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NVP-2 | NVP-2 : ATP competitive inhibitor of CDK9
RATINGS:
Cellular Use: (2 reviews)

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

Targets Biochemical/Biophysical Potency Cellular Potency
CDK9
  • IC50:0.514 nM
  • IC50:9 nM
  • IC50:92-574 nM
ATP competitive
250 to 1000 nM

Selectivity

In Vitro Selectivity Assessment
Selectivity Assessment Description:
Exhibits selectivity for CDK9 over a panel of 468 kinases, but inhibits DYRK1B (IC50 = 350 nM), d ...

Potency
Cellular
In Vitro

CDK9

Mode of Action: ATP competitive

Structure-Activity-Relationship data available? Yes

DOI Reference: 10.1038/nchembio.2538

Orthogonal Probes def

THAL-SNS-032

Chemical Information

Molecular Formula C27H37ClN6O2
SMILEs COC[C@@H](C)NC1CCC(Nc2cc(-c3cccc(NCC4(C#N)CCOCC4)n3)c(Cl)cn2)CC1
InChI InChI=1S/C27H37ClN6O2/c1-19(16-35-2)32-20-6-8-21(9-7-20)33-26-14-22(23(28)15-30-26)24-4-3-5-25(34-24)31-18-27(17-29)10-12-36-13-11-27/h3-5,14-15,19-21,32H,6-13,16,18H2,1-2H3,(H,30,33)(H,31,34)/t19-,20?,21?/m1/s1
Molecular weight 512.27 Da
AlogP 0.0
HBond acceptors 8
HBond donors 3
Atoms 73

References

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Expert Reviews

by SERP
(on 30 Jun 2021)
Cellular Use Rating
(The reviewer did not leave any public comments)
by SERP+
(on 23 Sept 2024)
Cellular Use Rating
Several CDK9 inhibitors are available and can be used with NVP-2 as orthogonal probe. For example, 2020 a highly selective CDK9-inhibitor (JHS-009; DOI: 10.1007/s10637-019-00868-3) was published which...
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