Chemical Probes logo
TH257 | TH257 : Allosteric inhibitor of LIMK1 and LIMK2
RATINGS:
Cellular Use: (3 reviews)

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

Probe Summary

Targets Biochemical/Biophysical Potency Cellular Potency
LIMK1
  • IC50:84 nM
  • IC50:250 nM
  • IC50:257 nM
LIMK2
  • IC50:39 nM
  • IC50:150 nM
up to 1 uM

Selectivity

In Vitro Selectivity Assessment
Potency Assay Off-Target:
TH257 is exquisitely selective and no significant activity against the wider kinome has been observe ...

Potency
Cellular
In Vitro

LIMK1

Mode of Action: Allosteric, Type III

Structure-Activity-Relationship data available? Yes

DOI Reference: 10.1021/acs.jmedchem.2c01106

LIMK2

Mode of Action: Allosteric,Type III

Structure-Activity-Relationship data available? Yes

DOI Reference: 10.1021/acs.jmedchem.2c01106

Negative Control Compounds

CANSAR3579025
Notes: TH-263 NanoBRET LIMK1 IC50>25,000 LIMK2 IC50>25,000

Chemical Information

Molecular Formula C24H26N2O3S
SMILEs CCCCN(Cc1ccccc1)C(=O)c1ccc(S(=O)(=O)Nc2ccccc2)cc1
InChI InChI=1S/C24H26N2O3S/c1-2-3-18-26(19-20-10-6-4-7-11-20)24(27)21-14-16-23(17-15-21)30(28,29)25-22-12-8-5-9-13-22/h4-17,25H,2-3,18-19H2,1H3
Molecular weight 422.17 Da
AlogP 0.0
HBond acceptors 5
HBond donors 1
Atoms 56

Vendors

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

Expert Reviews

by SERP
(on 25 May 2017 )
Cellular Use Rating
( The reviewer did not leave any comments )
by SERP
(on 2 Jun 2017 )
Cellular Use Rating
Selective allosteric molecule for use in cells to probe the effects of LIMK inhibition.
by SERP
(on 20 Jun 2017 )
Cellular Use Rating
Potent and selective chemical probe for LIMK1/2 kinases. TH-257 appears to bear a minor chemical modification from a previously disclosed 40 nM allosteric inhibitor (butyl replacement for a methyl group)....
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