目录号 | 产品详情 | 靶点 | |
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T3169 | HIF/HIF Prolyl-Hydroxylase HIF | ||
KC7F2 是缺氧诱导因子HIF-1通道抑制剂,在 LN229-HRE-AP 细胞中的IC50=20 μM,可用作抗癌试剂。 | |||
T6S0071 | HIF/HIF Prolyl-Hydroxylase STAT PD-1/PD-L1 | ||
Fraxinellone 是从白鲜的根皮中分离出来的一种天然产物,是PD-L1抑制剂,可抑制HIF-1α蛋白质合成。它通过靶向 PD-L1,有用于癌症免疫的潜力。 | |||
T22022 | HIF | ||
Adaptaquin 是缺氧诱导因子脯氨酰羟化酶(HIF-PH)的抑制剂。 | |||
T12675L | HIF/HIF Prolyl-Hydroxylase HIF | ||
PT2399 是高选择性的HIF-2α拮抗剂,能直接结合 HIF-2α PAS B 结构域,IC50=6 nM,具有显著的体内抗肿瘤特性。 | |||
T13398 | HIF | ||
ZINC13466751 是有效的 HIF-1α/von Hippel-Lindau 相互作用抑制剂,抑制作用的 IC50为 2.0 µM。 | |||
T7848 | HIF/HIF Prolyl-Hydroxylase HIF | ||
PT-2385 是一种选择性HIF-2α抑制剂,Ki< 50 nM。 | |||
T0244 | Influenza Virus HIF/HIF Prolyl-Hydroxylase IFNAR | ||
Tilorone dihydrochloride 是一种具有口服活性的干扰素诱导剂,具有抗肿瘤和抗炎作用。 | |||
T4106 | HIF/HIF Prolyl-Hydroxylase | ||
MK-8617 是一种口服具有活力的低氧诱导因子脯氨酰羟化酶 1-3 (HIF PHD1-3) 泛抑制剂,对于PHD2的IC50=1 nM。 | |||
T5392 | HIF/HIF Prolyl-Hydroxylase | ||
TP0463518 是缺氧诱导因子脯氨酰羟化酶抑制剂,能够作用于人 PHD2(Ki= 5.3 nM)。它还抑制人PHD1/PHD3,IC50分别为 18 和 63 nM,以及猴 PHD2(IC50=22 nM)。 | |||
T13050 | HIF/HIF Prolyl-Hydroxylase HIF | ||
SYP-5 是新型HIF-1抑制剂,阻碍肿瘤细胞侵袭和血管生成。 |
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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