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BSJ-03-123 | Degrader (PROTAC) of CDK6
RATINGS:
Cellular Use: (3 reviews)

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

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Targets Biochemical/Biophysical Potency Cellular Potency
CDK6
  • IC50:8.7 nM
  • IC50:41.6 nM
200 nM, up to 1 uM

Selectivity

In Vitro Selectivity Assessment
Selectivity Assessment Description:
Highly selective in KINOMEscan @ 1uM, 4-fold selective Vs CDK4
In Cell Selectivity Assessment
Selectivity Assessment Description:
CDK6 was sole destabilized protein in proteome-wide selectivity studies, check cellular data.

Potency
Cellular
In Vitro

CDK6

Mode of Action: Degrader (PROTAC)

Structure-Activity-Relationship data available? No

DOI Reference: 10.1016/j.chembiol.2018.11.006

Negative Control Compounds

BSJ-Bump

Orthogonal Probes def

CP-10
Palbociclib
Abemaciclib

Chemical Information

Molecular Formula C47H56N10O11
SMILEs CC(=O)c1c(C)c2cnc(Nc3ccc(N4CCN(CCOCCOCCOCCNC(=O)COc5cccc6c5C(=O)N(C5CCC(=O)NC5=O)C6=O)CC4)cn3)nc2n(C2CCCC2)c1=O
InChI InChI=1S/C47H56N10O11/c1-29-34-27-50-47(53-42(34)56(31-6-3-4-7-31)45(63)40(29)30(2)58)51-37-12-10-32(26-49-37)55-17-15-54(16-18-55)19-21-66-23-25-67-24-22-65-20-14-48-39(60)28-68-36-9-5-8-33-41(36)46(64)57(44(33)62)35-11-13-38(59)52-43(35)61/h5,8-10,12,26-27,31,35H,3-4,6-7,11,13-25,28H2,1-2H3,(H,48,60)(H,52,59,61)(H,49,50,51,53)
Molecular weight 936.41 Da
AlogP 2.3244200000000035
HBond acceptors 21
HBond donors 3
Atoms 124

Vendors

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

Expert Reviews

by SERP
(on 7 Jan 2021)
Cellular Use Rating
This is a potent and selective CDK6 degrader and I recommend it as a Protac chemical probe.
by SERP
(on 7 Jan 2021)
Cellular Use Rating
BSJ-03-123 is a selective CDK6 degrader. When used in combination with the negative control compound BSJ-Bump, it can be a useful probe to examine consequences of targeted degradation of CDK6. Given...
by SERP
(on 27 Jan 2021)
Cellular Use Rating
(The reviewer did not leave any public comments)
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