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Chromatin/Epigenetic HIF/HIF Prolyl-Hydroxylase HIF-PHD Inhibitor II

HIF-PHD Inhibitor II

Catalog No. T3180   CAS 1193383-09-3
Synonyms: JNJ-42041935

JNJ-42041935 is a potent (pKi = 7.3-7.9), 2-oxoglutarate competitive, reversible, and selective inhibitor of PHD enzymes.

HIF-PHD Inhibitor II, CAS 1193383-09-3
Pack Size Availability Price/USD Quantity
2 mg In stock 69.00
5 mg In stock 124.00
10 mg In stock 204.00
25 mg In stock 367.00
1 mL * 10 mM (in DMSO) In stock 132.00
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Purity 99.95%
Purity 98.00%
Purity 100.00%
Biological Description
Chemical Properties
Storage & Solubility Information
Description JNJ-42041935 is a potent (pKi = 7.3-7.9), 2-oxoglutarate competitive, reversible, and selective inhibitor of PHD enzymes.
Targets&IC50 PHD1 : pKi:7.91±0.04 ,   PHD2 : ic50 7.29±0.05 ,   PHD3 : ic50 7.65±0.09
Kinase Assay The potency of JNJ-42041935 for inhibition of the structurally related enzyme FIH is assessed by methods similar to those described for PHD2. In brief, activity of FIH is determined using purified glutathione transferase-tagged full-length FIH amino acids 1 to 350 and a synthetic HIF-1α peptide corresponding to residues Asp788 to Leu822. Compounds are preincubated with 17.1 nM FIH for 30 min, followed by a 10-min incubation with 1 μM [2-14C]2-oxoglutarate, in the presence of 10 μM FeNH4SO4 in reaction buffer. The selectivity of JNJ-42041935 for inhibition of a range of other targets available for testing in commercial assays is also assessed at concentrations of 1 and 10 μM[1].
Animal Research
Animal Model: Balb/C mice
Synonyms JNJ-42041935
Purity 99.95%
Molecular Weight 346.65
Formula C12H6ClF3N4O3
CAS No. 1193383-09-3

Storage

0-4℃ for short term (days to weeks), or -20℃ for long term (months).

Solubility Information

DMSO: 36 mg/mL

( < 1 mg/ml refers to the product slightly soluble or insoluble )

Citations

References and Literature
1. Barrett TD, et al. Pharmacological characterization of 1-(5-chloro-6-(trifluoromethoxy)-1H-benzoimidazol-2-yl)-1H-pyrazole-4-carboxylic acid (JNJ-42041935), a potent and selective hypoxia-inducible factor prolyl hydroxylase inhibitor. Mol Pharmacol. 2011

Related compound libraries

This product is contained In the following compound libraries:
Bioactive Compound Library Inhibitor Library Anti-cancer Compound Library Epigenetics Compound Library Protease Inhibitor Library Fluorochemical Library Anti-Metabolism Disease Compound Library

Related Products

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IOX 2 FG2216 Molidustat Glucosamine hydrochloride HIF-PHD Inhibitor II MK8617 Vadadustat Desidustat

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