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Merck

SML4327

1,4-DPCA

new

≥98% (HPLC)

Synonym(s):

1,4-Dihydrophenonthrolin-4-one-3-carboxylic acid, 4-Hydroxy-1,10-phenanthroline-3-carboxylic acid, 4-Oxo-1,4-dihydro-1,10-phenanthroline-3-carboxylic acid, FG-0041, FG0041, FG 0041

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About This Item

Empirical Formula (Hill Notation):
C13H8N2O3
CAS Number:
Molecular Weight:
240.21
UNSPSC Code:
12352200
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Quality Level

Assay

≥98% (HPLC)

form

powder

color

white to beige

solubility

DMSO: 2 mg/mL, clear (warmed)

storage temp.

-10 to -25°C

Biochem/physiol Actions

1,4-DPCA potently inhibits collagen prolyl-4-hydroxylase (P4H; IC50 ~ 2 µM), HIF-prolyl hydroxylase, and TET1/TET2 enzymes (pIC50 5.42/5.26), impacting collagen biosynthesis, hypoxia signaling, and DNA demethylation. Through 2-oxoglutarate competition, it reduces proline hydroxylation, stabilizes HIF-1α protein levels, affecting collagen maturation, decreasing CD44+/CD24-/low cancer stem cells, and modulating α-KG/succinate levels. Consequently, 1,4-DPCA demonstrates significant anti-cancer effects in breast cancer models, inhibiting tumor growth, metastasis, and altering cellular metabolism via downregulation of HIF-1 targets LDHA/PDK1. FG-0041 in combination with Y-27632 initiates differentiation of mesenchymal stem cells into neuron-like cells. Notably, DPCA enhances CAR-T cell expansion and function, improving chemotherapeutic efficacy, potentially by affecting oxygen consumption, extracellular acidification, and reactive oxygen species levels.

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