TH-257|TH257|CAS 2244678-29-1|DC Chemicals

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.

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