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

HIF/HIF Prolyl-Hydroxylase

HIFs (Hypoxia-inducible factors) are transcription factors that respond to changes in available oxygen in the cellular environment, to be specific, to decreases in oxygen, or hypoxia. The HIF signaling cascade mediates the effects of hypoxia, the state of low oxygen concentration, on the cell. Hypoxia often keeps cells from differentiating. However, hypoxia promotes the formation of blood vessels, and is important for the formation of a vascular system in embryos, and cancer tumors. The hypoxia in wounds also promotes the migration of keratinocytes and the restoration of the epithelium. In general, HIFs are vital to development. In mammals, deletion of the HIF-1 genes results in perinatal death. HIF-1 has been shown to be vital to chondrocyte survival, allowing the cells to adapt to low-oxygen conditions within the growth plates of bones. HIF plays a central role in the regulation of human metabolism. Recently, several drugs that act as selective HIF prolyl-hydroxylase inhibitors have been developed.

HIF/HIF Prolyl-Hydroxylase 相关产品 (36):

Cat. No. Product Name Effect Purity
  • HY-12867
    PT-2385 Antagonist 99.48%
    PT-2385是选择性 HIF-2α 拮抗剂,Ki 值小于50 nM。
  • HY-15893
    DMOG Inhibitor 99.15%
    DMOG (Dimethyloxallyl Glycine) 是可渗透细胞,竞争型的 HIF-1α脯氨酰羟化酶 (HIF-PH) 抑制剂。
  • HY-13426
    Roxadustat Inhibitor 99.91%
    Roxadustat (FG-4592) 是一种口服的脯氨酰羟化酶 HIF 抑制剂,开发用于治疗贫血症。
  • HY-10231
    PX-478 Inhibitor >98.0%
    PX-478 是有抗癌活性的缺氧诱导因子-1α (HIF-1α) 抑制剂,对一些癌细胞系 IC50 为 20-30 μM。
  • HY-101277
    Vadadustat Inhibitor 98.02%
    Vadadustat是一种新型的可滴定口服的缺氧诱导因子脯氨酰羟化酶 (HIF-PH) 抑制剂,目前开发用于治疗贫血。
  • HY-111547
    M1001 Agonist
    M1001 是一种较弱的 HIF-2α 激动剂,直接与 HIF-2α PAS-B 结构域结合,Kd 值为 667 nM。M1001 能够增强 HIF-2α-ARNT 复合体之间的稳定性。
  • HY-112144
    TP0463518 Inhibitor
    TP0463518 是一种有效的缺氧诱导因子脯氨酰羟化酶 (PHDs) 抑制剂,作用于人 PHD2Ki 值为 5.3 nM。TP0463518 还抑制人 PHD1/PHD3IC50 分别为 18 和 63 nM,以及猴 PHD2,IC50 值为 22 nM。
  • HY-15836
    BAY 87-2243 Inhibitor 99.41%
    BAY 87-2243 是一种有效的选择性的 缺氧诱导因子-1 (HIF-1) 抑制剂。
  • HY-17608
    Daprodustat Inhibitor 99.39%
    Daprodustat 是一种口服的缺氧诱导因子脯氨酰羟化酶(HIFPH) 抑制剂,用于治疗与慢性肾病相关的贫血病。
  • HY-12519
    Oltipraz Inhibitor 99.82%
    Oltipraz抑制HIF-1α激活, 这种作用具时间依赖性, 浓度≥10μM时完全废除HIF-1α诱导, Oltipraz抑制HIF-1α, IC50为10μM。
  • HY-13671
    LW6 Inhibitor >98.0%
    LW6是新颖的HIF-1抑制剂,IC50值为4.4 μM。
  • HY-N0055
    Chlorogenic acid Inhibitor 99.29%
    Chlorogenic acid是咖啡和茶中的主要酚类化合物。 它具有一些重要的治疗作用,如抗氧化活性,抗菌,保肝,心脏保护,抗炎,解热,神经保护,抗肥胖,抗病毒,抗微生物,抗高血压。
  • HY-12654
    Molidustat Inhibitor 98.33%
    Molidustat是一种新型的HIF-PH抑制剂,对PHD1, PHD2, PHD3的IC50值分别为480 nM, 280 nM和450 nM。
  • HY-15468
    IOX2 Inhibitor 98.41%
    IOX2 是一种特异性的脯氨酰羟化酶-2 (PHD2) 抑制剂,IC50 为 22 nM。
  • HY-18777
    KC7F2 Inhibitor 99.61%
    KC7F2是一种有效的HIF-1途径抑制剂,可用作癌症治疗剂。
  • HY-N0293
    Paeoniflorin Inhibitor >98.0%
    Paeoniflorin由白芍根提取的天然产物。
  • HY-N0560
    Oroxylin A Inhibitor 99.90%
    千层纸素 (Oroxylin A) 是一种有活性的黄酮类化合物,具有较强的抗癌作用。
  • HY-100575
    Acriflavine Inhibitor 98.62%
    Acriflavine是用于标记高分子量RNA的荧光染料。它也是一种局部防腐剂。
  • HY-103227
    Desidustat Inhibitor >98.0%
    Desidustat是HIF羟化酶 (HIF hydroxylase) 的抑制剂, 来自专利专利WO 2014102818 A1化合物实例2。
  • HY-12832
    JNJ-42041935 Inhibitor 99.79%
    JNJ-42041935是高效的,竞争性和选择性的脯氨酰羟化酶PHD抑制剂,抑制PHD1, PHD2, and PHD3的pKi值分别为7.91±0.04,7.29 ±0.05和7.65±0.09。
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