CPS2 | CPS2 : Degrader (PROTAC) of CDK2
RATINGS:
Cellular Use: (3 reviews)

In Model Organisms: (0 reviews)
In Vivo
Vendors

Probe Summary

Targets Biochemical/Biophysical Potency Cellular Potency
CDK2
  • IC50:24 nM
  • Dmax:100 %
  • DC50:12-61 nM
Degrader (PROTAC)
250 nM
up to 1 uM

Selectivity

In Vitro Selectivity Assessment
Potency Assay Off-Target:
Kinome scan for 1 μM CPS2 highlighted unwanted interactions with AURKA and KDR. Cell-free binding- ...
In Cell Selectivity Assessment
Potency Assay Off-Target:
Proteomics analysis was performed in NB4 cells treated with 250-nM CPS2 for 6 h confirming CDK2 was ...
In Cell Selectivity Assessment
Potency Assay Off-Target:
Selectivity within target family: CPS2 induced only CDK2 degradation and did not directly perturb th ...
Selectivity Assessment Description:
Western blot

Potency
Cellular
In Vitro

CDK2

Mode of Action: Degrader (PROTAC)

Structure-Activity-Relationship data available? Yes

DOI Reference: 10.1038/s41589-021-00742-5

Negative Control Compounds

Neg-CPS2
Notes: Cpd 7 is the negative control and is unable to induce degradation

Chemical Information

Molecular Formula C38H42N12O10S2
SMILEs Cc1ccsc1C(=O)n1nc(Nc2ccc(S(=O)(=O)NCCOCc3cn(CCOCCOCCNc4cccc5c4C(=O)N(C4CCC(=O)NC4=O)C5=O)nn3)cc2)nc1N
InChI InChI=1S/C38H42N12O10S2/c1-23-11-20-61-32(23)36(55)50-37(39)44-38(46-50)42-24-5-7-26(8-6-24)62(56,57)41-13-16-60-22-25-21-48(47-45-25)14-17-59-19-18-58-15-12-40-28-4-2-3-27-31(28)35(54)49(34(27)53)29-9-10-30(51)43-33(29)52/h2-8,11,20-21,29,40-41H,9-10,12-19,22H2,1H3,(H,43,51,52)(H3,39,42,44,46)
Molecular weight 890.26 Da
AlogP 0.0
HBond acceptors 22
HBond donors 6
Atoms 104

References

Cross References

canSAR

Expert Reviews


(on 20 Feb 2025 )
Cellular Use Rating
Users are advised to re-assess the DC50 (both for CDK2 and for AURKA) of the compounds since the published data are conflicting. The Recommended In cell concentration should be in the range of 250 to...
(on 16 Apr 2025 )
Cellular Use Rating
CPS2 is a valuable tool compound for investigating CDK2 biology and the therapeutic potential of CDK2 degradation. At a concentration of 250 nM and following 6 hours of treatment of NB4 cells, CPS2 induces...
(on 6 Feb 2026 )
Cellular Use Rating
A concentration of 250 nM is recommended. At this concentration CPS2 is a potent degrader of Aurora A - it is worth assaying alongside AURKA inhibitors/other CDK2 inhibitors with other different profiles...
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