LDN-192960 hydrochloride 是 Haspin 和 DYRK2 的双重抑制剂,IC50 值分别为 10 nM 和 48 nM。
货号:ajcx14756
CAS:2309172-48-1
分子式:C18H22Cl2N2O2S
分子量:401.35
溶解度:DMSO: 33 mg/ml,PBS (pH 7.2): 10 mg/ml
纯度:98%
存储:Store at -20°C
库存:
现货
Background:
LDN-192960 hydrochloride is an inhibitor of Haspin and Dual-specificity Tyrosine-regulated Kinase 2 (DYRK2) with IC50s of 10 nM and 48 nM, respectively[1].
LDN-192960 hydrochloride (10 μM) is selective and inhibits ten of the other kinases by ≥90%, with only five being potently inhibited (IC50<1 μM), including CLK1 (IC50=0.21 μM), DYRK1A (IC50= 0.10 μM), DYRK2 (IC50=2 nM), DYRK3 (IC50=19 nM) and PIM1 (IC50=0.72 μM)[1].
[1]. Cuny GD, et al. Structure-activity relationship study of acridine analogs as haspin and DYRK2 kinase inhibitors. Bioorg Med Chem Lett. 2010 Jun 15;20(12):3491-4.