IOX2 - Moligand™, 10mM in DMSO , Inhibitor of egl-9 family hypoxia inducible factor 1;Inhibitor of lysine demethylase 2A;Inhibitor of lysine demethylase 5C, CAS No.931398-72-0, Inhibitor of egl-9 family hypoxia inducible factor 1;Inhibitor of lysine demethylase 2A;Inhibitor of lysine demethylase 5C

CAS: 931398-72-0 Cat. No.: I407921 Molecular Weight: 352.34 EC Number: 804-733-4

GRADE & PURITY Moligand™, 10mM in DMSO

Synonyms

JICL38 | Glycine, N-[[1,2-dihydro-4-hydroxy-2-oxo-1-(phenylmethyl)-3-quinolinyl]carbonyl]-

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

Overview

Information

IOX2 IOX2 (JICL38) is a potent inhibitor of HIF-1α prolyl hydroxylase-2 (PHD2) with IC50 of 21 nM in a cell-free assay, >100-fold selectivity over JMJD2A, JMJD2C, JMJD2E, JMJD3, or the 2OG oxygenase FIH.
In vitro

IOX2 potently inhibits PHD2 (IC50 of 21 nM) with over 100-fold selectivity compared to inhibition of JMJD2A, JMJD2C, JMJD2E, JMJD3, or the 2OG oxygenase FIH (IC50s <100 μM). IOX2 is active in cells, inhibiting HIF-1α hydroxylation in RCC4 cells at 50 μM. Hypoxia Inducible Factor (HIF) is regulated by the hydroxylation of prolyl residues in oxygen-dependent degradation domains in the HIF-1α subunit, which mark it for degradation by the proteosome. 1,2 HIF prolyl hydroxylation is catalyzed by prolyl hydroxylase domain enzymes (PHD1, 2, and 3), members of the Fe(II) and 2-oxoglutarate (2OG) oxygenase family. They require dioxygen as a cosubstrate, thus acting as the hypoxia-sensing component of the HIF system. The activity of PHD is suppressed by hypoxia, increasing both the abundance and activity of the HIF transcriptional complex.

In vivo

Cell Data

cell lines：

Concentrations：

Incubation Time：

Powder Purity:≥99%

Specifications

Synonyms

JICL38 | Glycine, N-[[1, 2-dihydro-4-hydroxy-2-oxo-1-(phenylmethyl)-3-quinolinyl]carbonyl]-

Specifications & Purity

Moligand™, 10mM in DMSO

Biochemical and Physiological Mechanisms

IOX2 (JICL38) is a potent inhibitor of HIF-1α prolyl hydroxylase-2 (PHD2) with IC50 of 21 nM in a cell-free assay, >100-fold selectivity over JMJD2A, JMJD2C, JMJD2E, JMJD3, or the 2OG oxygenase FIH.

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

This product requires cold chain shipping. Ground and other economy services are not available.

Grade

Moligand™

Action Type

INHIBITOR

Mechanism of action

Inhibitor of egl-9 family hypoxia inducible factor 1;Inhibitor of lysine demethylase 2A;Inhibitor of lysine demethylase 5C

Names and Identifiers

• Isomeric SMILES: C1=CC=C(C=C1)CN2C3=CC=CC=C3C(=C(C2=O)C(=O)NCC(=O)O)O
• WGK Germany: 3
• Molecular Weight: 352.34
• Reaxy-Rn: 12851765
• Reaxys-RN_link_address: https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=12851765&ln=

Associated Targets(Human)

EGLN1 Tclin Egl nine homolog 1 (3 Activities)

Discover Target: EGLN1

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

KDM5C Tchem Lysine-specific demethylase 5C (1 Activities)

Discover Target: KDM5C

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

KDM2A Tchem Lysine-specific demethylase 2A (1 Activities)

Discover Target: KDM2A

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)