1. Metabolic Enzyme/Protease
  2. HIF/HIF Prolyl-Hydroxylase

JNJ-42041935 

Cat. No.: HY-12832 Purity: 99.93%
Data Sheet SDS Handling Instructions

JNJ-42041935 is a potent, competitive and selective inhibitor of prolyl hydroxylase PHD; inhibits PHD1, PHD2, and PHD3 with pKi values of 7.91±0.04, 7.29 ±0.05, and 7.65±0.09, respectively.

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JNJ-42041935 Chemical Structure

JNJ-42041935 Chemical Structure

CAS No. : 1193383-09-3

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Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO $132 In-stock
5 mg $120 In-stock
10 mg $190 In-stock
50 mg   Get quote  
100 mg   Get quote  

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Description

JNJ-42041935 is a potent, competitive and selective inhibitor of prolyl hydroxylase PHD; inhibits PHD1, PHD2, and PHD3 with pKi values of 7.91±0.04, 7.29 ±0.05, and 7.65±0.09, respectively.

IC50 & Target

pKi: 7.91±0.04 (PHD1), 7.29 ±0.05 (PHD2), 7.65±0.09(PHD3)[1]

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 is used to compare the effect of selective inhibition of PHD to intermittent, high doses (50 μg/kg i.p.) of an exogenous erythropoietin receptor agonist in an inflammation induced anemia model in rats. JNJ-42041935 (100 μmol/kg, once a day for 14 days) is effective in reversing inflammation induced anemia, whereas erythropoietin has no effect. Administration of JNJ-42041935 (100 μmol/kg p.o.) for 5 consecutive days resulted in a 2-fold increase in reticulocytes, an increase in hemoglobin by 2.3 g/dl, and an increase in the hematocrit of 9%. Two hours after oral administration of 300 μmol/kg JNJ-42041935, the bioluminescence over the peritoneal area is increased by 2.2 ± 0.3-fold relative to luciferase-treated vehicle controls in the mouse [1].

References
Preparing Stock Solutions
Concentration Volume Mass 1 mg 5 mg 10 mg
1 mM 2.8848 mL 14.4238 mL 28.8475 mL
5 mM 0.5770 mL 2.8848 mL 5.7695 mL
10 mM 0.2885 mL 1.4424 mL 2.8848 mL
Please refer to the solubility information to select the appropriate solvent.
Kinase Assay
[1]

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]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration
[1]

Mouse: JNJ-42041935 is administered at doses of 30, 100, and 300 μmol/kg to Balb/C mice . Plasma is collected 6 h after the dose. Plasma erythropoietin concentration is measured. The hematological effects of JNJ-42041935 are assessed by administering the 100 μmol/kg dose on 5 consecutive days and collecting blood anticoagulated with EDTA on day 8 (3 days after the last dose)[1]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
Molecular Weight

346.65

Formula

C₁₂H₆ClF₃N₄O₃

CAS No.

1193383-09-3

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Shipping

Room temperature in continental US; may vary elsewhere

Solvent & Solubility

DMSO: ≥ 36 mg/mL

* "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.

Purity: 99.93%

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JNJ-42041935
Cat. No.:
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