| Bioactivity | Col003 is a selective and potent inhibitor of Hsp47 and competitively binds to the collagen binding site on Hsp47 (IC50=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[1] |
| Invitro | 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[1].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[1].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[1].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[1]. . Western Blot Analysis[1] Cell Line: |
| Name | Col003 |
| CAS | 328565-16-8 |
| Formula | C14H11NO4 |
| Molar Mass | 257.24 |
| Appearance | Solid |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | 4°C, stored under nitrogen *In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen) |
| Reference | [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. |