Col003 是 Hsp47 的选择性有效抑制剂，竞争性结合的胶原蛋白结合位点 Hsp47 (IC₅₀，1.8 μM)。Col003 抑制 Hsp47 与胶原蛋白的相互作用，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。Col003 可用于肺纤维化的相关研究。

Col003 is a selective and potent inhibitor of Hsp47 and competitively binds to the collagen binding site on Hsp47 (IC 50 =1.8 μM). Col003 discourages the interaction of Hsp47 with collagen and inhibits collagen secretion by destabilizing the collagen triple helix. Col003 can be used for the investigation of fibrosis

Solid

HSP47 1.8 μM (IC50)

Col003 (4.4-40 μM) is cleaved from Col001 (AK-778). 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. The IC50 value is 1.8 μM for Hsp47.
Col003 (100 μM; 20-60 mins) has an nhibitory effects 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 it resistant to trypsin digestion at 37 °C.
 . has not independently confirmed the accuracy of these methods. They are for reference only.

Room temperature in continental US; may vary elsewhere.

4°C, stored under nitrogen In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)

[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.

In Vitro: DMSO : 50 mg/mL (194.37 mM; Need ultrasonic)配制储备液