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JWZ-5-13 | JWZ-5-13 : Degrader (PROTAC) of CDK7
RATINGS:
Cellular Use: (2 reviews)

In Model Organisms: (2 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
CDK7
  • IC50:20.1 nM
  • Dmax:~100%
  • IC50:160 nM
Degrader (PROTAC)
100 nM, up to 5 uM

Selectivity

In Vitro Selectivity Assessment
Potency Assay Off-Target:
At concentrations ranging from 0.1 to 0.5 μM, 17 barely affected the protein levels of other CDK fam ...
In Cell Selectivity Assessment
Potency Assay Off-Target:
Proteome-wide analysis on OVCAR3 cells 6 h after 0.1 μM compound 17 treatment was performed: out of ...

Potency
Cellular
In Vitro

CDK7

Mode of Action: Degrader (PROTAC)

Structure-Activity-Relationship data available? Yes

DOI Reference: 10.1016/j.ejmech.2024.116613

In Vivo Validations

Mouse
Dose: 3 mg/Kg
Route of delivery: Intravenous
Plasma half life: 3.76 h
Systemic clearance: 8.3 mL/min/Kg
Cmax: 17.1 mM
Tmax: 0.083 h
Area Under the Curve:: 6.12 h*mM
Volume of Distribution at Steady-State: 0.345 L/Kg

DOI Reference: 10.1016/j.ejmech.2024.116613

Dose: 10 mg/Kg
Route of delivery: Intraperitoneal
Plasma half life: 2.82 h
Systemic clearance: 8.7 mL/min/Kg
Cmax: 3.39 mM
Tmax: 1.0 h
Area Under the Curve:: 19.4 h*mM

DOI Reference: 10.1016/j.ejmech.2024.116613

Negative Control Compounds

canSAR7437534
Notes: 17-Neg displayed similar in vitro CDK7 inhibition (21.1 nM) to 17. As expected, 17-Neg fails to reduce the level of CDK7 protein in Jurkat cells.

Orthogonal Probes def

THZ1

Chemical Information

Molecular Formula C54H66N10O6S
SMILEs Cc1ncsc1-c1ccc([C@H](C)NC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)CCCC#Cc2ccc(C(=O)Nc3n[nH]c4c3CN(C(=O)N[C@H](CN(C)C)c3ccccc3)C4(C)C)cc2)C(C)(C)C)cc1
InChI InChI=1S/C54H66N10O6S/c1-33(36-24-26-38(27-25-36)45-34(2)55-32-71-45)56-50(68)43-28-40(65)29-63(43)51(69)47(53(3,4)5)58-44(66)19-15-10-12-16-35-20-22-39(23-21-35)49(67)59-48-41-30-64(54(6,7)46(41)60-61-48)52(70)57-42(31-62(8)9)37-17-13-11-14-18-37/h11,13-14,17-18,20-27,32-33,40,42-43,47,65H,10,15,19,28-31H2,1-9H3,(H,56,68)(H,57,70)(H,58,66)(H2,59,60,61,67)/t33-,40+,42+,43-,47+/m0/s1
Molecular weight 982.49 Da
AlogP 7.049020000000007
HBond acceptors 16
HBond donors 6
Atoms 137

References

Publications

Cross References

Expert Reviews

by SERP
(on 20 Aug 2024 )
Cellular Use Rating
In Model Organisms
JWZ-5-13 is a highly selective and potent PROTAC degrader that fulfils probe criteria, offering a robust strategy for CDK7 targeting with significant potential in cancer treatment. The PROTAC degrader...
by SERP+
(on 6 Feb 2026 )
Cellular Use Rating
In Model Organisms
Selective and well validated chemical probe.
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