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THAL-SNS-032 | Degrader (PROTAC) of CDK9, CDK10
RATINGS:
Cellular Use: (4 reviews)

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

Targets Biochemical/Biophysical Potency Cellular Potency
CDK9
  • EC 50:50 nM
CDK10
  • EC 50:250 nM
Degrader (PROTAC)
250 - 1000 nM

Selectivity

In Cell Selectivity Assessment
Selectivity Assessment Description:
Within Target Family: >15-fold selectivity for Cdk9 over other CDKs (EC50 values are 62, 171 and 398 ...

Potency
Cellular
In Vitro

CDK9

Mode of Action: Degrader (PROTAC)

Structure-Activity-Relationship data available? No

DOI Reference: 10.1038/nchembio.2538

CDK10

Mode of Action: Degrader (PROTAC)

Structure-Activity-Relationship data available? No

DOI Reference: 10.1038/nchembio.2538

Orthogonal Probes def

NVP-2

Chemical Information

Molecular Formula C40H52N8O10S2
SMILEs CC(C)(C)c1cnc(CSc2cnc(NC(=O)C3CCN(CC(=O)NCCOCCOCCOCCNc4cccc5c4C(=O)N(C4CCC(=O)NC4=O)C5=O)CC3)s2)o1
InChI InChI=1S/C40H52N8O10S2/c1-40(2,3)29-21-43-32(58-29)24-59-33-22-44-39(60-33)46-35(51)25-9-13-47(14-10-25)23-31(50)42-12-16-56-18-20-57-19-17-55-15-11-41-27-6-4-5-26-34(27)38(54)48(37(26)53)28-7-8-30(49)45-36(28)52/h4-6,21-22,25,28,41H,7-20,23-24H2,1-3H3,(H,42,50)(H,44,46,51)(H,45,49,52)
Molecular weight 868.32 Da
AlogP 3.0507000000000044
HBond acceptors 18
HBond donors 4
Atoms 112

Vendors

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Expert Reviews

by SERP
(on 13 Mar 2021 )
Cellular Use Rating
( The reviewer did not leave any comments )
by SERP
(on 19 Mar 2021 )
Cellular Use Rating
This probe is a degrader version of the inhibitor NVP-2. Both probes inhibit additional kinases in vitro, but the probe here selectively degrades CDK9 (and CDK10). Best use would be comparison of...
by SERP
(on 29 Mar 2021 )
Cellular Use Rating
A potential and selective PROTAC molecule to degrade cellular level of CDK9. Very fast degradation kinetics was observed. Good evidence of UPS mediated degradation using CRBN negative cell line control....
by SERP+
(on 17 Jun 2024 )
Cellular Use Rating
The PROTAC was well and intensively characterized and represents a very good chemical probe. However, a negative control compound for easy cellular experiment performance and validation would be appreciated....
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