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A-1155463 | A-1155463 : BH3 mimetic inhibitor of BCL2L1
RATINGS:
Cellular Use: (3 reviews)

In Model Organisms: (3 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
  • Ki:<0.01 nM
  • EC50:8 nm
50-500 nM

Selectivity

In Vitro Selectivity Assessment

Potency: Ki - BCL2: 80 nM, BCLW: 19 nM, MCL1: >440 nM

Potency Assay Off-Target:
TR-FRET assays

Potency
Cellular
In Vitro

BCL2L1

Mode of Action: BH3 mimetic

Structure-Activity-Relationship data available? No

In Vivo Validations

Mouse
Dose: 5 mg/kg
Route of delivery: Intraperitoneal
Organ of interest (O): Platelets, tumor xenografts
Target engagement assay: In mice treated with A1155463, platelet counts declined within 6 hours of dosing and rebounded by 72 hours. In mice with H146 tumor xenografts, A1155463 inhibited tumor growth.

Reference: --

Negative Control Compounds

A-1107969
Notes: A-1107969 >100- fold less potent in binding and cellular assays (BCL2L1: IC50 = 270 nM (TR-FRET))

Orthogonal Probes def

DT-2216
WEHI-539

Chemical Information

Molecular Formula C35H32FN5O4S2
SMILEs CN(C)CC#Cc1ccc(OCCCc2sc(N3CCc4cccc(C(=O)Nc5nc6ccccc6s5)c4C3)nc2C(=O)O)c(F)c1
InChI InChI=1S/C35H32FN5O4S2/c1-40(2)17-6-8-22-14-15-28(26(36)20-22)45-19-7-13-30-31(33(43)44)38-35(47-30)41-18-16-23-9-5-10-24(25(23)21-41)32(42)39-34-37-27-11-3-4-12-29(27)46-34/h3-5,9-12,14-15,20H,7,13,16-19,21H2,1-2H3,(H,43,44)(H,37,39,42)
Molecular weight 669.19 Da
AlogP 6.329800000000007
HBond acceptors 9
HBond donors 2
Atoms 79

Vendors

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Expert Reviews

by SERP
(on 25 Apr 2017)
Cellular Use Rating
In Model Organisms
(The reviewer did not leave any public comments)
by SERP
(on 19 May 2017)
Cellular Use Rating
In Model Organisms
This is a very promising probe.
by SERP
(on 12 Jun 2017)
Cellular Use Rating
In Model Organisms
This probe is a selective picomolar inhibitor of BCL-XL. I recommend to use this probe to interrogate BCL-XL target in cells. It should be used in combination with ABT-199 (a selective inhibitor of...
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