1. Metabolic Enzyme/Protease
  2. HIF/HIF Prolyl-Hydroxylase
  3. 1,4-DPCA

1,4-DPCA 

目录号: HY-121172
产品使用指南

1,4-DPCA,一种有效的选择性脯氨酰-4-羟化酶 (prolyl-4-hydroxylase) 抑制剂,也是人包皮成纤维细胞中的胶原蛋白羟基化抑制剂,IC50 为 2.4 µM。1,4-DPCA 抑制脯氨酰-4-羟化酶 α 同工型,可稳定 HIF-1α 蛋白。1,4-DPCA 还抑制 FIHIC50 为 60 μM。

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1,4-DPCA Chemical Structure

1,4-DPCA Chemical Structure

CAS No. : 331830-20-7

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Description

1,4-DPCA, a potent prolyl-4-hydroxylase inhibitor, is a collagen hydroxylation inhibitor in human foreskin fibroblasts with an IC50 of 2.4 µM. 1,4-DPCA inhibits prolyl-4-hydroxylases α isoforms stabilizes HIF-1α protein. 1,4-DPCA also inhibits factor inhibiting HIF (FIH) with an IC50 of 60 μM[1][2].

IC50 & Target

IC50: 2.4 µM (Collagen hydroxylation); 60 μM (Factor inhibiting HIF (FIH))[2]

In Vitro

1,4-DPCA (24 hours) treatment specifically increases the expression of multiple target genes, including the proangiogenic target genes Vegfa and Hmox1 and proglycolytic targets Ldh-a, Pgk1, Pdk1, and Glut1 in mouse B6 cells[1].
1,4-DPCA treatment significantly reduces the colony sizes of T4-2 (10 μM 1,4-DPCA) and ZR-75-1 cells (20 μM 1,4-DPCA). 1,4-DPCA-treated T4-2 cells form polarized spheroids in 3D culture. 1,4-DPCA treatment significantly reduces invasive branches in DA-MB-157 (20 μM 1,4-DPCA) and MDA-MB-231 (10 μM 1,4-DPCA) cells.1,4-DPCA inhibits the proliferation of T4-2, ZR-75-1, MDA-MB-157 and MDA-MB-231 cells[3].

In Vivo

1,4-DPCA treatment suppresses connective tissue ingrowth in porous porous poly (lactic-co-glycolic acid) (PLGA) discs implanted in the peritoneal cavity for 28 days in mice. 1,4-DPCA is found to be effective at inhibiting collagen deposition within and on the outer surface of the disc, and also limited connective tissue ingrowth, but not to the extent of glucocorticoid inhibition[2].

Molecular Weight

240.21

Formula

C₁₃H₈N₂O₃

CAS No.

331830-20-7

SMILES

O=C(C1=CN=C2C3=NC=CC=C3C=CC2C1=O)O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

References
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Keywords:

1,4-DPCAHIF/HIF Prolyl-HydroxylaseHypoxia-inducible factorsHIFsHIF-PHHIF-1αprolyl-4-hydroxylasewoundhealingP4HA1P4HA2P4HA3FIHInhibitorinhibitorinhibit

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HY-121172
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