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N-[(4-hydroxy-8-iodoisoquinolin-3-yl)carbonyl]glycine

Development stage
Preclinical
Modality
Small Molecules
01

Overview

N‑[(4‑hydroxy‑8‑iodoisoquinolin‑3‑yl)carbonyl]glycine (also known as 4HG or CHEMBL509064; DrugBank ID DB07112), is a synthetic small molecule and experimental compound. It acts as an inhibitor of prolyl hydroxylase domain-containing protein 2 (PHD2/Egl nine homolog 1), an enzyme that regulates the stability of hypoxia-inducible factor alpha (HIFα). By binding to the active site of PHD2 and chelating its catalytic iron ion (Fe²⁺), this compound blocks HIFα hydroxylation and degradation under normoxic conditions. This mechanism can stabilize HIFα levels and modulate cellular responses to hypoxia. The compound has been studied in structural biology for its interaction with PHD2 but is not approved for clinical use[1][6][4].

Other names
2-((4-hydroxy-8-iodoisoquinolin-3-yl)formamido)acetic acid2-[(4-hydroxy-8-iodoisoquinolin-3-yl)formamido]acetic acidN-((4-hydroxy-8-IODOISOQUINOLIN–3-YL)CARBONYL)GLYCINE2-(4-hydroxy–8–iodoisoquinoline–3-carboxamido)acetic acid{[(4-hydroxy–8–iodoisoquinolin–3-YL)carbonyl]amino}acetic acid
02

Targets

EGLN1 (Prolyl hydroxylase domain-containing protein 2)

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