目录号 | 产品详情 | 靶点 | |
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T16679 | HIF | ||
Belzutifan (MK-6482) 是具有口服活性的 HIF-2α选择性抑制剂,IC50为 9 nM。Belzutifan 具有提高的效力和改善的药代动力学特征。Belzutifan (MK-6482) 可以抑制透明细胞肾细胞癌。 | |||
T2763 | Others HIF/HIF Prolyl-Hydroxylase | ||
Panaxadiol (20(R)-Panaxadiol) 是从人参根中获得,具有神经保护和抗肿瘤作用,能够抑制程序性细胞死亡配体-1(PD-L1)的表达和肿瘤增殖。 | |||
T9890 | HIF | ||
HIF1-IN-3 (Benzenepropanamide, N-[(8-hydroxy-7-quinolinyl)(4-methoxyphenyl)methyl]-) 是HIF-1的有效抑制剂(EC50 = 0.9 μM),可用于抗癌的研究。 | |||
T50099 | Others HIF/HIF Prolyl-Hydroxylase | ||
HIF-2a translation inhibitor 是一种有效的HIF-2α翻译抑制剂,IC50=5 μM,能够抑制组成型和缺氧诱导的 HIF-2α 蛋白表达。其中 HIF-2α-IN-4 将 5'UTR 铁响应元件与氧传感联系起来。 | |||
T3289 | Others HIF/HIF Prolyl-Hydroxylase | ||
Amifostine (Ethyol) 是一种广谱细胞保护剂和辐射防护剂,具有清除自由基的作用。它可选择性保护正常组织免受放射线和化学疗法造成的损害。它是有效的 HIF-α1和 p53诱导剂,可降低肾脏毒性并具有抗血管生成作用。 | |||
T6S1315 | Virus Protease HIF/HIF Prolyl-Hydroxylase Autophagy | ||
Oroxylin A (Baicalein 6-methyl ether) 是一种有活性的黄酮,具有较强的抗癌作用。 | |||
T5684 | Apoptosis Others Reactive Oxygen Species HIF/HIF Prolyl-Hydroxylase NO Synthase Autophagy | ||
Ethyl 3,4-dihydroxybenzoate 是从花生种子的种皮中发现的脯氨酰羟化酶抑制剂,是一种抗氧化剂。它是胶原蛋白合成抑制剂,具有骨骼保护作用。它通过激活 NO 合酶并产生线粒体 ROS 来保护心肌,可诱导 ESCC 细胞自噬和凋亡。 | |||
T0153 | HIF/HIF Prolyl-Hydroxylase HIV Protease Reverse Transcriptase Nrf2 HIF | ||
Oltipraz (RP 35972) 是一种 Nrf2的强效激活剂。它时间依赖性地抑制 HIF-1α激活,IC50为 10 μM,浓度 ≥ 10 μM 时完全消除 HIF-1α诱导。 | |||
T2445 | HIF/HIF Prolyl-Hydroxylase | ||
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。 | |||
T3494 | Apoptosis Dehydrogenase HIF/HIF Prolyl-Hydroxylase HIF | ||
LW6 (HIF-1α inhibitor) 是一种新型 HIF-1抑制剂,IC50值为 4.4 μM。它降低 HIF-1α蛋白表达,但不影响 HIF-1β 表达。 |
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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