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TH-257

  Cat. No.:  DC12564   Featured
Chemical Structure
2244678-29-1
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Field of application
TH-257 (TH257) is a potent, selective, allosteric inhibitor of LIMK1 and LIMK2 with IC50 of 84 nM for LIMK1 and 39 nM for LIMK2 in a RapidFire MS assay.
Chemicals PropertiesBiological activity COA & MSDSRelated productsDatasheet
Cas No.: 2244678-29-1
Chemical Name: N-benzyl-N-butyl-4-(N-phenylsulfamoyl)benzamide
Synonyms: TH-257;TH 257;TH257
SMILES: C(N(CC1=CC=CC=C1)CCCC)(=O)C1=CC=C(S(NC2=CC=CC=C2)(=O)=O)C=C1
Formula: C24H26N2O3S
M.Wt: 422.543
Purity: >98%
Sotrage: 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
Publication: [1]. 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.
Description: TH-257 is a potent inhibitor of LIMK1 and LIMK2 with IC50 values of 84 nM and 39 nM for LIMK1 and LIMK2, 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[1].
Target: LIMK1:84 nM (IC50) LIMK2:39 nM (IC50)
References: [1]. 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.
MSDS
COA
LOT NO. DOWNLOAD
2018-0101
2018-0101
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