Col003 是一种选择性和有效的 HSP47 抑制剂,可竞争性结合 HSP47 上的胶原蛋白结合位点,IC50为1.8 μM。它通过破坏胶原蛋白三螺旋的稳定性来抑制胶原蛋白的分泌,可用于肺纤维化的相关研究。
产品描述
Col003 is a selective and potent inhibitor of Hsp47 and competitively binds to the collagen-binding site on Hsp47 (IC50: 1.8 μM). It can be used for the investigation of fibrosis.
体外活性
A molecule AK778 and its cleavage product Col003 competitively inhibited the interaction and caused the inhibition of collagen secretion by destabilizing the collagen triple helix.?Structural information obtained with NMR analysis revealed that Col003 competitively binds to the collagen-binding site on Hsp47.?Col003 has an inhibitory effect on the interaction of Hsp47 with collagen in Hsp47 KO ?/? MEFs.?Col003 (0.01-100 μM) exhibits dose-dependent effects on the interactions of Hsp47 with collagen (IC50: 1.8 μM for Hsp47).?Col003 (100 μM;?20-60 mins) has an inhibitory effect on collagen secretion and accumulation.?It inhibits collagen secretion by wild-type MEFs and the secretion is not abolished completely.?Col003 (100 μM) degrades α,α′-dipyridyl collagen secretion completely by incubation with trypsin at a high temperature (50 °C for 15 min), but is resistant to trypsin digestion at 37 °C.
Cas No.
328565-16-8
分子式
C14H11NO4
分子量
257.24
储存和溶解度
DMSO:25 mg/mL (97.19 mM),Need ultrasonic
Powder: -20°C for 3 years
In solvent: -80°C for 2 years