1,4-DPCA

• GMP format available

1,4-DPCA is a potent inhibitor of prolyl 4-hydroxylase (P4H), with IC50 values of 3.6 µM in embryonic chick tendon cells and 2.4 µM in human foreskin fibroblasts. It also inhibits the factor inhibiting hypoxia-inducible factor (FIH) with an IC50 of 60 µM.

Key features and applications include:

• High Selectivity: Specifically inhibits prolyl 4-hydroxylase and FIH.
• Potency: Demonstrates strong inhibitory effects with IC50 values of 2-4 µM and 60 µM for P4H and FIH, respectively.
• Stabilize HIF-1α Protein: Inhibits prolyl-4-hydroxylases α isoforms, leading to increased HIF-1α stability.
• Suppress Connective Tissue Ingrowth: Effective in models of connective tissue ingrowth and collagen deposition.

Relevant disease states include:

• Fibrosis: Reduces collagen deposition, making it useful in studying fibrotic diseases.
• Cancer: Inhibits proliferation and invasive behavior of certain cancer cell lines.
• Hypoxia-Related Conditions: Stabilizes HIF-1α, which is relevant in conditions involving hypoxia.