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Description: TH257 (TH-257; TH 257) is a novel and selective allosteric inhibitor of LIM kinases-LIMK1 and LIMK2 with important biological activity. It inhibits LIMK1 and LIMK2 with IC50 values of 84 nM and 39 nM, respectively, and it can be used as a chemical probe for LIMK1 and LIMK2. TH-257 is an allosteric inhibitor targeting a binding pocket induced by an αC and DFG-out conformation. TH257 is exquisitely selective and no significant activity against the wider kinome has been observed in the KINOMEscan assay at 1 μM.
References: Manetti F. Recent advances in the rational design and development of LIM kinase inhibitors are not enough to enter clinical trials. Eur J Med Chem. 2018 Jul 15;155:445-458.
Formula: C24H26N2O3SExact Mass: 422.1664Molecular Weight: 422.543
CAS#: 2244678-29-1
Synonym: TH257; TH-257; TH 257;
Chemical Name: N-Butyl-4-[(phenylamino)sulfonyl]-N-(phenylmethyl)benzamide
SMILES Code: O=C(N(CCCC)CC1=CC=CC=C1)C2=CC=C(S(=O)(NC3=CC=CC=C3)=O)C=C2
Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
This equation is commonly abbreviated as: C1V1 = C2V2
Purity ≥98%
COA
MSDS