400093

HIF-PHD Inhibitor II, JNJ-42041935

The HIF-PHD Inhibitor II, JNJ-42041935 controls the biological activity of HIF-PHD. This small molecule/inhibitor is primarily used for Cell Structure applications.

• Synonym(s): HIF-PHD Inhibitor II, JNJ-42041935, 1-(5-Chloro-6-(trifluoromethoxy)-1H-benzoimidazol-2-yl)-1H-pyrazole-4-carboxylic acid, HIF Prolyl Hydroxylase Inhibitor II
• Empirical Formula (Hill Notation): C₁₂H₆ClF₃N₄O₃
• CAS Number: 1193383-09-3
• Molecular Weight: 346.65
• MDL number: MFCD28900740
• UNSPSC Code: 12352200
• NACRES: NA.28

Properties

• Quality Level: 100
• Assay: ≥99% (HPLC)
• form: solid
• manufacturer/tradename: Calbiochem^®
• storage condition: OK to freeze; protect from light
• color: white
• solubility: DMSO: 100 mg/mL
• shipped in: ambient
• storage temp.: 2-8°C
• SMILES string: ClC1=CC2=C(NC(N3C=C(C=N3)C(O)=O)=N2)C=C1OC(F)(F)F

Description

General description

A cell-permeable benzimidazolopyrazole compound that acts as an active-site binding, iron insensitive, 2-oxoglutarate competitive, reversible and potent inhibitor of PHD1, 2 and 3 isozymes (pK_i = 7.91, 7.29 and 7.65, respectively). Displays >100-fold selectivity over FIH (factor inhibiting hydroxylase; pIC₅₀ ~ 4) and minimal affinity towards a panel of receptors, enzymes and kinases. Shown to elevate HIF-1α levels in Hep3B cells and stimulate erythropoietin secretion in mice, and reverse inflammation-induced anemia in rats (100 µM/kg).

A cell-permeable benzimidazolopyrazole compound that acts as an active-site binding, iron insensitive, 2-oxoglutarate competitive, reversible and potent inhibitor of PHD1, 2 and 3 isozymes (pK_i = 7.91, 7.29 and 7.65, respectively). Displays >100-fold selectivity over FIH (factor inhibiting hydroxylase; pIC₅₀ ~ 4) and minimal affinity towards a panel of receptors, enzymes and kinases. Shown to elevate HIF-1α levels in Hep3B cells and stimulate erythropoietin secretion in mice, and reverse inflammation-induced anemia in rats (100 µM/kg). Shown to inhibit malate dehydrogenase 2 (MDH2) activity and suppress mitochondrial respiration.

Packaging

Packaged under inert gas

Warning

Toxicity: Standard Handling (A)

Reconstitution

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.

Other Notes

Lee, K., et al., 2013. Angew. Chem. Int. Ed.52, In press.
Barrett, T.D., et al. 2011. Mol. Pharmacol.79, 910.
Rosen, M.D., et al. 2010. ACS Med. Chem. Lett. 1, 526.

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Safety Information

• Storage Class Code: 11 - Combustible Solids
• WGK: WGK 3
• Flash Point(F): Not applicable
• Flash Point(C): Not applicable