FMF-04-159-2
Chemical Name: N-[1-[[3-[[(2E)-4-(Dimethylamino)-1-oxo-2-buten-1-yl]amino]phenyl]sulfonyl]-4-piperidinyl]-4-[(2,4,6- trichlorobenzoyl)amino]-1H-pyrazole-3-carboxamide
Purity: ≥98%
Biological Activity
FMF-04-159-2 is a potent inhibitor of CDK14 and CDK16 (IC50 = 40 nM for CDK14 in cellular BRET assay; IC50 values are 88 and 10 nM for CDK14 and CDK16 in kinase activity inhibition assay, respectively). Inhibits other TAIRE kinase family members at 1 μM (CDK17 and CDK18). Also binds CDK2 (IC50 = 256 nM). Displays covalent binding of CDK14, with binding sustained after washout. Causes cell cycle arrest at G2/M in cancer cell lines.Reversible control FMF-04-159-R (Cat. No. 7159) also available.
Technical Data
The technical data provided above is for guidance only.
For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Additional Information
Background References
-
Discovery of covalent CDK14 inhibitors with pan-TAIRE family specificity.
Ferguson et al.
Cell Chem.Biol., 2019;26:804 -
Synthesis and structure activity relationships of a series of 4-amino-1H-pyrazoles as covalent inhibitors of CDK14
Ferguson et al.
Bioorg.Med.Chem.Letts., 2019;29:1985
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