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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
      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
      dCDK9-202
      1-7a-B1

      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

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

      Expert Reviews

      by SERP
      (on 13 Mar 2021)
      Cellular Use Rating
      (The reviewer did not leave any public 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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