1,4-DPCA, Prolyl 4-hydroxylase (P4H) Inhibitor


Catalog No. size PriceQuantity
M60288-2S 2 mg solid $79
M60288-10S 10mg solid $312

Description

1, 4-DPCA is a selective and cell permeable prolyl 4-hydroxylase (P4H) inhibitor. It inhibits α-prolyl4-hydroxylase, an oxygen-sensing enzyme that targets the pro-angiogenic factor HIF-1α for destruction upon hydroxylation of a specific proline residue. It also inhibits asparaginyl-hydroxylase factor inhibiting HIF (FIH) and is useful for controlling excess collagen deposition in pathological fibrosis.

Product information

CAS Number: 331830-20-7

Molecular Weight: 240.21

Formula: C13H8N2O3

Chemical Name: 4-oxo-1,4-dihydro-1,10-phenanthroline-3-carboxylic acid

Smiles: OC(=O)C1=CNC2=C(C=CC3=CC=CN=C32)C1=O

InChiKey: XZZHOJONZJQARN-UHFFFAOYSA-N

InChi: InChI=1S/C13H8N2O3/c16-12-8-4-3-7-2-1-5-14-10(7)11(8)15-6-9(12)13(17)18/h1-6H,(H,15,16)(H,17,18)

Technical Data

Appearance: Solid Power.

Purity: ≥98% (or refer to the Certificate of Analysis)

Solubility: DMSO up to 10 mM, EtOH up to 20 mM

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥360 days if stored properly.

Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined.

HS Tariff Code: 382200

How to use

In Vitro:

1, 4-DPCA was used at 10 µM final concentration in vitro and in cellular assays.

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.

References:

  1. Jaakkola P, et al. Targeting of HIF-alpha to the von Hippel-Lindau ubiquitylation complex by O2-regulated prolyl hydroxylation. (2001) Science. 292(5516):468-72.
  2. Franklin TJ, et al. Inhibition of prolyl 4-hydroxylase in vitro and in vivo by members of a novel series of phenanthrolinones. (2001) Biochem J. 353(Pt 2):333-8.
  3. Banerji B, et al. The inhibition of factor inhibiting hypoxia-inducible factor (FIH) by beta-oxocarboxylic acids. (2005) Chem Commun (Camb). (43):5438-40.

Products are for research use only. Not for human use.

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