CAY10603
别名: BML-281
CAY10603 (BML-281)是一种强效的选择性HDAC6抑制剂，IC50为2 pM，选择性比其它HDACs高200多倍。
CAY10603 Chemical Structure
CAS: 1045792-66-2
产品质控
批次：
S759601
DMSO]89 mg/mL]false]Ethanol]5 mg/mL]false]Water]Insoluble]false
纯度：
99.85%
99.85
CAY10603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 |
|---|---|---|---|---|---|
| human SU.86.86 cells | Proliferation assay | 72 h | Antiproliferative activity against human SU.86.86 cells after 72 hrs by MTT assay, IC50=0.6 μM | 18642892 | |
| HPDE 6c7 cells | Cytotoxicity assay | 72 h | Cytotoxicity against HPDE 6c7 cells after 72 hrs by MTT assay, IC50=0.5 μM | 18642892 | |
| human HupT3 cells | Proliferation assay | 72 h | Antiproliferative activity against human HupT3 cells after 72 hrs by MTT assay, IC50=0.3 μM | 18642892 | |
| human MiaPaca2 cells | Proliferation assay | 72 h | Antiproliferative activity against human MiaPaca2 cells after 72 hrs by MTT assay, IC50=0.1 μM | 18642892 | |
| human Panc04.03 cells | Proliferation assay | 72 h | Antiproliferative activity against human Panc04.03 cells after 72 hrs by MTT assay, IC50=0.1 μM | 18642892 | |
| human BxPC3 cells | Proliferation assay | 72 h | Antiproliferative activity against human BxPC3 cells after 72 hrs by MTT assay, IC50=1 μM | 18642892 | |
| HMEC | Cytotoxicity assay | 72 h | Cytotoxicity against HMEC after 72 hrs by MTT assay, IC50=1 μM | 18642892 | |
| sf9 | Function assay | 5 to 10 mins | Inhibition of recombinant full length C-terminal His/FLAG tagged human HDAC1 (1 to 482 residues) expressed in baculovirus infected sf9 insect cells using p53 (379 to 382 residues) derived fluorogenic peptide RHKKAc as substrate preincubated for 5 to 10 mins, IC50=0.0032μM. | 31414801 | |
| sf9 | Function assay | 5 to 10 mins | Inhibition of recombinant N-terminal GST-tagged human HDAC6 (1 to 1215 residues) expressed in baculovirus infected sf9 insect cells using p53 (379 to 382 residues) derived fluorogenic peptide RHKKAc as substrate preincubated for 5 to 10 mins, IC50=0.0138μM. | 31414801 | |
| HeLa | Function assay | 2 hrs | Inhibition of dye-labeled tracer binding to HDAC10 (unknown origin) transfected in human HeLa cells measured after 2 hrs by nano-luciferase reporter gene-based BRET assay, IC50=0.79433μM. | 30964290 | |
| MV4-11 | Function assay | 1 hr | Binding affinity to HDAC6 in human MV4-11 cells assessed as increase in cellular protein stabilization at 1 uL preincubated for 1 hr followed by heating at 52 degree C for 3.5 mins by CETSA | 32212730 | |
| TC32 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for TC32 cells | 29435139 | ||
| 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 | ||
| BT-12 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 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 | ||
| NB1643 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for NB1643 cells | 29435139 | ||
| A673 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for A673 cells) | 29435139 | ||
| SK-N-MC | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for SK-N-MC cells | 29435139 | ||
| BT-12 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for BT-12 cells | 29435139 | ||
| SJ-GBM2 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for SJ-GBM2 cells | 29435139 | ||
| U-2 OS | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for U-2 OS cells | 29435139 | ||
| Rh41 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Rh41 cells | 29435139 | ||
| RD | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for RD cells | 29435139 | ||
| Rh18 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Rh18 cells | 29435139 | ||
| Rh30 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Rh30 cells | 29435139 | ||
| SK-N-SH | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for SK-N-SH cells | 29435139 | ||
| 点击查看更多细胞系数据 | |||||
生物活性
| 产品描述 | CAY10603 (BML-281)是一种强效的选择性HDAC6抑制剂，IC50为2 pM，选择性比其它HDACs高200多倍。 | ||
|---|---|---|---|
| 靶点 |
|
| 体外研究(In Vitro) | ||||
| 体外研究活性 | CAY10603，通过抑制HDAC6，对胰腺癌细胞系表现出有效的抗增殖活性，IC50 <1 μM，其可以用作新的分子探针以探索HDAC的生物学性能。[1] | |||
|---|---|---|---|---|
| 激酶实验 | HDAC 抑制试验 | |||
| 纯化的HDACs与1 mM羧基荧光素(FAM)-标记的乙酰化多肽底物和测试化合物在HDAC试验缓冲液中于25℃下培养17小时，试验缓冲液包含100 mM HEPES (pH 7.5)，25 mM KCl，0.1% BSA，和0.01% Triton X-100。加入包含0.078% SDS的缓冲液(终SDS浓度为0.05%)终止反应。底物和产物使用Caliper LabChip 3000系统电泳分离，以蓝色激光激发，绿色荧光检测(CCD2)。底物和产品峰的荧光强度使用Well Analyzer软件在Caliper系统中检测。对每个样品，反应重复进行两次。IC50值使用Microsoft Excel 中IDBS XLFit版4.2.1 插件和XLFit 4参数Logistic模型: ((A+((B_A)/1+((C/x)D))))自动计算，公式中X是化合物浓度，A和B分别为估计的最小和最大抑制百分比，C是拐点，D是S形曲线的Hill斜率。IC50的标准差使用Microsoft Excel 中IDBS XLFit版4.2.1 插件和公式xf4_FitResultStdError自动计算。 | ||||
| 细胞实验 | 细胞系 | BxPc-3，HupT3，Mia Paca-2，Panc 04.03，和 SU 86.86 细胞 | ||
| 浓度 | ~50 μM | |||
| 孵育时间 | 72小时 | |||
| 方法 | 胰腺癌细胞系BxPc-3，HupT3，Mia Paca-2，Panc 04.03，和SU 86.86在包含10%胎牛血清和左旋谷酰胺的培养基(DMEM或RPMI)中生长。胰腺癌细胞重复两份接种在96孔板的6孔中。接种4小时后，各孔用稀释剂(DMSO)或不同浓度的SAHA或指示的1 nM到50 mM浓度的HDACIs进行处理。细胞毒性在处理后 “0”，和 72 小时使用比色MTT法根据制造商的建议进行测量。IC50值使用XLfit计算。 | |||
化学信息&溶解度
| 分子量 | 446.5 | 分子式 | C22H30N4O6 |
| CAS号 | 1045792-66-2 | SDF | Download CAY10603 SDF |
| Smiles | CC(C)(C)OC(=O)NC1=CC=C(C=C1)C2=CC(=NO2)C(=O)NCCCCCCC(=O)NO | ||
| 储存条件(自收到货起) | |||
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体外溶解度 |
DMSO : 89 mg/mL ( (199.32 mM) ；DMSO吸湿会降低化合物溶解度，请使用新开封DMSO) Ethanol : 5 mg/mL (11.19 mM) Water : 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。
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常见问题及建议解决方法
问题 1:
I want to use CAY10603 and Tubastatin A via IP for mice. What can serve as the working solution instead of DMSO?
回答：
S7596 CAY10603 can be dissolved in 5% DMSO+50% PEG 300+ddH2O at 9mg/ml as a clear solution. The dissolving protocol is the same as S8049.
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