Col003是一种有效的Hsp47抑制剂,竞争性地与Hsp47上的胶原结蛋白合位点结合(IC50,1.8μM),通过破坏胶原蛋白的三重螺旋结构抑制胶原蛋白的分泌。
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Col003 is a potent inhibitor of Hsp47, competitively binds to the collagen binding site on Hsp47 (IC50, 1.8 μM), and inhibits collagen secretion by destabilizing the collagen triple helix[1]. HSP47|1.8 μM (IC50)
[1]. Ito S, et al. A small-molecule compound inhibits a collagen-specific molecular chaperone and could represent a potential remedy for fibrosis. J Biol Chem. 2017 Dec 8;292(49):20076-20085.
IPI-504 (Retaspimycin hydrochloride)
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