MFH290
Product Specifications
CAS Number
2088715-91-5
Target
Others|||CDK
Related Pathways
Others|||Cell Cycle/Checkpoint
Bioactivity
MFH290 is a novel cysteine (Cys) -directed covalent inhibitor of CDK12/13. MFH290 forms a covalent bond with Cys-1039 of CDK12, exhibits excellent kinome selectivity, inhibits the phosphorylation of serine-2 in the C-terminal domain (CTD) of RNA-polymerase II (Pol II), and reduces the expression of key DNA damage repair genes. Importantly, these effects were demonstrated to be CDK12-dependent as mutation of Cys-1039 rendered the kinase refractory to MFH290 and restored Pol II CTD phosphorylation and DNA damage repair gene expression. Consistent with its effect on DNA damage repair gene expression, MFH290 augments the antiproliferative effect of the PARP inhibitor olaparib.
Smiles
C(=O)(N1C[C@H](NC=2SC(SCC=3OC(C(C)(C)C)=CN3)=CN2)CCC1)C4=CC=C(NC(C=C)=O)C=C4
Molecular Formula
C26H31N5O3S2
Molecular Weight
525.69
Shipping Conditions
Cool pack
Storage Temperature
-20°C
Available Sizes
Curated Selection
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