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JNJ-42041935

Catalog No. T3180   CAS 1193383-09-3
Synonyms: HIF-PHD Inhibitor II

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

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JNJ-42041935 Chemical Structure
JNJ-42041935, CAS 1193383-09-3
Pack Size Availability Price/USD Quantity
1 mg In stock $ 34.00
2 mg In stock $ 48.00
5 mg In stock $ 80.00
10 mg In stock $ 122.00
25 mg In stock $ 222.00
50 mg In stock $ 372.00
100 mg In stock $ 597.00
500 mg In stock $ 1,260.00
1 mL * 10 mM (in DMSO) In stock $ 89.00
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Purity: 100%
Purity: 99.95%
Purity: 98%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description JNJ-42041935 (HIF-PHD Inhibitor II) is a potent (pKi = 7.3-7.9), 2-oxoglutarate competitive, reversible, and selective inhibitor of PHD enzymes.
In vitro JNJ-42041935 is the most potent inhibitor of PHD2181–417 with a pIC50 value of 7.0±0.03. JNJ-42041935 also inhibits full-length PHD1, PHD2, and PHD3 enzymes (pKi values 7.91±0.04, 7.29 ±0.05, and 7.65±0.09, respectively) [1].
In vivo JNJ-42041935 has been evaluated for its capability to selectively inhibit prolyl hydroxylase domain (PHD) enzymes compared to the effect of intermittent, high doses (50 μg/kg i.p.) of an erythropoietin receptor agonist in a rat model of inflammation-induced anemia. The study demonstrates that JNJ-42041935, administered at a dose of 100 µmol/kg orally once daily for 14 days, successfully ameliorates inflammation-induced anemia, whereas erythropoietin shows no efficacy. Further, a 5-day consecutive oral administration of JNJ-42041935 at 100 µmol/kg led to a doubling in reticulocyte count, a 2.3 g/dl increase in hemoglobin levels, and a 9% rise in hematocrit values. Additionally, a single oral dose of 300 µmol/kg of JNJ-42041935 resulted in a 2.2 ± 0.3-fold increase in peritoneal bioluminescence, relative to luciferase-treated vehicle controls in mice, indicating enhanced activity two hours post-administration [1].
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].
Synonyms HIF-PHD Inhibitor II
Molecular Weight 346.65
Formula C12H6ClF3N4O3
CAS No. 1193383-09-3

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 50 mg/mL (144.24 mM)

TargetMolReferences 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:
Anti-Metabolism Disease Compound Library Anti-Cancer Compound Library Glutamine Metabolism Compound Library Bioactive Compounds Library Max Reprogramming Compound Library Inhibitor Library Transcription Factor-Targeted Compound Library Glycolysis Compound Library Metabolism Compound Library Anti-Cancer Metabolism Compound Library

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Keywords

JNJ-42041935 1193383-09-3 Chromatin/Epigenetic Metabolism HIF/HIF Prolyl-Hydroxylase HIF-PH inhibit HIFs JNJ42041935 Inhibitor Hypoxia-inducible factors JNJ 42041935 HIF-PHD Inhibitor II inhibitor

 

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