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BIX-01294 | Inhibitor of EHMT2
RATINGS:
Cellular Use: (3 reviews)

In Model Organisms: (2 reviews)
Probe Summary
Selectivity
Potency
In Vivo
Control Compounds
Chemical Information
References
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Probe Summary

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Targets Biochemical/Biophysical Potency Cellular Potency
EHMT2
  • IC50:1700 nM
  • IC50:2700 nM
up to 5 uM

Selectivity

In Vitro Selectivity Assessment

Potency: IC50 - EHMT1 38 uM

Potency Assay Off-Target:
MS-based histone methyltransferase assay. No activity was detected up to 45 uM BIX-01294 against PRM ...
Selectivity Assessment Description:
Not available

Potency
Cellular
In Vitro

EHMT2

Mode of Action: Inhibitor

Structure-Activity-Relationship data available? Yes

DOI Reference: 10.1016/j.molcel.2007.01.017

Orthogonal Probes def

A-366
UNC0642
MS8709

Chemical Information

Molecular Formula C28H38N6O2
SMILEs COc1cc2nc(N3CCCN(C)CC3)nc(NC3CCN(Cc4ccccc4)CC3)c2cc1OC
InChI InChI=1S/C28H38N6O2/c1-32-12-7-13-34(17-16-32)28-30-24-19-26(36-3)25(35-2)18-23(24)27(31-28)29-22-10-14-33(15-11-22)20-21-8-5-4-6-9-21/h4-6,8-9,18-19,22H,7,10-17,20H2,1-3H3,(H,29,30,31)
Molecular weight 490.31 Da
AlogP 3.865400000000003
HBond acceptors 8
HBond donors 1
Atoms 74

Expert Reviews

by SERP
(on 4 Nov 2016)
Cellular Use Rating
In Model Organisms
Whilst there are many published references using this molecule in various cell-based studies, there is limited selectivity data disclosed for it beyond the closely associated family of proteins listed...
by SERP
(on 22 Dec 2016)
Cellular Use Rating
In Model Organisms
BIX-01294 should be used with caution. I have several specific concerns about this molecule: Selectivity over GLP is reportedly ~20x and >>20x for five related family members. Subsequent reports...
by SERP
(on 23 Jan 2017)
Cellular Use Rating
Users should note selectivity experiments were performed against a limited panel of targets in the initial report. The lack of specificity data of BIX-01294 versus other targets (besides GLP, PRMT1,...
The limited selectivity assessement of BIX-0194 within the HMT family and also outside the family restricts its usefulness. The compound is not very potent in vitro (low micromolar) and...
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