| Name | FG-2216 |
| Description | FG-2216 (YM-311) is a potent HIF-prolyl hydroxylase inhibitor for the PDH2 enzyme (IC50: 3.9 uM); orally bioavailable and induced reversible and significant Epo induction in vivo. |
| Kinase Assay | Metabolic Labeling and Gel Electrophoresis: COLO 320DM cells (200,000) are injected into each well of 12-well plastic plates 2 days before incubation in the presence of KNK437 for 1 h before heat shock. The cells are then heat-shocked at 42°C for 90 min or kept at 37°C for the same length of time and incubated at 37°C for 2 h. For metabolic labeling, cells are washed with PBS without Ca2+ or Mg2+ and incubated for 1 h with 1.22 MBq of [35S]methionine in 250 μL of methionine-free DMEM supplemented with 10% dialyzed fetal bovine serum. After metabolic labeling, cells are washed twice with PBS and lysed in a buffer containing 1% NP40, 0.15 M NaCl, 50 mM Tris-HCl (pH 8.0), 5 mM EDTA, and protease inhibitors [0.2 mM 4-(2-aminoethyl)benzenesulfonyl fluoride hydrochloride, 2 mM N-ethylmaleimide, 1 μg/mL pepstatin, and 1 μg/mL leupeptin]. After centrifugation at 12,000×g for 20 min, cell extracts containing equal amounts of trichloroacetic acid-insoluble radioactivity are analyzed by two-dimensional gel electrophoresis (the one-dimensional gel electrophoresis is a nonequilibrium pH gradient gel electrophoresis, and the two-dimensional gel electrophoresis is 10% SDS-PAGE). |
| In vitro | FG-2216 shows the ability to stabilize HIF-α to stimulate EPO secretion. [1] |
| In vivo | In male rhesus macaques, FG-2216 (60 mg/kg, p.o.), induces significant and reversible Epo induction, and induces a small elevation of HbF expression. [2] |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| Solubility Information | Ethanol : < 1 mg/mL (insoluble or slightly soluble)
H2O : < 1 mg/mL (insoluble or slightly soluble)
DMSO : 50 mg/mL (178.15 mM)
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| Keywords | IOX 3 | fetal | IOX3 | inhibit | HIFs | Hypoxia-inducible factors | prolyl | IOX-3 | HIF/HIF Prolyl-Hydroxylase | erythropoietin | HIF-PH | YM311 | FG-2216 | hydroxylase | hemoglobin | PHD2 | YM 311 | HIF | Inhibitor |
| Inhibitors Related | Deferoxamine Mesylate | Hydralazine hydrochloride | 1,4-DPCA | DMOG | Chlorogenic Acid | Roxadustat | Glucosamine | Hydroxycitric acid tripotassium hydrate | Glucosamine hydrochloride | Minocycline hydrochloride | Oltipraz | Glucosamine sulfate |
| Related Compound Libraries | Bioactive Compound Library | HIF-1 Signaling Pathway Compound Library | Anti-Cancer Clinical Compound Library | Drug Repurposing Compound Library | Inhibitor Library | Anti-Aging Compound Library | Clinical Compound Library | Bioactive Compounds Library Max | Anti-Cancer Compound Library | Anti-Cancer Drug Library |
United States
