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首页-小分子抑制剂&激动剂-Cell Cycle/DNA Damage-Cyclin-dependent Kinase (CDK)-LDC000067
LDC000067

Chemical Structure : LDC000067

CAS No.: 1073485-20-7

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LDC000067 (LDC-000067, LDC 000067, LDC067)

货号: PC-21088Not For Human Use, Lab Use Only.

LDC000067 (LDC067) is a highly specific inhibitor of CDK9 with IC50 of 44 nM (CDK9-Cyclin T1), highly selective over other CDKs in the range of 55-fold (CDK2) to over 230-fold (CDK6 and CDK7).

规格 价格 库存 数量
10 mg ￥880 In stock
25 mg ￥1380 In stock
50 mg ￥2180 In stock
100 mg ￥3580 In stock
250 mg Get quote
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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

LDC000067 (LDC067) is a highly specific inhibitor of CDK9 with IC50 of 44 nM (CDK9-Cyclin T1), highly selective over other CDKs in the range of 55-fold (CDK2) to over 230-fold (CDK6 and CDK7).
LDC000067 displays 55/125/210/ >227/ >227-fold selectivity for CDK9 versus CDK2/1/4/6/7, shows better selectivity profile than the known and widely used inhibitors DRB and flavopiridol.
LDC000067 inhibits P-TEFb-dependent in vitro transcription in an ATP-competitive manner, decreases phosphorylation of the Ser2 residue within the CTD of RNAPII, both in cells and nuclear extracts.
CDK9 inhibition by LDC067 increases promoter-proximal RNAPII levels.
LDC000067 attenuates atherosclerosis by inhibiting inflammation and phenotypic switching of vascular smooth muscle cells.

物理化学性质&存储条件

分子量 370.43
分子式 C18H18N4O3S
外观性状 Solid
CAS No.
储存条件
固体粉末
-20°C 12 个月; 4°C 6 个月
配置液
-80°C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO
Chemical Name/SMILES

(3-((6-(2-methoxyphenyl)pyrimidin-4-yl)amino)phenyl) methanesulfonamide

参考文献

1. Albert TK, et al. Br J Pharmacol. 2014 Jan;171(1):55-68.

2. Huang S, et al. Aging (Albany NY). 2021 Jun 8;13(11):14892-14909.

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