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WEHI-539 | WEHI-539 : BH3 mimetic inhibitor of BCL2L1
RATINGS:
Cellular Use: (1 reviews)

In Model Organisms: (1 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
BCL2L1
  • Kd:1.4 nM
BH3 mimetic
100 nM - 1 uM

Selectivity

In Vitro Selectivity Assessment

Potency: KD - BCL-2: >750 nM, BCL-W: >550 nM, MCL-1: >550 nM, A1: >550 nM

Potency Assay Off-Target:
Direct binding assay by SPR.
In Cell Selectivity Assessment
Potency Assay Off-Target:
As noted above, deletion of BCL2 protein family members other than MCL1 does not render MEFs sensiti ...

Potency
Cellular
In Vitro

BCL2L1

Mode of Action: BH3 mimetic

Structure-Activity-Relationship data available? Yes

DOI Reference: 10.1038/nchembio.1246

Orthogonal Probes def

DT-2216
A-1155463
A-1331852

Chemical Information

Molecular Formula C31H29N5O3S2
SMILEs NCc1ccc(OCCCc2sc(-c3ccc4c(c3)/C(=N/Nc3nc5ccccc5s3)CCC4)nc2C(=O)O)cc1
InChI InChI=1S/C31H29N5O3S2/c32-18-19-10-14-22(15-11-19)39-16-4-9-27-28(30(37)38)34-29(40-27)21-13-12-20-5-3-7-24(23(20)17-21)35-36-31-33-25-6-1-2-8-26(25)41-31/h1-2,6,8,10-15,17H,3-5,7,9,16,18,32H2,(H,33,36)(H,37,38)/b35-24+
Molecular weight 583.17 Da
AlogP 6.7408
HBond acceptors 8
HBond donors 4
Atoms 70

Vendors

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Expert Reviews

by SERP
(on 3 Aug 2017 )
Cellular Use Rating
In Model Organisms
WEHI-539 is an inhibitor of BCL-2 family proteins, binding potently and selectively to BCL-XL with an IC50 of ~1.1 nM. It was the first small molecule that selectively antagonizes the prosurvival activity...
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