SR-2890 is a highly selective, ATP-competitive inhibitor of casein kinase CK1delta and CK1epsilon, with IC50 values of 4 nM and 44 nM, respectively, and a Ki of 14 nM for CK1delta. SR-2890 exhibits antiproliferative effects. SR-2890 blocks the serine/threonine kinase activity of CK1delta and weakly inhibits a few off-target kinases such as FLT3, CDK4. SR-2890 has an oral bioavailability of 10% and a blood-brain barrier penetration rate of in vitro metabolism and favorable in vivo pharmacokinetic properties, effectively inhibiting the growth of human A375 melanoma cells. SR-2890 can be used in melanoma research and is also a useful compound for studying CK1delta/epsilon-related diseases such as Alzheimers disease[1].
Molekulargewicht:
477.92
CAS Nummer:
[1454584-91-8]
Formel:
C23H21ClFN9
Target-Kategorie:
Casein Kinase,CDK,FLT3
Anwendungsbeschreibung:
MCE Product type: Reference compound
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