotoxicity against human NCI60 cells after 6 days by MTT assay, LC50 = 3.5 μM. | 21967146 | |
| MDA-MB-231 | Cytotoxicity assay | 6 days | Cytotoxicity against human MDA-MB-231 cells after 6 days by MTT assay, LC50 = 4.08 μM. | 21967146 | |
| MDA-MB-468 | Cytotoxicity assay | 6 days | Cytotoxicity against human MDA-MB-468 cells after 6 days by MTT assay, LC50 = 4.14 μM. | 21967146 | |
| ACHN | Cytotoxicity assay | 6 days | Cytotoxicity against human ACHN cells after 6 days by MTT assay, LC50 = 5.37 μM. | 21967146 | |
| UACC257 | Cytotoxicity assay | 6 days | Cytotoxicity against human UACC257 cells after 6 days by MTT assay, LC50 = 5.46 μM. | 21967146 | |
| NCI-H322M | Cytotoxicity assay | 6 days | Cytotoxicity against human NCI-H322M cells after 6 days by MTT assay, LC50 = 9.02 μM. | 21967146 | |
| SF295 | Cytotoxicity assay | 6 days | Cytotoxicity against human SF295 cells after 6 days by MTT assay, LC50 = 10.2 μM. | 21967146 | |
| Caki1 | Cytotoxicity assay | 6 days | Cytotoxicity against human Caki1 cells after 6 days by MTT assay, LC50 = 20.9 μM. | 21967146 | |
| CD4+ T | Function assay | 7 days | Reactivation of latent HIV1 NL4-3-Luc expression in human naive CD4+ T cells treated 7 days post-infection measured after 48 hrs by luminescence plate reader analysis, EC50 = 0.003 μM. | 24495105 | |
| 293T | Function assay | 30 mins | Inhibition of human HDAC1 expressed in human 293T cells using Ac-KGLGK(Ac)-MCA as substrate after 30 mins by fluorescence assay, IC50 = 0.0036 μM. | 24589486 | |
| 293T | Function assay | 30 mins | Inhibition of mouse HDAC6 expressed in human 293T cells using Ac-KGLGK(Ac)-MCA as substrate after 30 mins by fluorescence assay, IC50 = 0.39 μM. | 24589486 | |
| mink Mv1Lu | Function assay | 24 hrs | Increase in human wild type p21 protein expression in mink Mv1Lu cells after 24 hrs by p21 promoter assay in presence of 0.1 mM dithiothreitol, EC1000 = 0.0157 μM. | 24997578 | |
| HCT116 | Antiproliferative assay | 48 hrs | Antiproliferative activity against human HCT116 cells after 48 hrs in presence of DTT by MTT assay, IC50 = 0.003 μM. | 25147612 | |
| MOLT4 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human MOLT4 cells after 72 hrs by CCK8 assay, GI50 = 0.00206 μM. | 26331334 | |
| DU145 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human DU145 cells after 72 hrs by CCK8 assay, GI50 = 0.00255 μM. | 26331334 | |
| U937 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human U937 cells after 72 hrs by CCK8 assay, GI50 = 0.00341 μM. | 26331334 | |
| HLF | Antiproliferative assay | 72 hrs | Antiproliferative activity against human HLF cells after 72 hrs by CCK8 assay, GI50 = 0.00489 μM. | 26331334 | |
| WI38 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human WI38 cells after 72 hrs by CCK8 assay, GI50 = 0.00539 μM. | 26331334 | |
| U937 | Function assay | 24 hrs | Inhibition of HDAC6 in human U937 cells assessed as reduction of alpha-tubilin acetylation at 5 nM to 5 uM after 24 hrs by Western blot analysis | 26331334 | |
| HCT116 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human HCT116 cells assessed as cell viability incubated for 72 hrs by coulter counter method, IC50 = 0.028 μM. | 26481659 | |
| IGROV1/Pt1 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human IGROV1/Pt1 cells assessed as cell viability incubated for 72 hrs by coulter counter method, IC50 = 0.08 μM. | 26481659 | |
| IGROV1 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human IGROV1 cells assessed as cell viability incubated for 72 hrs by coulter counter method, IC50 = 0.22 μM. | 26481659 | |
| CD4+ T | Growth Inhibition Assay | EC50=3 nM | 24495105 | ||
| HuT-78 | Growth Inhibition Assay | IC50=1.73±0.44 nM | 24954856 | ||
| H526 | Growth Inhibition Assay | IC50=0.15±0.03 nM | 24954856 | ||
| H146 | Growth Inhibition Assay | IC50=0.22±0.07 nM | 24954856 | ||
| EKVX | Growth Inhibition Assay | IC50=1.33±0.34 nM | 24954856 | ||
| H460 | Growth Inhibition Assay | IC50=2.58±0.80 nM | 24954856 | ||
| A549 | Growth Inhibition Assay | IC50=1.26±0.24 nM | 24954856 | ||
| SF-295 | Growth Inhibition Assay | IC50=0.88±0.15 nM | 24954856 | ||
| MDA-MB-435 | Growth Inhibition Assay | IC50=0.90±0.06 nM | 24954856 | ||
| UACC-62 | Growth Inhibition Assay | IC50=0.56±0.16 nM | 24954856 | ||
| LOX-IMVI | Growth Inhibition Assay | IC50=0.87±0.03 nM | 24954856 | ||
| SW620 | Growth Inhibition Assay | IC50=0.93±0.29 nM | 24954856 | ||
| S1 | Growth Inhibition Assay | IC50=7.67±0.29 nM | 24954856 | ||
| HCT116-p21-/- | Growth Inhibition Assay | IC50=1.26±0.37 nM | 24954856 | ||
| HCT116 | Growth Inhibition Assay | IC50=1.00±0.00 nM | 24954856 | ||
| PC3 | Growth Inhibition Assay | IC50=1.65±0.35 nM | 24954856 | ||
| MDA-MB-231 | Growth Inhibition Assay | IC50=0.68±0.14 nM | 24954856 | ||
| SK-BR-3 | Growth Inhibition Assay | IC50=1.00±0.35 nM | 24954856 | ||
| MCF-7 | Growth Inhibition Assay | IC50=1.10±0.20 nM | 24954856 | ||
| MCF-10A | Growth Inhibition Assay | IC50=0.17±0.01 nM | 24954856 | ||
| 697 | Growth Inhibition Assay | IC50 = 2.5 nM | 21538216 | ||
| 697-R | Growth Inhibition Assay | IC50 = 8.6 nM | 21538216 | ||
| HUT78 | Growth Inhibition Assay | IC50=1 nM | 21198545 | ||
| NCI-H1299 | Growth Inhibition Assay | IC50=4.6±0.2 ng/ml | 19179890 | ||
| NCI-2882 | Growth Inhibition Assay | IC50=1.6±0.04 ng/ml | 19179890 | ||
| HCC95 | Growth Inhibition Assay | IC50=2.5±0.05 ng/ml | 19179890 | ||
| NCI-H23 | Growth Inhibition Assay | IC50=2.9±0.2 ng/ml | 19179890 | ||
| NCI-H157 | Growth Inhibition Assay | IC50=1.6±0.02 ng/ml | 19179890 | ||
| NCI-H460 | Growth Inhibition Assay | IC50=2.1±0.07 ng/ml | 19179890 | ||
| NCI-H1975 | Growth Inhibition Assay | IC50=1.3±0.04 ng/ml | 19179890 | ||
| NCI-H820 | Growth Inhibition Assay | IC50=2.4±0.1 ng/ml | 19179890 | ||
| NCI-H1650 | Growth Inhibition Assay | IC50=4.9±0.3 ng/ml | 19179890 | ||
| DTC1 | Growth Inhibition Assay | IC50=0.51 nM | 18566246 | ||
| KAO | Growth Inhibition Assay | IC50=0.91 nM | 18566246 | ||
| SU-CCS-1 | Growth Inhibition Assay | IC50=0.89 nM | 18566246 | ||
| SYO-1 | Growth Inhibition Assay | IC50=0.67 nM | 18566246 | ||
| FUJI | Growth Inhibition Assay | IC50=1.31 nM | 18566246 | ||
| SKNMC | Growth Inhibition Assay | IC50=1.17 nM | 18566246 | ||
| 402-91 | Growth Inhibition Assay | IC50=1.26 nM | 18566246 | ||
| 1765-92 | Growth Inhibition Assay | IC50=1.77 nM | 18566246 | ||
| JN-DSRCT-1 | Growth Inhibition Assay | IC50=1.25 nM | 18566246 | ||
| NMS-2PC | Growth Inhibition Assay | IC50=0.81 nM | 18566246 | ||
| HL60 | Growth Inhibition Assay | IC50=1.86 nM | 18566246 | ||
| A549 | Growth Inhibition Assay | IC50=3.24 nM | 18566246 | ||
| SW480 | Growth Inhibition Assay | IC50=2.69 nM | 18566246 | ||
| MCF7 | Growth Inhibition Assay | IC50=3.55 nM | 18566246 | ||
| PC-3 | Growth Inhibition Assay | IC50=2.51 nM | 18566246 | ||
| MMRU | Growth Inhibition Assay | IC50=2.57 nM | 18566246 | ||
| Hs68 | Growth Inhibition Assay | IC50=>10 nM | 18566246 | ||
| hMSC-001F | Growth Inhibition Assay | IC50=>10 nM | 18566246 | ||
| mammalian cells | Function assay | Inhibition of Histone deacetylase 4 in mammalian cells, IC50 = 0.51 μM. | 14584932 | ||
| mammalian cells | Function assay | Inhibition of Histone deacetylase 1 induced acetylated histone in mammalian cells., EC50 = 36 μM. | 14584932 | ||
| MCF7 | Growth inhibition assay | Growth inhibition of MCF7 cells, IC50 = 0.00075 μM. | 17958342 | ||
| LLC | Function assay | Inhibition of HDAC-mediated HIF-1alpha activity in mouse LLC cells, IC50 = 2 μM. | 22305612 | ||
| NCI-H522 | Growth inhibition assay | Growth inhibition of human NCI-H522 cells by sulforhodamine B colorimetric method, GI50 = 0.0018 μM. | 23313638 | ||
| LOXIMVI | Growth inhibition assay | Growth inhibition of human LOXIMVI cells by sulforhodamine B colorimetric method, GI50 = 0.0025 μM. | 23313638 | ||
| A549 | Growth inhibition assay | Growth inhibition of human A549 cells by sulforhodamine B colorimetric method, GI50 = 0.0026 μM. | 23313638 | ||
| OVCAR5 | Growth inhibition assay | Growth inhibition of human OVCAR5 cells by sulforhodamine B colorimetric method, GI50 = 0.0028 μM. | 23313638 | ||
| MKN74 | Growth inhibition assay | Growth inhibition of human MKN74 cells by sulforhodamine B colorimetric method, GI50 = 0.003 μM. | 23313638 | ||
| NCI-H460 | Growth inhibition assay | Growth inhibition of human NCI-H460 cells by sulforhodamine B colorimetric method, GI50 = 0.003 μM. | 23313638 | ||
| HCT116 | Growth inhibition assay | Growth inhibition of human HCT116 cells by sulforhodamine B colorimetric method, GI50 = 0.0031 μM. | 23313638 | ||
| HCC2998 | Growth inhibition assay | Growth inhibition of human HCC2998 cells by sulforhodamine B colorimetric method, GI50 = 0.0031 μM. | 23313638 | ||
| MKN1 | Growth inhibition assay | Growth inhibition of human MKN1 cells by sulforhodamine B colorimetric method, GI50 = 0.0032 μM. | 23313638 | ||
| SKOV3 | Growth inhibition assay | Growth inhibition of human SKOV3 cells by sulforhodamine B colorimetric method, GI50 = 0.0033 μM. | 23313638 | ||
| HT-29 | Growth inhibition assay | Growth inhibition of human HT-29 cells by sulforhodamine B colorimetric method, GI50 = 0.0033 μM. | 23313638 | ||
| KM12 | Growth inhibition assay | Growth inhibition of human KM12 cells by sulforhodamine B colorimetric method, GI50 = 0.0034 μM. | 23313638 | ||
| DMS114 | Growth inhibition assay | Growth inhibition of human DMS114 cells by sulforhodamine B colorimetric method, GI50 = 0.0036 μM. | 23313638 | ||
| SF539 | Growth inhibition assay | Growth inhibition of human SF539 cells by sulforhodamine B colorimetric method, GI50 = 0.0036 μM. | 23313638 | ||
| U251 | Growth inhibition assay | Growth inhibition of human U251 cells by sulforhodamine B colorimetric method, GI50 = 0.0039 μM. | 23313638 | ||
| SF295 | Growth inhibition assay | Growth inhibition of human SF295 cells by sulforhodamine B colorimetric method, GI50 = 0.004 μM. | 23313638 | ||
| MCF7 | Growth inhibition assay | Growth inhibition of human MCF7 cells by sulforhodamine B colorimetric method, GI50 = 0.0042 μM. | 23313638 | ||
| NCI-H23 | Growth inhibition assay | Growth inhibition of human NCI-H23 cells by sulforhodamine B colorimetric method, GI50 = 0.0046 μM. | 23313638 | ||
| OVCAR3 | Growth inhibition assay | Growth inhibition of human OVCAR3 cells by sulforhodamine B colorimetric method, GI50 = 0.0046 μM. | 23313638 | ||
| MKN7 | Growth inhibition assay | Growth inhibition of human MKN7 cells by sulforhodamine B colorimetric method, GI50 = 0.0049 μM. | 23313638 | ||
| SF268 | Growth inhibition assay | Growth inhibition of human SF268 cells by sulforhodamine B colorimetric method, GI50 = 0.0049 μM. | 23313638 | ||
| MDA-MB-231 | Growth inhibition assay | Growth inhibition of human MDA-MB-231 cells by sulforhodamine B colorimetric method, GI50 = 0.0055 μM. | 23313638 | ||
| OVCAR8 | Growth inhibition assay | Growth inhibition of human OVCAR8 cells by sulforhodamine B colorimetric method, GI50 = 0.0055 μM. | 23313638 | ||
| DMS273 | Growth inhibition assay | Growth inhibition of human DMS273 cells by sulforhodamine B colorimetric method, GI50 = 0.0058 μM. | 23313638 | ||
| DU145 | Growth inhibition assay | Growth inhibition of human DU145 cells by sulforhodamine B colorimetric method, GI50 = 0.006 μM. | 23313638 | ||
| RXF631L | Growth inhibition assay | Growth inhibition of human RXF631L cells by sulforhodamine B colorimetric method, GI50 = 0.0066 μM. | 23313638 | ||
| HBC4 | Growth inhibition assay | Growth inhibition of human HBC4 cells by sulforhodamine B colorimetric method, GI50 = 0.0069 μM. | 23313638 | ||
| SNB75 | Growth inhibition assay | Growth inhibition of human SNB75 cells by sulforhodamine B colorimetric method, GI50 = 0.0072 μM. | 23313638 | ||
| BSY1 | Growth inhibition assay | Growth inhibition of human BSY1 cells by sulforhodamine B colorimetric method, GI50 = 0.0085 μM. | 23313638 | ||
| NCI-H226 | Growth inhibition assay | Growth inhibition of human NCI-H226 cells by sulforhodamine B colorimetric method, GI50 = 0.0089 μM. | 23313638 | ||
| SNB78 | Growth inhibition assay | Growth inhibition of human SNB78 cells by sulforhodamine B colorimetric method, GI50 = 0.0096 μM. | 23313638 | ||
| HBC5 | Growth inhibition assay | Growth inhibition of human HBC5 cells by sulforhodamine B colorimetric method, GI50 = 0.013 μM. | 23313638 | ||
| MKN45 | Growth inhibition assay | Growth inhibition of human MKN45 cells by sulforhodamine B colorimetric method, GI50 = 0.014 μM. | 23313638 | ||
| MKN28 | Growth inhibition assay | Growth inhibition of human MKN28 cells by sulforhodamine B colorimetric method, GI50 = 0.017 μM. | 23313638 | ||
| PC3 | Growth inhibition assay | Growth inhibition of human PC3 cells by sulforhodamine B colorimetric method, GI50 = 0.018 μM. | 23313638 | ||
| ACHN | Growth inhibition assay | Growth inhibition of human ACHN cells by sulforhodamine B colorimetric method, GI50 = 0.02 μM. | 23313638 | ||
| OVCAR4 | Growth inhibition assay | Growth inhibition of human OVCAR4 cells by sulforhodamine B colorimetric method, GI50 = 0.02 μM. | 23313638 | ||
| St-4 | Growth inhibition assay | Growth inhibition of human St-4 cells by sulforhodamine B colorimetric method, GI50 = 0.022 μM. | 23313638 | ||
| HCT15 | Growth inhibition assay | Growth inhibition of human HCT15 cells by sulforhodamine B colorimetric method, GI50 = 0.45 μM. | 23313638 | ||
| NCI-H522 | Cytotoxicity assay | Cytotoxicity against human NCI-H522 cells by SRB assay, GI50 = 0.0018 μM. | 24589486 | ||
| LOXIMVI | Cytotoxicity assay | Cytotoxicity against human LOXIMVI cells by SRB assay, GI50 = 0.0025 μM. | 24589486 | ||
| A549 | Cytotoxicity assay | Cytotoxicity against human A549 cells by SRB assay, GI50 = 0.0026 μM. | 24589486 | ||
| OVCAR5 | Cytotoxicity assay | Cytotoxicity against human OVCAR5 cells by SRB assay, GI50 = 0.0028 μM. | 24589486 | ||
| NCI-H460 | Cytotoxicity assay | Cytotoxicity against human NCI-H460 cells by SRB assay, GI50 = 0.003 μM. | 24589486 | ||
| MKN74 | Cytotoxicity assay | Cytotoxicity against human MKN74 cells by SRB assay, GI50 = 0.003 μM. | 24589486 | ||
| HCC2998 | Cytotoxicity assay | Cytotoxicity against human HCC2998 cells by SRB assay, GI50 = 0.0031 μM. | 24589486 | ||
| HCT116 | Cytotoxicity assay | Cytotoxicity against human HCT116 cells by SRB assay, GI50 = 0.0031 μM. | 24589486 | ||
| MKN1 | Cytotoxicity assay | Cytotoxicity against human MKN1 cells by SRB assay, GI50 = 0.0032 μM. | 24589486 | ||
| HT-29 | Cytotoxicity assay | Cytotoxicity against human HT-29 cells by SRB assay, GI50 = 0.0033 μM. | 24589486 | ||
| SKOV3 | Cytotoxicity assay | Cytotoxicity against human SKOV3 cells by SRB assay, GI50 = 0.0033 μM. | 24589486 | ||
| KM12 | Cytotoxicity assay | Cytotoxicity against human KM12 cells by SRB assay, GI50 = 0.0034 μM. | 24589486 | ||
| SF539 | Cytotoxicity assay | Cytotoxicity against human SF539 cells by SRB assay, GI50 = 0.0036 μM. | 24589486 | ||
| DMS114 | Cytotoxicity assay | Cytotoxicity against human DMS114 cells by SRB assay, GI50 = 0.0036 μM. | 24589486 | ||
| U251 | Cytotoxicity assay | Cytotoxicity against human U251 cells by SRB assay, GI50 = 0.0039 μM. | 24589486 | ||
| SF295 | Cytotoxicity assay | Cytotoxicity against human SF295 cells by SRB assay, GI50 = 0.004 μM. | 24589486 | ||
| MCF7 | Cytotoxicity assay | Cytotoxicity against human MCF7 cells by SRB assay, GI50 = 0.0042 μM. | 24589486 | ||
| OVCAR3 | Cytotoxicity assay | Cytotoxicity against human OVCAR3 cells by SRB assay, GI50 = 0.0046 μM. | 24589486 | ||
| NCI-H23 | Cytotoxicity assay | Cytotoxicity against human NCI-H23 cells by SRB assay, GI50 = 0.0046 μM. | 24589486 | ||
| SF268 | Cytotoxicity assay | Cytotoxicity against human SF268 cells by SRB assay, GI50 = 0.0049 μM. | 24589486 | ||
| MKN7 | Cytotoxicity assay | Cytotoxicity against human MKN7 cells by SRB assay, GI50 = 0.0049 μM. | 24589486 | ||
| OVCAR8 | Cytotoxicity assay | Cytotoxicity against human OVCAR8 cells by SRB assay, GI50 = 0.0055 μM. | 24589486 | ||
| MDA-MB-231 | Cytotoxicity assay | Cytotoxicity against human MDA-MB-231 cells by SRB assay, GI50 = 0.0055 μM. | 24589486 | ||
| DMS273 | Cytotoxicity assay | Cytotoxicity against human DMS273 cells by SRB assay, GI50 = 0.0058 μM. | 24589486 | ||
| DU145 | Cytotoxicity assay | Cytotoxicity against human DU145 cells by SRB assay, GI50 = 0.006 μM. | 24589486 | ||
| RXF631L | Cytotoxicity assay | Cytotoxicity against human RXF631L cells by SRB assay, GI50 = 0.0066 μM. | 24589486 | ||
| HBC4 | Cytotoxicity assay | Cytotoxicity against human HBC4 cells by SRB assay, GI50 = 0.0069 μM. | 24589486 | ||
| SNB75 | Cytotoxicity assay | Cytotoxicity against human SNB75 cells by SRB assay, GI50 = 0.0072 μM. | 24589486 | ||
| BSY1 | Cytotoxicity assay | Cytotoxicity against human BSY1 cells by SRB assay, GI50 = 0.0085 μM. | 24589486 | ||
| NCI-H226 | Cytotoxicity assay | Cytotoxicity against human NCI-H226 cells by SRB assay, GI50 = 0.0089 μM. | 24589486 | ||
| SNB78 | Cytotoxicity assay | Cytotoxicity against human SNB78 cells by SRB assay, GI50 = 0.0096 μM. | 24589486 | ||
| HBC5 | Cytotoxicity assay | Cytotoxicity against human HBC5 cells by SRB assay, GI50 = 0.013 μM. | 24589486 | ||
| MKN45 | Cytotoxicity assay | Cytotoxicity against human MKN45 cells by SRB assay, GI50 = 0.014 μM. | 24589486 | ||
| MKN28 | Cytotoxicity assay | Cytotoxicity against human MKN28 cells by SRB assay, GI50 = 0.017 μM. | 24589486 | ||
| PC3 | Cytotoxicity assay | Cytotoxicity against human PC3 cells by SRB assay, GI50 = 0.018 μM. | 24589486 | ||
| ACHN | Cytotoxicity assay | Cytotoxicity against human ACHN cells by SRB assay, GI50 = 0.02 μM. | 24589486 | ||
| OVCAR4 | Cytotoxicity assay | Cytotoxicity against human OVCAR4 cells by SRB assay, GI50 = 0.02 μM. | 24589486 | ||
| St-4 | Cytotoxicity assay | Cytotoxicity against human St-4 cells by SRB assay, GI50 = 0.022 μM. | 24589486 | ||
| HCT15 | Cytotoxicity assay | Cytotoxicity against human HCT15 cells by SRB assay, GI50 = 0.45 μM. | 24589486 | ||
| 点击查看更多细胞系数据 | |||||
生物活性
| 产品描述 | Romidepsin (FK228, Depsipeptide, FR 901228, NSC 630176)是一种有效的HDAC1和HDAC2抑制剂，无细胞试验中IC50分别为36 nM和47 nM。Romidepsin (FK228/depsipeptide) 在神经母细胞瘤肿瘤细胞中可控制生长并诱导凋亡。 | ||||
|---|---|---|---|---|---|
| 特性 | Romidepsin对I型HDAC的抑制作用明显强于对II型HDAC的抑制。 | ||||
| 靶点 |
|
| 体外研究(In Vitro) | ||||
| 体外研究活性 | Romidepsin抑制NSCLC细胞系生长，IC50范围从1.3 ng/mL到4.9 ng/mL。 Romidepsin可以降低Erlotinib对NSCLC细胞系的IC50值， 增加NSCLC细胞系对Erlotinib的敏感性[1]。Romidepsin处理72小时可以抑制6/6 人 NB 肿瘤细胞系的生长，而 NIH3T3细胞系并不受影响。 Romidepsin对于单拷贝或N-myc 多拷贝的NB细胞系以及含有正常或突变的p53 和含有Alk突变体的细胞系都有选择性的细胞毒性，这种毒性具有剂量依赖的特性。[2] | |||
|---|---|---|---|---|
| 细胞实验 | 细胞系 | NCI-H1975, NCI-H157, NCI-2882, NCI-H460 和 HCC95 细胞系 | ||
| 浓度 | 1 ng/mL | |||
| 孵育时间 | 72 小时 | |||
| 方法 | 使用MTS法分析药物敏感性。在96孔平板中每孔接种2×103个细胞(包括NCI-H1975, NCI-H157, NCI-2882, NCI-H460和HCC95) 。24小时后, 在存在或者缺少1 ng/mL Romidepsin的条件下将细胞与不同浓度 (0.01 µM - 250 µM) 的Erlotinib 37°C 孵育72 小时。 MTS 溶液加到每个孔中37°C孵育1小时。利用分光光度计测量490 nm 处的光密度值。每种药物浓度的实验都设置8个复孔并重复两次。基于细胞生存曲线的吸光度值计算药物的半抑制浓度 (IC50) 。 | |||
| 实验图片 | 检测方法 | 检测指标 | 实验图片 | PMID |
| Western blot | p21 / Cyclin D1 AcH3(K9) / Ac-α-Tubulin(K40) / Ac-NFκB2(K310) p65 / 3MeH3(K27) HDAC3 / HDAC4 / HDAC6 / HDAC2 γH2AX / PARP1 / Cleaved caspase3 / BAK / p21(waf1/cip1) / XIAP Cyclin E1 / BRCA1 / E2F1 / Cleaved PARP / H3Ac pAKT(S473) / pAKT(T308) / AKT |
|
19682393 | |
| Growth inhibition assay | Cell viability |
|
27444036 | |
| Immunofluorescence | SS18/TLE1 Cleaved caspase-3 |
|
27120803 | |
| 体内研究(In Vivo) | ||
| 体内研究活性 | 与PBS处理的对照组相比，单独使用Erlotinib 和 Romidepsin分别可以对NCI-H1299细胞系的异种移植生长抑制到72% 和 43% ，但是并不具有明显的统计学意义。只有当两种药物联用的时候才会对其生长造成明显的抑制作用，此时生长被抑制到28% [1]。在免疫功能低下的小鼠中，Romidepsin 会抑制皮下NB 异种移植的生长，这种抑制作用具有剂量依赖的特性 。此外, 在NB病人的肿瘤组织中Romidepsin 会诱导某些基因的表达，如 p21 和p75 以及NTRK (TrkA) [2]。 | |
|---|---|---|
| 动物实验 | Animal Models | 携带NCI-H1299 细胞的 BALB/c无胸腺裸小鼠 |
| Dosages | 1.2 mg/kg | |
| Administration | 腹腔注射 | |
| NCT Number | Recruitment | Conditions | Sponsor/Collaborators | Start Date | Phases |
|---|---|---|---|---|---|
| NCT03770000 | Completed | T Cell Lymphoma |
Rhizen Pharmaceuticals SA |
March 12 2019 | Phase 1|Phase 2 |
| NCT02616965 | Active not recruiting | Cutaneous T-cell Lymphoma (CTCL) |
Fox Chase Cancer Center|Seagen Inc.|Celgene Corporation |
February 22 2017 | Phase 1 |
| NCT02616874 | Completed | HIV |
IrsiCaixa|Germans Trias i Pujol Hospital|Fundación FLS de Lucha Contra el Sida las Enfermedades Infecciosas y la Promoción de la Salud y la Ciencia|Hospital Clinic of Barcelona|Hospital de Sant Pau|HIVACAT|University of Oxford|BCN Checkpoint |
February 2016 | Phase 1 |
化学信息&溶解度
| 分子量 | 540.7 | 分子式 | C24H36N4O6S2 |
| CAS号 | 128517-07-7 | SDF | -- |
| Smiles | CC=C1C(=O)NC(C(=O)OC2CC(=O)NC(C(=O)NC(CSSCCC=C2)C(=O)N1)C(C)C)C(C)C | ||
| 储存条件(自收到货起) | |||
|
体外溶解度 |
DMSO : 100 mg/mL ( (184.94 mM) ；DMSO吸湿会降低化合物溶解度，请使用新开封DMSO) Water : Insoluble Ethanol : Insoluble |
摩尔浓度计算器 |
|
体内溶解度 现配现用，请按从左到右的顺序依次添加，澄清后再加入下一溶剂 |
动物体内配方计算器 | ||||
实验计算
动物体内配方计算器（澄清溶液）
第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量）
mg/kg
g
μL
只
第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系Selleck为您提供正确的澄清溶液配方）
% DMSO
%
% Tween 80
% ddH2O
%DMSO
%
计算结果：
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于μL DMSO溶液（母液浓度mg/mL，注：如该浓度超过该批次药物DMSO溶解度，请先联系Selleck）；
体内配方配制方法：取μL DMSO母液，加入μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入μL ddH2O，混匀澄清。
体内配方配制方法：取μL DMSO母液，加入μL Corn oil，混匀澄清。
注意：1. 首先保证母液是澄清的；
2.一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
技术支持
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