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JNJ-42041935 was the most potent inhibitor of PHD2181–417 with a pIC50 value of 7.0 ± 0.03. JNJ-42041935 caused a concentration-dependent elevation of cellular HIF-1α and erythropoietin release in Hep3B cells. JNJ-42041935 (100 μmol/kg, once a day for 14 days) was effective in reversing inflammation-induced anemia.
| Cell Experiment | |
|---|---|
| Cell lines | Hep3B cells |
| Preparation method | The potency of compounds for stabilization of intracellular HIF-1α and release of erythropoietin into the media was assessed in the human hepatoma cell line Hep3B. Cells were cultured in Dulbecco's modified Eagle's medium/high glucose (Invitrogen) supplemented with 10% fetal calf serum and 2 mM l-glutamine, 1% nonessential amino acids, 1 mM sodium pyruvate, 50 IU/ml penicillin, and 50 μg/ml streptomycin. A range of concentrations was incubated in 96-well plates with 30,000 cells/well for 24 h. Incubation media were collected, and cells were subsequently lysed for assessment of cellular HIF-1α content and erythropoietin concentration. |
| Concentrations | 1 to 10 μM |
| Incubation time | 24 h |
| Animal Experiment | |
|---|---|
| Animal models | Balb/C mice |
| Formulation | |
| Dosages | 30, 100, and 300 μmol/kg |
| Administration | p.o. |
| Molecular Weight | 346.65 |
| Formula | C12H6ClF3N4O3 |
| CAS Number | 1193383-09-3 |
| Solubility (25°C) | DMSO ≥ 30 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Related HIF Products |
|---|
| HIF-1α-IN-3
HIF-1α-IN-3 is a hypoxia-selective HIF-1α inhibitor. |
| HIF-2α-IN-2
HIF-2α-IN-2 is a hypoxia-inducible factors (HIF-2α) inhibitor, has an IC50 of 16 nM in scintillation proximity assay (SPA). |
| PRLX-93936 dihydrochloride
PRLX-93936 dihydrochloride is a HIF-1α inhibitor with anticancer activity. |
| 3-Aminobenzoic acid
3-Aminobenzoic acid is a hypoxia-inducible factor-1α (HIF-1α) inhibitor. |
| Steppogenin
Steppogenin is a potent inhibitor of HIF-1α and DLL4, with IC50 values of 0.56 and 8.46 μM, respectively. |
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