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首页-小分子抑制剂&激动剂-Cell Cycle/DNA Damage-Cyclin-dependent Kinase (CDK)-KY-273
KY-273

Chemical Structure : KY-273

CAS No.: 1670224-61-9

KY-273 (KY273)

货号: PC-22032Not For Human Use, Lab Use Only.

KY-273 (KY273) is a potent, specific CDK8/19 inhibitor with IC50 of 29.1 and 44.7  nM respectively, promotes osteoblast differentiation and has cortical-bone-selective osteogenic effects.

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纯度 & COA & 质检文件 纯度: >98% (HPLC)

生物&药学活性

KY-273 (KY273) is a potent, specific CDK8/19 inhibitor with IC50 of 29.1 and 44.7  nM respectively, promotes osteoblast differentiation and has cortical-bone-selective osteogenic effects.
KY-273 displays little effect on CDK2, CDK3, CDK4, CDK5 and CDK6 even at 1000 nM, also has no effect on CDK7 and CDK9 activities.
KY-273 promotes osteoblast differentiation with an increase in alkaline phosphatase (ALP) activity.
KY-273 (0.1-10 uM) concentration- and time-dependently increased ALP activities in ST2 Cells, enhances mRNA expression of Type I collagen.
KY-273 (10 mg/kg/d, p.o. 6 Weeks) increases metaphyseal and diaphyseal Ct.BV, Ct.BMC, and BSPs without affecting medullary volume (Med.V), but doesnot affect Tb.BV and Tb.BMC, in ovaries-intact and ovariectomized rats.
KY-273 increases bone formation rate/bone surface at the periosteal but not the endocortical side, in ovaries-intact and ovariectomized rats.

物理化学性质&存储条件

分子量 401.46
分子式 C22H27NO6
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

(R)-4-(1-hydroxyethyl)-3-(4-(2-((tetrahydro-2H-pyran-4-yl)oxy)ethoxy)phenoxy)benzamide

参考文献

1. Megumi Yamamoto, et al. Biol Pharm Bull. 2024;47(3):669-679.

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