TK22

Chemical Structure : TK22

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货号: PC-27520Not For Human Use, Lab Use Only.

规格	价格	库存	数量
50 mg		Get quote
100 mg		Get quote
250 mg		Get quote

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生物&药学活性

TK22 is a small molecule that selectively erases Endothelial-to-mesenchymal transition (EndMT)-competent endothelial state and reverses experimental pulmonary hypertension, inhibits interphase cell-cycle kinases CDK2/3/4/6 node as well as a pro-mesenchymal node of AMPK-related kinases (NUAK1 and SIK1/2/3) together with PDGFRβ and MLK3.
TK22 is developed by structure-based design as an ATP-competitive CDK5 inhibitor with IC50 of 181 nM (CDK5/p35 complex), docking into the CDK5/p25 ATP-binding pocket.
TK22 reversed TGF-β1-induced EndMT across morphological, proteomic, and functional readouts, normalizing α-SMA, SM22, and Calponin, restoring angiogenic tube formation, abolishing acquired smooth-muscle-like contractility, and returning TGF-β1-driven hyperproliferation to baseline without suppressing normal endothelial growth, in primary murine lung endothelial cells.
TK22 selectively eliminated the EndMT-competent and metabolic-stress subpopulations while leaving the remaining endothelial landscape intact.
TK22 normalized right ventricular systolic pressure, Fulton index, and cardiac function in Su5416/hypoxia rat PH model.

物理化学性质&存储条件

分子量	307.40
分子式	C18H21N5
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	N-phenyl-7-(piperidin-4-ylmethyl)-7H-pyrrolo[2,3-d]pyrimidin-2-amine

参考文献

1. Rafikov R, et al. Res Sq [Preprint]. 2026 Jul 23:rs.3.rs-9306408.

TK22

生物&药学活性

物理化学性质&存储条件

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TK22

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