Bioactivity | 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]. | |||||||||
Target | IC50: 2.7 nM (SRPK1), 81 nM (SRPK2), 0.6 nM (SRPK3); EC50 in HEK293T cells: 98 nM (SRPK1), 40 nM (SRPK3). | |||||||||
Invitro | 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]。 | |||||||||
Name | MSC-1186 | |||||||||
CAS | 2871698-23-4 | |||||||||
Formula | C19H17ClFN7O2S | |||||||||
Molar Mass | 461.90 | |||||||||
Appearance | Solid | |||||||||
Transport | Room temperature in continental US; may vary elsewhere. | |||||||||
Storage |
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Reference | [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. |