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CAY10603

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Chemical Structure| 1045792-66-2 同义名 : BML-281;HDAC 6 inhibitor;Histone Deacetylase Inhibitor VIII
CAS号 : 1045792-66-2
货号 : A160958
分子式 : C22H30N4O6
纯度 : 98%
分子量 : 446.497
MDL号 : MFCD17010286
存储条件:

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

液体 -20°C:3-6个月-80°C:12个月

溶解度 :

DMSO: 50 mg/mL(111.98 mM),注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO

动物实验配方:

5% DMSO+50% PEG 300+water 9 mg/mL

生物活性
靶点
  • HDAC6

    HDAC6, IC50:2 pM

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
细胞系 浓度 检测类型 检测时间 活动说明 数据源
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
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.24mL

0.45mL

0.22mL

11.20mL

2.24mL

1.12mL

22.40mL

4.48mL

2.24mL

参考文献

[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.