IC50: 2.7 nM (SRPK1), 81 nM (SRPK2), 0.6 nM (SRPK3); EC50 in HEK293T cells: 98 nM (SRPK1), 40 nM (SRPK3)[1].
MSC-1186 is a highly selective pan-SRPK inhibitor. MSC-1186 has activity for SRPK1, SRPK2 and SRPK3 with IC50 values of 2.7 nM, 81 nM and 0.6 nM, respectively. MSC-1186 can be used for the research of cancer[1].
MSC-1186 对 HEK293T 细胞中的 SRPK1 和 SRPK3 具有活性，EC50 值分别为 98 nM 和 40 nM[1]。
MSC-1186 对 SRPK1、SRPK2 和 SRPK3 具有活性，IC50 值分别为 2.7 nM、81 nM 和 0.6 nM[1]。
MSC-1186 具有出色的全激酶组选择性[1]。
当与 CDC2 样激酶 (CLK) 抑制剂联合使用时，MSC-1186 显示出 SR 蛋白磷酸化的累加衰减[1]。
[1]. Martin SchrÖder, et al. MSC-1186, a Highly Selective Pan-SRPK Inhibitor Based on an Exceptionally Decorated Benzimidazole-Pyrimidine Core. J Med Chem. 2022 Dec 14.