Chemical Probes logo
OTS964 | OTS964 : Inhibitor of CDK11A
RATINGS:
Cellular Use: (2 reviews)

In Model Organisms: (0 reviews)
Probe Summary
Selectivity
Potency
In Vivo
Control Compounds
Chemical Information
References
Vendors
Download

Probe Summary

Targets Biochemical/Biophysical Potency Cellular Potency
CDK11A
  • IC50:10 nM
  • IC50:102 nM
  • IC50:30-100 nM
  • IC50:9.1 nM
Inhibitor
At the highest concentration of 1 uM, keep in mind some inhibition (in vitro kinase data) might be possible of TOPK (IC50 = 353 nM), TYK2 (IC50 = 207 nM), PRK1 (IC50 = 508 nM) and CDK9 (IC50 = 538 nM), whereas 200 nM should be sufficient to very strongly inhibit CDK11A biochemically, and significantly influence cell-based activity, whereas this is relatively unlikely for other kinases.
up to 1 uM

Selectivity

In Vitro Selectivity Assessment
Potency Assay Off-Target:
OTS964 was profiled at 1 µM concentration in a panel of 412 human kinases (Eurofins) showing only 11 ...

Potency
Cellular
In Vitro

CDK11A

Mode of Action: Inhibitor

Structure-Activity-Relationship data available? Yes

DOI Reference: 10.1038/s41586-022-05204-z

Chemical Information

Molecular Formula C22H22N2O2S
SMILEs CC(CN(C)C)c1ccc(-c2c(O)ccc3[nH]c(=O)c4sccc4c23)cc1
InChI InChI=1S/C22H22N2O2S/c1-13(12-24(2)3)14-4-6-15(7-5-14)19-18(25)9-8-17-20(19)16-10-11-27-21(16)22(26)23-17/h4-11,13,25H,12H2,1-3H3,(H,23,26)
Molecular weight 378.14 Da
AlogP 4.7805000000000035
HBond acceptors 4
HBond donors 2
Atoms 49

References

Publications

Cross References

Vendors

Note: This is not an exhaustive list and does not indicate endorsement by the portal.

Expert Reviews

by SERP
(on 8 Nov 2022 )
Cellular Use Rating
OTS964 was originally reported as a PBK/TOPK inhibitor. Some references still refer to it in this context ([1] Yang Y et al. PBK/TOPK inhibitor OTS964 resistance is mediated by ABCB1-dependent transport...
by SERP+
(on 23 May 2024 )
Cellular Use Rating
Based on the data found in the literature we can state that this compound can be a suitable selective inhibitor for CDK11. In vivo and cytotoxicity experiments are recommended to validate this probe. Other...

Change of use

Originally considered a TOPK inhibitor, OTS964 is a selective CDK11 inhibitor as shown in a recent publication, where the compound has been assessed in a broad Kinase panel.

(last updated: 21 Sept 2022)

Note: The Chemical Probes Portal only endorses compounds as chemical probes for use as specific and selective modulators of the proposed target if they receive three or more (3-4) stars. Read more about our evaluation criteria