Col003

Col003 is an inhibitor of the protein-protein interaction between collagen and heat shock protein 47 (Hsp47; IC₅₀ = 1.8 µM).¹ It decreases procollagen secretion from, and reduces the collagen levels in the extracellular matrix (ECM) of, primary mouse embryonic fibroblasts (MEFs) when used at a concentration of 100 µM. Col003 is also an inhibitor of penicillin-binding protein 2 (PBP2; IC₅₀ = 128 µM) and decreases the growth of wild-type, penicillin-resistant, and penicillin- and cephalosporin-resistant N. gonorrhea strains (MIC₅₀ = 4, 8, 16 µg/ml, respectively).² It reduces collagen-induced, but not arachidonic acid- or thrombin-induced, isolated rat platelet aggregation when used at a concentration of 50 µM.³ Col003 (50 µM) increases the time to occlusion induced by ferric chloride in carotid arteries in rats. In vivo, Col003 (50 µM) reduces brain infarct area and cell death, as well as improves grip strength, in a rat model of ischemia-reperfusion injury induced by middle cerebral artery occlusion (MCAO).

WARNING This product is not for human or veterinary use.

1. Ito, S., Ogawa, K., Takeuchi, K., et al. A small-molecule compound inhibits a collagen-specific molecular chaperone and could represent a potential remedy for fibrosis. The Journal of Biological Chemisty 292(49), 20076-20085 (2017).

2. Fedarovich, A., Djordjevic, K.A., Swanson, S.M., et al. High-throughput screening for novel inhibitors of Neisseria gonorrhoeae penicillin-binding protein 2. PLos One 7(9), e44918 (2012).

3. Wu, S., Liang, C., Xie, X., et al. Hsp47 inhibitor Col003 attenuates collagen-induced platelet activation and cerebral ischemic-reperfusion injury in rats. Front. Pharmacol. 12:792263, (2022).