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CAS No.: 1045792-66-2

CAY10603 Catalog No. CSN13836

Synonyms: BML-281;HDAC 6 inhibitor;Histone Deacetylase Inhibitor VIII

CAY10603 is a selective inhibitor of HDAC6 with IC50 of 2 pM.

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400-920-2911

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靶点选择性

生物活性

实验方案

技术信息

生物活性

描述There are 18 mammalian HDACs, HDAC 1-11 and sirt 1-7. One of the member, HDAC6 can target specific substrates like HSP90 andα-tubulin which involve in protein trafficking and degradation or cell shape and migration, thus participates in the pathways relating to neurodegenerative diseases, cancer, and immunology. CAY10603 is a highly selective HDAC 6 inhibitor with IC50 value of 0.002nM, also exhibited weaker inhibitory effect on HDAC3 and HDAC 10 with IC50 values of 0.42nM and 90.7nM, respectively. CAY10603 were active against both the Mia Paca-2 and Panc04.03 cell lines at the 100 nM level, and against HupT3 at the 200-300 nM^[1]. CAY10603 led growth inhibition of A549 and HCC827 cells at concentration<10μM. CAY10603 induced apoptosis at concentration of 0.16μM and 0.32μM in A549 after 48h treatment. Inhibition of HDAC6 through CAY10603 inactivated the EGFR pathway^[2]. HDAC6 inhibition by CAY10603 prevented LPS-induced ɑ-tubulin deacetylation in the lung tissues and exhibited protective effects against LPS-induced acute lung inflammation^[3].
作用机制CAY10603 can bind directly to HDAC6 and chelate Zn²⁺ through its Zn-binding domain.^[1]^[3]
细胞研究

Cell Data

Cell Lines	Concentration	Assay Type	Time	Activity Description	Data Sources
HMEC	-	Cytotoxicity assay	72 h	Cytotoxicity against HMEC after 72 hrs by MTT assay, IC50=1 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 BxPC3 cells	-	Proliferation assay	72 h	Antiproliferative activity against human BxPC3 cells after 72 hrs by MTT assay, IC50=1 μM	18642892

更多
动物研究
剂量
Mice: 5 mg/kg^[4] (i.p.); 1 mg/kg, 10 mg/kg^[5] (s.c.)

给药途径
i.p., s.c.
参考文献

动物研究
剂量	Mice: 5 mg/kg^[4] (i.p.); 1 mg/kg, 10 mg/kg^[5] (s.c.)
给药途径	i.p., s.c.

[1] Kozikowski AP, Tapadar S, et al. Use of the nitrile oxide cycloaddition (NOC) reaction for molecular probe generation: a new class of enzyme selective histone deacetylase inhibitors (HDACIs) showing picomolar activity at HDAC6. J Med Chem. 2008 Aug 14;51(15):4370-3.
[2] Wang Z, Tang F, et al. HDAC6 promotes cell proliferation and confers resistance to gefitinib in lung adenocarcinoma. Oncol Rep. 2016 Jul;36(1):589-97.
[3] Sixto-López Y, Bello M, et al. Structural and energetic basis for the inhibitory selectivity of both catalytic domains of dimeric HDAC6. J Biomol Struct Dyn. 2018 Dec 17:1-20.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.2397 mL
- 11.1983 mL
- 22.3966 mL
- 5 mM
- 0.4479 mL
- 2.2397 mL
- 4.4793 mL
- 10 mM
- 0.2240 mL
- 1.1198 mL
- 2.2397 mL

技术信息

CAS号

1045792-66-2

储存条件

粉末: Sealed in dry,Store in freezer, under -20°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C22H30N4O6

运输

蓝冰

分子量

446.50

别名

BML-281;HDAC 6 inhibitor;Histone Deacetylase Inhibitor VIII

溶解度

DMSO	89.0 mg/mL (199.3 mM)
Water	Insoluble
Ethanol	5.0 mg/mL (11.2 mM) warming

动物实验配方

5% DMSO+50% PEG 300+water

9 mg/mL

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