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JH-XI-10-02 | JH-XI-10-02 : Degrader (PROTAC) of CDK8
RATINGS:
Cellular Use: (2 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
CDK8
  • IC50:159 nM
  • Activity:1 µM
Degrader (PROTAC)
1-5 uM

Selectivity

In Vitro Selectivity Assessment
Selectivity Assessment Description:
KinomeScan binding analysis against a panel of 468 kinases at a concentration of 10 μM for parent co ...

Potency
Cellular
In Vitro

CDK8

Mode of Action: Degrader (PROTAC)

Structure-Activity-Relationship data available? Yes

DOI Reference: 10.1021/acsmedchemlett.8b00011

Orthogonal Probes def

CCT251545

Chemical Information

Molecular Formula C53H69N5O9
SMILEs CN(C(=O)CCOCCOCCOCCOCCNc1cccc2c1C(=O)N(C1CCC(=O)NC1=O)C2=O)[C@H]1CC[C@@]2(C)C(CC[C@@H]3C2CC[C@]2(C)[C@@H](c4ccc5ccncc5c4)CC[C@@H]32)C1
InChI InChI=1S/C53H69N5O9/c1-52-19-15-38(32-37(52)9-10-39-42-12-11-41(53(42,2)20-16-43(39)52)35-8-7-34-17-21-54-33-36(34)31-35)57(3)47(60)18-23-64-25-27-66-29-30-67-28-26-65-24-22-55-44-6-4-5-40-48(44)51(63)58(50(40)62)45-13-14-46(59)56-49(45)61/h4-8,17,21,31,33,37-39,41-43,45,55H,9-16,18-20,22-30,32H2,1-3H3,(H,56,59,61)/t37?,38-,39-,41+,42-,43?,45?,52-,53+/m0/s1
Molecular weight 919.51 Da
AlogP 0.0
HBond acceptors 14
HBond donors 2
Atoms 136

Vendors

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Expert Reviews

by SERP
(on 9 Mar 2022 )
Cellular Use Rating
I would not view this chemical probe as of sufficient quality to interrogate consequences of CDK8 degradation in cells. No selectivity data is available for either the kinase binding selectivity or, more...
by SERP+
(on 31 Oct 2024 )
Cellular Use Rating
Insufficient degradation data: DCmax, DC50, and degradation selectivity by proteomics are not reported.
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