YK-2-69 | DYRK2 inhibitor | Probechem Biochemicals

Chemical Structure : YK-2-69

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YK-2-69 (DYRK2 inhibitor YK-2-69)

货号: PC-38751Not For Human Use, Lab Use Only.

YK-2-69 is a potent, hilghly selective inhibitor of dual-specificity tyrosine phosphorylation-regulated kinase 2 (DYRK2) with IC50 value of 9 nM, shows weak inhibition against DYRK1B (IC50=542 nM) and no activity against DYRK1A/3/4 (IC50>1,000 nM).

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生物&药学活性

YK-2-69 is a potent, hilghly selective inhibitor of dual-specificity tyrosine phosphorylation-regulated kinase 2 (DYRK2) with IC50 value of 9 nM, shows weak inhibition against DYRK1B (IC50=542 nM) and no activity against DYRK1A/3/4 (IC50>1,000 nM).
YK-2-69 specifically interacts with Lys-231 and Lys-234 of DYRK2.
YK-2-69 remarkably reduces PCa burden in vitro and in vivo.
YK-2-69 exhibits more potent anti-PCa efficacy than the first-line drug enzalutamide in vivo.
YK-2-69 displays favorable safety properties with a maximal tolerable dose of more than 10,000 mg/kg and pharmacokinetic profiles with 56% bioavailability.

物理化学性质&存储条件

分子量	506.604
分子式	C25H27FN8OS
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	(6-((4-(2-(dimethylamino)benzo[d]thiazol-6-yl)-5-fluoropyrimidin-2-yl)amino)pyridin-3-yl)(4-ethylpiperazin-1-yl)methanone

参考文献

1. Yuan K, et al. Nat Commun. 2022 May 25;13(1):2903.

YK-2-69 (DYRK2 inhibitor YK-2-69)

生物&药学活性

物理化学性质&存储条件

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YK-2-69 (DYRK2 inhibitor YK-2-69)

生物&药学活性

物理化学性质&存储条件

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