- Guide to PHARMACOLOGY
Synonyms: AC1NRD9P | SU-9516
Compound class: Synthetic organic
Comment: SU9516 is a potent inhibitor of several cyclin-dependent kinases (CDKs) with reported selectivity for CDK2 . Later analysis of SU9516's selectivity profile indicates a similar level of potency as an inhibitor of CDK5/p25 compared to CDK2 . Inhibition of CDK5 was confirmed in a cellular assay measuring dephosphorylation of pFAK(S732). SU9516 also arrests cells at the G2/M phase in cells lacking CDK2, in which case it must be causing the cell cycle arrest via inhibition of CDK1 .
Ligand Activity Visualisation Charts
These are box plot that provide a unique visualisation, summarising all the activity data for a ligand taken from ChEMBL and GtoPdb across multiple targets and species. Click on a plot to see the median, interquartile range, low and high data points. A value of zero indicates that no data are available. A separate chart is created for each target, and where possible the algorithm tries to merge ChEMBL and GtoPdb targets by matching them on name and UniProt accession, for each available species. However, please note that inconsistency in naming of targets may lead to data for the same target being reported across multiple charts.✖
1. Anastassiadis T, Deacon SW, Devarajan K, Ma H, Peterson JR. (2011)
Comprehensive assay of kinase catalytic activity reveals features of kinase inhibitor selectivity.
Nat Biotechnol, 29 (11): 1039-45. [PMID:22037377]
2. Gao Y, Davies SP, Augustin M, Woodward A, Patel UA, Kovelman R, Harvey KJ. (2013)
A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery.
Biochem J, 451 (2): 313-28. [PMID:23398362]
3. Jorda R, Hendrychová D, Voller J, Řezníčková E, Gucký T, Kryštof V. (2018)
How Selective Are Pharmacological Inhibitors of Cell-Cycle-Regulating Cyclin-Dependent Kinases?.
J Med Chem, 61 (20): 9105-9120. [PMID:30234987]
4. Lane ME, Yu B, Rice A, Lipson KE, Liang C, Sun L, Tang C, McMahon G, Pestell RG, Wadler S. (2001)
A novel cdk2-selective inhibitor, SU9516, induces apoptosis in colon carcinoma cells.
Cancer Res, 61 (16): 6170-7. [PMID:11507069]