Tubastatin A
Tubastatin A 是一种有效的，选择性HDAC6抑制剂，无细胞试验中IC50为15 nM，选择性远高于所有其他同工酶(1000倍)除了HDAC8(57倍)。Tubastatin A 可促进自噬并增加凋亡。
Tubastatin A Chemical Structure
CAS: 1252003-15-8
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纯度：
99.63%
99.63
Tubastatin A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 |
|---|---|---|---|---|---|
| KB | Function assay | 14 uM | 24 hrs | Inhibition of HDAC1 in human KB cells assessed as increase in histone H4 acetylation at 14 uM after 24 hrs by Western blotting analysis | 25899338 |
| KMS-12-BM | Function assay | 15 uM | up to 48 hrs | Inhibition of HDAC6 in human KMS-12-BM cells assessed as increase in acetylated tubulin level at 15 uM up to 48 hrs by immunoblot method | 27541357 |
| MOLM14 | Function assay | 15 uM | up to 48 hrs | Inhibition of HDAC6 in human MOLM14 cells assessed as increase in acetylated tubulin level at 15 uM up to 48 hrs by immunoblot method | 27541357 |
| U937 | Function assay | 2 uM | 18 hrs | Inhibition of HDAC6 in human U937 cells assessed as increase in alpha-tubulin acetylation at Lys-40 residue at 2 uM after 18 hrs by Western blot method | 28337317 |
| HEL | Cell cycle assay | 1 to 5 uM | 48 hrs | Cell cycle arrest in human HEL cells assessed as accumulation at G1 phase at 1 to 5 uM after 48 hrs propidium iodide staining based flow cytometry | 29940115 |
| HeLa | Function assay | 2 uM | 12 hrs | Inhibition of HDAC6 in human HeLa cells assessed as increase in acetyl-tubulin level at 2 uM after 12 hrs by Western blot analysis | 29533873 |
| HEK293 | Function assay | 10 uM | 24 hrs | Inhibition of HDAC1 in HEK293 cells assessed as increase in histone H3 acetylation at 10 uM after 24 hrs by Western blot method | 28523102 |
| MV4-11 | Function assay | 200 nM | 24 hrs | Inhibition of HDAC6 in human MV4-11 cells assessed as accumulation of acetylated alpha-tubulin at 200 nM after 24 hrs by Western blot analysis | 29738953 |
| HCT116 | Cell cycle assay | 5 uM | 48 hrs | Cell cycle arrest in human HCT116 cells assessed as accumulation at sub-G1 phase at 5 uM after 48 hrs by propidium iodide staining-based flow cytometric method | 28038324 |
| PC12 | Neuroprotective assay | 10 uM | 24 hrs | Neuroprotective activity against H2O2-induced toxicity in rat PC12 cells assessed as cell viability at 10 uM pretreated for 24 hrs followed by H2O2 challenge and measured after 12 hrs by MTT assay relative to control | 30385227 |
| PC12 | Neuroprotective assay | 5 uM | 24 hrs | Neuroprotective activity against 6-OHDA-induced toxicity in rat PC12 cells assessed as increase in cell viability at 5 uM pretreated for 24 hrs followed by 6-OHDA challenge and measured after 12 hrs by MTT assay | 30385227 |
| PC12 | Neuroprotective assay | 10 uM | 24 hrs | Neuroprotective activity against 6-OHDA-induced toxicity in rat PC12 cells assessed as increase in cell viability at 10 uM pretreated for 24 hrs followed by 6-OHDA challenge and measured after 12 hrs by MTT assay | 30385227 |
| PC12 | Neuroprotective assay | 5 to 10 uM | 24 hrs | Neuroprotective activity against 6-OHDA-induced toxicity in rat PC12 cells assessed as increase in cell viability at 5 to 10 uM pretreated for 24 hrs followed by 6-OHDA challenge and measured after 12 hrs coincubated with ebselen by MTT assay | 30385227 |
| PC12 | Antioxidant assay | 5 uM | 24 hrs | Antioxidant activity against H2O2-induced oxidative stress in rat PC12 cells assessed as decrease in ROS accumulation at 5 uM preincubated for 24 hrs followed by H2O2 challenge and measured after 12 hrs by DCFH-DA dye-based fluorescence analysis | 30385227 |
| PC12 | Antioxidant assay | 5 uM | 24 hrs | Antioxidant activity against H2O2-induced oxidative stress in rat PC12 cells assessed as decrease in ROS accumulation at 5 uM preincubated for 24 hrs followed by H2O2 challenge and measured after 12 hrs coincubated with ebselen by DCFH-DA dye-based fluore | 30385227 |
| Sf9 | Function assay | 30 mins | Inhibition of full length human recombinant N-terminal GST-tagged HDAC6 expressed in baculovirus infected sf9 cells using fluorogenic HDAC substrate 3 after 30 mins by fluorescence assay, IC50 = 0.013 μM. | 29549837 | |
| Sf9 | Function assay | 2 hrs | Inhibition of full length human recombinant N-terminal GST-tagged HDAC6 (1 to 1215 residues) expressed in sf9 cells preincubated with enzyme followed by fluorogenic Arg-His-Lys-Lys(Ac)-AMC substrate addition measured after 2 hrs by fluorescence assay, IC50 = 0.0035 μM. | 27541357 | |
| Sf9 | Function assay | 90 mins | Inhibition of full length human recombinant N-terminal GST-tagged HDAC6 expressed in Sf9 cells using RHKK(Ac) as substrate after 90 mins by fluorimetric method, IC50 = 0.0137 μM. | 28038324 | |
| Sf9 | Function assay | 2 hrs | Inhibition of human recombinant HDAC6 expressed in Sf9 cells incubated for 2 hrs using RHKK-Ac fluorogenic substrate, IC50 = 0.015 μM. | 23009203 | |
| Sf9 | Function assay | 90 mins | Inhibition of human recombinant N-terminal GST-tagged full length HDAC6 expressed in insect SF9 cells using fluorogenic ZMAL as substrate after 90 mins by fluorescence-based assay, IC50 = 0.0304 μM. | 30092367 | |
| HeLaS3 | Function assay | 15 mins | Inhibition of HDAC6 in human HeLaS3 cells preincubated for 15 mins followed by HDAC-Glo substrate addition measured after 30 to 45 mins by ELISA, IC50 = 0.031 μM. | 28337317 | |
| insect cells | Function assay | 4 hrs | Inhibition of human recombinant HDAC6 expressed in baculovirus infected insect cells using BATCP as substrate after 4 hrs by UHPLC-ESI-MS/MS analysis, IC50 = 0.0349 μM. | 27650925 | |
| SHSY5Y | Function assay | 8 hrs | Inhibition of HDAC6 in human SHSY5Y cells using BATCP as substrate after 8 hrs by UHPLC-ESI-MS/MS analysis, IC50 = 0.0943 μM. | 27650925 | |
| SHSY5Y | Function assay | 8 hrs | Inhibition of HDAC in human SHSY5Y cells using MAL as substrate after 8 hrs by UHPLC-ESI-MS/MS analysis, IC50 = 0.1221 μM. | 27650925 | |
| Sf9 | Function assay | 4 hrs | Inhibition of full length human recombinant C-terminal FLAG/His-tagged HDAC1 expressed in baculovirus infected sf9 cells using fluorogenic HDAC substrate 3 after 4 hrs fluorescence assay, IC50 = 0.718 μM. | 29549837 | |
| Sf9 | Function assay | 1 hr | Inhibition of full length human recombinant C-terminal FLAG/His-tagged HDAC1 expressed in baculovirus infected sf9 cells using fluorogenic HDAC substrate 3 after 1 hr fluorescence assay, IC50 = 0.967 μM. | 29549837 | |
| SHSY5Y | Function assay | 8 hrs | Inhibition of HDAC1 in human SHSY5Y cells using MOCPAC as substrate after 8 hrs by UHPLC-ESI-MS/MS analysis, IC50 = 1.1097 μM. | 27650925 | |
| Sf9 | Function assay | 30 mins | Inhibition of full length human recombinant C-terminal FLAG/His-tagged HDAC1 expressed in baculovirus infected sf9 cells using fluorogenic HDAC substrate 3 after 30 mins by fluorescence assay, IC50 = 1.54 μM. | 29549837 | |
| Sf9 | Function assay | 90 mins | Inhibition of human recombinant C-terminal His/FLAG-tagged full length HDAC1 expressed in insect SF9 cells using fluorogenic ZMAL as substrate after 90 mins by fluorescence-based assay, IC50 = 1.91 μM. | 30092367 | |
| HCT116 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human HCT116 cells after 72 hrs by MTT assay, IC50 = 2 μM. | 27541357 | |
| Sf9 | Function assay | 30 mins | Inhibition of full length human recombinant C-terminal His-tagged HDAC3/N-terminal GST-tagged NCOR2 (95 to 489 residues) expressed in baculovirus infected sf9 cells using fluorogenic HDAC substrate 3 after 30 mins by fluorescence assay, IC50 = 2.26 μM. | 29549837 | |
| HeLa | Function assay | 6 hrs | Inhibition of HDAC6 in human HeLa cells assessed as reduction in K40 hyperacetylation of alpha-tubulin incubated for 6 hrs by immunofluorescence assay, IC50 = 2.5 μM. | 25454270 | |
| HL60 | Antiproliferative assay | 48 hrs | Antiproliferative activity against human HL60 cells after 48 hrs in presence of JAK2 inhibitor CYT-387 by CCK-8 assay, IC50 = 2.54 μM. | 29940115 | |
| K562 | Antiproliferative assay | 48 hrs | Antiproliferative activity against human K562 cells after 48 hrs in presence of JAK2 inhibitor CYT-387 by CCK-8 assay, IC50 = 2.54 μM. | 29940115 | |
| HEL | Antiproliferative assay | 48 hrs | Antiproliferative activity against human HEL cells after 48 hrs in presence of JAK2 inhibitor CYT-387 by CCK-8 assay, IC50 = 2.54 μM. | 29940115 | |
| HeLaS3 | Function assay | 15 mins | Inhibition of HDAC1 in human HeLaS3 cells preincubated for 15 mins followed by HDAC-Glo substrate addition measured after 30 to 45 mins by ELISA, IC50 = 2.7 μM. | 28337317 | |
| HeLaS3 | Function assay | 15 mins | Inhibition of HDAC3 in human HeLaS3 cells preincubated for 15 mins followed by HDAC-Glo substrate addition measured after 30 to 45 mins by ELISA, IC50 = 2.9 μM. | 28337317 | |
| Jurkat | Cytotoxicity assay | 72 hrs | Cytotoxicity against human Jurkat cells assessed as growth inhibition after 72 hrs by MTS assay, IC50 = 3.38 μM. | 24304348 | |
| MCF7 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human MCF7 cells after 72 hrs by MTT assay, IC50 = 3.7 μM. | 27541357 | |
| HL60 | Antiproliferative assay | 48 hrs | Antiproliferative activity against human HL60 cells after 48 hrs by CCK-8 assay, IC50 = 3.75 μM. | 29940115 | |
| K562 | Antiproliferative assay | 48 hrs | Antiproliferative activity against human K562 cells after 48 hrs by CCK-8 assay, IC50 = 3.75 μM. | 29940115 | |
| HEL | Antiproliferative assay | 48 hrs | Antiproliferative activity against human HEL cells after 48 hrs by CCK-8 assay, IC50 = 3.75 μM. | 29940115 | |
| HeLaS3 | Function assay | 15 mins | Inhibition of HDAC2 in human HeLaS3 cells preincubated for 15 mins followed by HDAC-Glo substrate addition measured after 30 to 45 mins by ELISA, IC50 = 3.9 μM. | 28337317 | |
| CAL27 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human CAL27 cells measured after 72 hrs by MTT assay, IC50 = 4.6 μM. | 28581289 | |
| PC3 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human PC3 cells after 72 hrs by MTT assay, IC50 = 8.6 μM. | 27541357 | |
| Sf9 | Function assay | 30 mins | Inhibition of full length human recombinant C-terminal His-tagged HDAC2 expressed in baculovirus infected sf9 cells using fluorogenic HDAC substrate 3 after 30 mins by fluorescence assay, IC50 = 9.97 μM. | 29549837 | |
| MDA-MB-231 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human MDA-MB-231 cells after 72 hrs by MTT assay, IC50 = 10.4 μM. | 27541357 | |
| Cal27CisR | Antiproliferative assay | 72 hrs | Antiproliferative activity against human Cal27CisR cells measured after 72 hrs by MTT assay, IC50 = 10.8 μM. | 28581289 | |
| LNCAP | Cytotoxicity assay | 72 hrs | Cytotoxicity against androgen-dependent human LNCAP cells assessed as growth inhibition after 72 hrs by MTS assay, IC50 = 10.88 μM. | 24304348 | |
| Cal27CisR | Function assay | 18 hrs | Inhibition of HDAC in human Cal27CisR cells using Boc-Lys(epsilon-Ac)-AMC as substrate preincubated for 18 hrs followed by substrate addition measured after 3 hrs by fluorescence assay, IC50 = 12.1 μM. | 28581289 | |
| KB | Cytotoxicity assay | 72 hrs | Cytotoxicity against human KB cells after 72 hrs by MTS assay, IC50 = 14.81 μM. | 25899338 | |
| THLE2 | Cytotoxicity assay | 72 hrs | Cytotoxicity against human THLE2 cells after 72 hrs by vialight cell proliferation assay, LC50 = 15.1 μM. | 29549837 | |
| CAL27 | Function assay | 18 hrs | Inhibition of HDAC in human CAL27 cells using Boc-Lys(epsilon-Ac)-AMC as substrate preincubated for 18 hrs followed by substrate addition measured after 3 hrs by fluorescence assay, IC50 = 16.1 μM. | 28581289 | |
| Sf9 | Function assay | 2 hrs | Inhibition of human recombinant HDAC1 expressed in Sf9 cells incubated for 2 hrs using RHKK-Ac fluorogenic substrate, IC50 = 16.4 μM. | 23009203 | |
| B16 | Growth inhibition assay | 48 hrs | Growth inhibition of mouse B16 cells incubated for 48 hrs by MTT assay, GI50 = 40.5 μM. | 23009203 | |
| LNCAP | Function assay | 24 hrs | Inhibition of HDAC6 in human LNCAP cells assessed as inhibition of DHT-induced alpha-tubulin deacetylation by measuring increase in alpha-tubulin acetylation measured after 24 hrs relative to control | 27717544 | |
| human | Function assay | 24 hrs | Antagonist activity at AR in human LNCAP cells assessed as suppression of DHT-induced AR protein level measured after 24 hrs relative to control | 27717544 | |
| PC12 | Cytoprotective assay | 24 hrs | Cytoprotective activity against H2O2-induced damage in rat PC12 cells assessed as decrease in ROS accumulation preincubated for 24 hrs followed by H2O2 challenge measured after 12 hrs by DCFH-DA dye-based fluorescence analysis | 30385227 | |
| PC12 | Cytoprotective assay | 24 hrs | Cytoprotective activity against H2O2-induced damage in rat PC12 cells assessed as decrease in ROS accumulation preincubated for 24 hrs followed by H2O2 challenge measured after 12 hrs by DCFH-DA dye-based inverted fluorescence microscopic analysis | 30385227 | |
| Sf9 | Function assay | Inhibition of full length human recombinant N-terminal GST-tagged HDAC6 (1 to 1215 residues) expressed in sf9 cells using RHK-K(Ac)-AMC as substrate by fluorescence assay, IC50 = 0.011 μM. | 27541357 | ||
| Sf9 | Function assay | Inhibition of human recombinant HDAC6 expressed in baculovirus/sf9 cells using RHKKAc as substrate, IC50 = 0.015 μM. | 23905680 | ||
| Sf9 | Function assay | Inhibition of human recombinant HDAC8 expressed in baculovirus/sf9 cells using RHKAcKAc as substrate, IC50 = 0.854 μM. | 23905680 | ||
| HCT116 | Antiproliferative assay | Antiproliferative activity against human HCT116 cells, IC50 = 2 μM. | 29945795 | ||
| MCF7 | Antiproliferative assay | Antiproliferative activity against human MCF7 cells, IC50 = 3.7 μM. | 29945795 | ||
| PC3 | Antiproliferative assay | Antiproliferative activity against human PC3 cells, IC50 = 8.6 μM. | 29945795 | ||
| MDA-MB-231 | Antiproliferative assay | Antiproliferative activity against human MDA-MB-231 cells, IC50 = 10.4 μM. | 29945795 | ||
| Sf9 | Function assay | Inhibition of human recombinant HDAC1 expressed in baculovirus/sf9 cells using RHKKAc as substrate, IC50 = 16.4 μM. | 23905680 | ||
| DAOY | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY cells | 29435139 | ||
| SJ-GBM2 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells | 29435139 | ||
| A673 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells | 29435139 | ||
| SK-N-MC | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells | 29435139 | ||
| BT-37 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells | 29435139 | ||
| NB-EBc1 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells | 29435139 | ||
| U-2 OS | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for U-2 OS cells | 29435139 | ||
| Saos-2 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells | 29435139 | ||
| SK-N-SH | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH cells | 29435139 | ||
| NB1643 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells | 29435139 | ||
| LAN-5 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells | 29435139 | ||
| Rh18 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh18 cells | 29435139 | ||
| OHS-50 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells | 29435139 | ||
| RD | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells | 29435139 | ||
| Rh30 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh30 cells | 29435139 | ||
| Rh41 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh41 cells | 29435139 | ||
| 点击查看更多细胞系数据 | |||||
生物活性
| 产品描述 | Tubastatin A 是一种有效的，选择性HDAC6抑制剂，无细胞试验中IC50为15 nM，选择性远高于所有其他同工酶(1000倍)除了HDAC8(57倍)。Tubastatin A 可促进自噬并增加凋亡。 | ||
|---|---|---|---|
| 靶点 |
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| 体外研究(In Vitro) | ||||
| 体外研究活性 | Tubastatin A选择性作用于所有同工酶除了HDAC8，对所有亚型不含HDAC8，保持超过1000倍的选择性，对HDAC8具有约57倍的选择性。2.5 μM Tubastatin A优先诱导α-tubulin 高度乙酰化。10 μM Tubastatin A轻微诱导组蛋白乙酰化。Tubastatin A 5 μM开始对同型半胱氨酸诱导的神经元细胞死亡具有保护作用，这种作用具有剂量依赖性，10 μM时，达到完全保护。[1]Tubastatin A (10 μM) 作用于胆管癌细胞系，诱导乙酰化的α-tubulin水平增加，和初级纤毛表达的恢复，初级纤毛表达的恢复与下调Hedgehog (Hh)和MAPK信号通路，以及减少细胞增殖率（平均50％）和浸润（40％）相关。[2]Tubastatin A作用于LPS刺激的人类 THP-1巨噬细胞，显著抑制TNF-α和IL-6，IC50分别为272 nM 和 712 nM。Tubastatin A作用于小鼠Raw 264.7巨噬细胞，抑制一氧化氮（NO）分泌，这种作用具有剂量依赖性，IC50为4.2 μM。[3] | |||
|---|---|---|---|---|
| 激酶实验 | HDAC酶试验 | |||
| Tubastatin A在实验 Buffer(50 mM HEPES, pH 7.4, 100 mM KCl, 0.001% Tween-20, 0.05% BSA，和 20 μM tris(2-carboxyethyl)phosphine) 中溶解和稀释到终浓度的6倍。HDAC酶在实验 Buffer 中稀释到终浓度的1.5倍，与Tubastatin A预温育10分钟，然后加入底物。 通过滴定曲线测得，用于每种酶的FTS(HDAC1, HDAC2, HDAC3, 和HDAC6) 或 MAZ-1675 (HDAC4, HDAC5, HDAC7, HDAC8, 和 HDAC9)量等于米氏常数(Km)。使用0.3 μM测序级胰蛋白酶将FTS或MAZ-1675在实验 Buffer中稀释到终浓度的6倍。底物/胰蛋白酶混合物加入到酶/化合物混合物中，震荡实验板60秒，然后置于SpectraMax M5酶标仪上。赖氨酸侧链在肽底物中脱乙酰化后，监测酶促反应的7-amino-4-methoxy-coumarin释放，监测30分钟，计算反应的线性速率。 | ||||
| 细胞实验 | 细胞系 | 人体胆管癌细胞系HuCCT-1 | ||
| 浓度 | ~10 μM | |||
| 孵育时间 | 21 天 | |||
| 方法 | 细胞生长在软琼脂中，测评锚定非依赖性生长。约25,000个细胞悬浮在培养基的0.4％琼脂中，超过1％琼脂层在6孔板中。每周加入两次培养基，温育21天，拍摄图片。使用Gel-Pro软件分析菌落的数量和尺寸。 |
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| 实验图片 | 检测方法 | 检测指标 | 实验图片 | PMID |
| Western blot | EGFR / p-AKT / AKT / p-ERK / ERK |
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29665050 | |
| Immunofluorescence | α-tubulin / Acetylated tubulin HDAC6 |
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23798680 | |
| 体内研究(In Vivo) | ||
| 体内研究活性 | Tubastatin A降低体内胆管癌的生长。Tubastatin A(10 mg/kg)处理同基因大鼠原位胆管癌模型，诱导低于平均瘤重6倍，降低肿瘤重量与肝脏重量和体重（分别为5和5.6倍）的比值。Tubastatin A 处理肿瘤，与对照组相比，显著降低PCNA阳性细胞的量(34% vs 65%)。[2]Tubastat A按30 mg/kg剂量腹腔注射给药弗氏完全佐剂（FCA）诱导的动物炎症模型，显著抑制鼠爪体积。Tubastat A(30 mg/kg 腹腔注射)处理胶原诱导型关节炎DBA1小鼠的爪子组织，显著降低临床评分（〜70％），和IL-6表达。[3] | |
|---|---|---|
| 动物实验 | Animal Models | 携带胆管癌移植瘤BDEneu的大鼠 |
| Dosages | 10 mg/kg | |
| Administration | 每天腹腔注射 | |
化学信息&溶解度
| 分子量 | 335.4 | 分子式 | C20H21N3O2 |
| CAS号 | 1252003-15-8 | SDF | Download Tubastatin A SDF |
| Smiles | CN1CCC2=C(C1)C3=CC=CC=C3N2CC4=CC=C(C=C4)C(=O)NO | ||
| 储存条件(自收到货起) | |||
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体外溶解度 |
DMSO : 16.7 mg/mL ( (49.79 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 |
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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。
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常见问题及建议解决方法
问题 1:
We are planning to order some tubastatin A but I found out there are two versions of it. One has HCl and one does not. Which one do you recommend for live cell use? Will the HCl containing version significantly change the pH?
回答：
S8049 and S2627 have same molecular structure. The only difference is S2627 containing HCl and has higher solubility in DMSO (74 mg/mL vs. S8049 9 mg/mL). Since they are the same molecule, the biological function should be similar. I would recommend to use S2627 for cell culture study.
问题 2:
What’s the vehicle do you recommend to dissolve the compound for in vivo experiments?
回答：
S8049 Tubastatin A can be dissolved in 2% DMSO/30% PEG 300/PBS at 2.5 mg/mL as a clear solution, and it is also a clear solution in 2% DMSO/ corn oil at 2.5 mg/mL. The drug in 2% DMSO/0.5% Tween 80/PBS is a homogeneous suspension at 2.5 mg/mL at first. After stay for a while, the precipitation goes out at the bottom of the tube.
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