71220  1,4-DPCA

1,4-dihydrophenonthrolin-4-one-3-Carboxylic acid (CAS 331830-20-7)



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The pro-angiogenic factor HIF-1α is targeted for destruction in non-hypoxic environments by the hydroxylation of a specific proline residue, P564, by the oxygen-sensing enzyme HIF-α prolyl hydroxylase (HIF-PH).1 Inhibitors of prolyl 4-hydroxylase are potentially useful in controlling excess collagen deposition in pathological fibrosis. 1,4-DPCA is a competitive inhibitor of prolyl 4-hydroxylase in embryonic chick tendon cells and of collagen hydroxylation in human foreskin fibroblasts with an IC50 value of 3.6 and 2.4 µM, respectively.2 β-oxocarboxylic acids such as 1,4-DPCA have also been found to inhibit the asparaginyl-hydroxylase, factor inhibiting HIF (FIH), with an IC50 value of 60 µM.3
1  Jaakkola, P., Mole, D.R., Tian, Y., et al. Targeting of HIF-α to the von Hippel-Lindau ubiquitylation complex by O2-regulated prolyl hydroxylation. Science 292 468-472 (2001).
2  Franklin, T.J., Morris, W.P., Edwards, P.N., et al. Inhibition of prolyl 4-hydroxylase in vitro and in vivo by members of a novel series of phenanthrolinones. Biochem J 353 333-338 (2001).
3  Banerji, B., Conejo-Garcia, A., McNeill, L.A., et al. The inhibiton of factor inhibiting hypoxia-inducible factor (FIH) by β-oxocarboxylic acids. Chem Commun (2005).

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Pricing Information

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Size Price Quantity
5 mg €18.00
10 mg €35.00
25 mg €82.00
50 mg €144.00
Pricing updated 2010-08-01.
Prices are subject to change without notice.