目录号 | 产品详情 | 靶点 | |
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T7848 | HIF/HIF Prolyl-Hydroxylase HIF | ||
PT-2385 是一种选择性HIF-2α抑制剂,Ki< 50 nM。 | |||
T21653 | HIF/HIF Prolyl-Hydroxylase | ||
1,4-DPCA 是一种脯氨酰羟化酶抑制剂,对人源包皮成纤维细胞中胶原羟基化的 IC50 为 2.4 μM,对因子抑制 HIF (FIH) 的 IC50 为 60 μM。 | |||
T7880 | HIF/HIF Prolyl-Hydroxylase | ||
IOX4 是选择性 PHD2抑制剂,IC50=1.6 nM,在细胞和野生型小鼠中诱导 HIFα表达,可透过血脑屏障。它与 PHD2 特性位点的 2-氧代戊二酸竞争并置换。 | |||
T2488 | Ferroptosis HIF/HIF Prolyl-Hydroxylase HIF | ||
BAY 87-2243 是一种选择性的低氧诱导因子-1 抑制剂。 | |||
T5S2347 | Others HIF/HIF Prolyl-Hydroxylase Antibacterial | ||
Deoxyshikonin (Arnebin 7) 是从紫草中分离的天然产物,具有抗肿瘤活性,在体外具有促血管生成作用。它和没食子酸十二烷基酯在体内外均与青霉素有显着的协同抗菌活性。 | |||
T15219 | Others HIF/HIF Prolyl-Hydroxylase | ||
Enarodustat (JTZ-951) 是口服具有活力的 hypoxia-inducible factor prolyl hydroxylase 抑制剂,EC50=0.22 μM,有用于肾性贫血症的研究潜力。 | |||
T11561 | HIF/HIF Prolyl-Hydroxylase HIF | ||
HIF-2α-IN-2 是低氧诱导因子抑制剂,IC50=16 nM。 | |||
T21806 | HDAC | ||
HNHA 是组蛋白去乙酰化酶抑制剂。它通过 p21诱导将细胞周期阻滞在 G1/S 期,抑制肿瘤生长及肿瘤新生血管形成。HNHA 可能是一种有效的抗乳腺癌药物。 | |||
T64336 | HIF/HIF Prolyl-Hydroxylase | ||
tert-butyl 4-[[1-[(4-chlorophenyl)methyl]-3-hydroxy-2-oxopyridin-4-yl]methyl]piperazine-1-carboxylate 是一种脯氨酰羟化酶抑制剂。 | |||
T29797 | VEGFR HIF/HIF Prolyl-Hydroxylase HIF | ||
AKB-6899 是脯氨酰羟化酶结构域 3 (PHD3) 的抑制剂,可增加 GM-CSF 处理的巨噬细胞产生的 VEGF 受体的可溶形式 (sVEGFR-1)。 AKB-6899 能稳定 HIF-2α,从而诱导肿瘤相关巨噬细胞产生 sVEGFR-1 并减少肿瘤生长。 |
目录号 | 产品名/同用名 | 种属 | 表达系统 | ||
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TMPH-01280 | EGLN1 Protein, Human, Recombinant (His & Myc) | Human | E. coli | ||
Cellular oxygen sensor that catalyzes, under normoxic conditions, the post-translational formation of 4-hydroxyproline in hypoxia-inducible factor (HIF) alpha proteins. Hydroxylates a specific proline found in each of the oxygen-dependent degradation (ODD) domains (N-terminal, NODD, and C-terminal, CODD) of HIF1A. Also hydroxylates HIF2A. Has a preference for the CODD site for both HIF1A and HIF1B. Hydroxylated HIFs are then targeted for proteasomal degradation via the von Hippel-Lindau ubiquitination complex. Under hypoxic conditions, the hydroxylation reaction is attenuated allowing HIFs to escape degradation resulting in their translocation to the nucleus, heterodimerization with HIF1B, and increased expression of hypoxy-inducible genes. EGLN1 is the most important isozyme under normoxia and, through regulating the stability of HIF1, involved in various hypoxia-influenced processes such as angiogenesis in retinal and cardiac functionality. Target proteins are preferentially recognized via a LXXLAP motif.
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