1622059-04-4
Chemical Structure
TH251
- CAS No.: 1622059-04-4
- Formula:C22H22N2O3S
- Molecular Weight:394.49
IUPAC Name: N-benzyl-N-ethyl-4-(N-phenylsulfamoyl)benzamide
InChIKey: HSFGCMJKYHQRQQ-UHFFFAOYSA-N
SMILES: O=C(C1=CC=C(C=C1)S(=O)(=O)NC=2C=CC=CC2)N(CC=3C=CC=CC3)CC
Biological Activity: TH251 is a LIMK1 and LIMK2 inhibitor with IC50s of 52 nM and 47 nM against LIMK1 and LIMK2, respectively. TH251 binds to inactive αC-out and DFG-out LIMK1 conformations, inhibits unphosphorylated LIMK1 and LIMK2 enzymatic activity, and exhibits unchanged potency despite PAK-mediated phosphorylation of either kinase. TH251 can be used for the research of cancers, glaucoma, and CNS diseases[1][2].
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TH251 | TH251 is a LIMK1 and LIMK2 inhibitor with IC50s of 52 nM and 47 nM against LIMK1 and LIMK2, respectively. TH251 binds to inactive αC-out and DFG-out LIMK1 conformations, inhibits unphosphorylated LIMK1 and LIMK2 enzymatic activity, and exhibits unchanged potency despite PAK-mediated phosphorylation of either kinase. TH251 can be used for the research of cancers, glaucoma, and CNS diseases. | |||||||||||||||||||||
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- [1]. Collins R, et al. Comparative Analysis of Small-Molecule LIMK1/2 Inhibitors: Chemical Synthesis, Biochemistry, and Cellular Activity. J Med Chem. 2022 Oct 27;65(20):13705-13713. [Content Brief]
- [2]. Mathea, S; et al. LIM Domain Kinase 1 (LIMK1), Human Kinase Domain; A Target Enabling Package. University of Oxford, 2017 Jun 2.
Keywords
