|(3-((6-(2-甲氧基苯基)嘧啶-4-基)氨基)苯基)甲磺酰胺|CsnPharm

CAS No.: 1073485-20-7

(3-((6-(2-Methoxyphenyl)pyrimidin-4-yl)amino)phenyl)methanesulfonamide Catalog No. CSN16940

Synonyms: LDC067

LDC000067 is a highly specific CDK9 inhibitor with IC50 of 32.7 nM for CDK9/cyclin T1.

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技术信息

生物活性

描述Cyclin-dependent kinases (CDKs) are a family of evolutionarily conserved serine/threonine kinases that form heterodimers with regulatory cyclin partner proteins. LDC000067 inhibits CDK9 in vitro with an IC₅₀ of 44 ± 10 nM. Its selectivity for CDK9 over other CDKs is in the range of 55-fold (vs. CDK2) to over 230-fold (vs. CDK6 and CDK7). It inhibits in vitro transcription in an ATP-competitive and dose-dependent manner. Transcription assays revealed a half-maximal inhibition of 4 μM for LDC000067 at 100 μM ATP. Notablely, apoptosis induction was most pronounced in cells of leukaemic origin such as THP1 (approximately 45% apoptotic cells at 10 μM LDC000067) and patient-derived blast cells (>60% at 10 μM). Furthermore, repression of mRNA synthesis was first detectable at a concentration of 1 μM, with 50 to 80% repression obtained at a concentration of 10 μM LDC000067. Half-maximal repression by LDC000067 was achieved in the range of 2 to 6 μM. Likewise, treatment with 10 μM LDC000067 caused an 80 to 90% reduction of RNA synthesis in HeLa cells. Luciferase expression decreased in a concentration-dependent manner, with half-maximal repression reached at 2 μM LDC000067^[2].
参考文献

[1] Albert TK, Rigault C, et al. Characterization of molecular and cellular functions of the cyclin-dependent kinase CDK9 using a novel specific inhibitor. Br J Pharmacol. 2014 Jan;171(1):55-68.
[2] Albert TK, Rigault C, Eickhoff J, et al. Characterization of molecular and cellular functions of the cyclin-dependent kinase CDK9 using a novel specific inhibitor. Br J Pharmacol. 2014;171(1):55-68

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
- 2.6996 mL
- 13.4980 mL
- 26.9960 mL
- 5 mM
- 0.5399 mL
- 2.6996 mL
- 5.3992 mL
- 10 mM
- 0.2700 mL
- 1.3498 mL
- 2.6996 mL

技术信息

CAS号

1073485-20-7

储存条件

粉末: Keep in dark place,Inert atmosphere,Room temperature

液体: -20°C:3-6 月 -80°C:12月

分子式

C18H18N4O3S

运输

蓝冰

分子量

370.43

别名

LDC067

溶解度

DMSO	74.0 mg/mL (199.8 mM)
Water	Insoluble
Ethanol	Insoluble

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(3-((6-(2-Methoxyphenyl)pyrimidin-4-yl)amino)phenyl)methanesulfonamide Catalog No. CSN16940

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