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

CAY10603 Chemical Structure

CAS: 1045792-66-2

规格 价格 库存 购买数量
10mM (1mL in DMSO) RMB 1367.73 现货
5mg RMB 1181.73 现货
25mg RMB 3898.21 现货
100mg RMB 8177.36 现货
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客户使用Selleck的CAY10603发表文献21

客户使用该产品的4个实验数据

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

HDAC抑制剂选择性比较

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
HDAC6 [1]
(Cell-free assay)
2 pM
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)

体外溶解度
批次:

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

Water : Insoluble

摩尔浓度计算器

体内溶解度
批次:

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

摩尔浓度计算器

质量 浓度 体积 分子量

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

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,: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: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: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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