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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
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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

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Expert Reviews

by SERP
(on 25 May 2017)
Cellular Use Rating
(The reviewer did not leave any public 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