化合物FG-2216 T2445

Product Introduction
Bioactivity


英文名: FG-2216

描述: FG-2216 (YM-311) 是一种有效的、口服具有活力的HIF 脯氨酰羟化酶-2 (PHD2) 抑制剂，IC50=3.9 nM。它在体内能够诱导促红细胞生成素生成和胎儿血红蛋白的表达。

激酶实验: 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).

体外活性: FG-2216 展现出稳定 HIF-α 以刺激 EPO 分泌的能力。[1]

体内活性: 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]

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

溶解度: Ethanol : < 1 mg/mL (insoluble or slightly soluble)
H2O : < 1 mg/mL (insoluble or slightly soluble)
DMSO : 50 mg/mL (178.15 mM)


关键字: 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

相关产品: SYP-5 | 1,4-DPCA | dencichine | Velutin | Oroxylin A | Panaxadiol | Albendazole | HIF-1 alpha (556-574) (TFA) | Glucosamine sulfate | Ethyl 3,4-dihydroxybenzoate

相关库: Anti-Aging Compound Library | Drug Repurposing Compound Library | Anti-Cancer Metabolism Compound Library | Transcription Factor-Targeted Compound Library | Angiogenesis related Compound Library | Anti-Cancer Drug Library | Inhibitor Library | Anti-Cancer Clinical Compound Library | Epigenetics Compound Library | Metabolism Compound Library

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