DC70622 |
MSC 2711186
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MSC2711186 is a potent, selective, cell active pan-SRPK with IC50 of 2.7/8.1/0.59 nM for SRPK1/2/3, repectively.MSC2711186 does not show any activity towards the CLKs, and is selective in an in vitro kinase panel from Reaction Biology at 1 µM against 395 Kinases.MSC2711186 displayed an IC50 of 98 nM on SRPK1 and 40 nM on SRPK3 in intact cells and 44 nM on SRPK1, 149 nM on SRPK2 and 40nM on SRPK3 in lysed cells in NanoBRETTM assay.Serine-arginine protein kinases (SPRKs) are a subfamily of serine-threonine kinases, regulating pre-mRNA splicing in response to extracellular stimuli by phosphorylating serine/arginine (SR)-rich splicing factors. The human genome encodes three SRPK genes, SRPK1, SRPK2 and SRPK3. While SRPK1 has been detected in many human tissues at varying expression levels, SRPK2 and SRPK3 exhibit a more tissue-specific expression. |