目录号 | 产品详情 | 靶点 | |
---|---|---|---|
TL0001 | Others HIF/HIF Prolyl-Hydroxylase | ||
Dencichine (ODAP) 是抑制从三七中分到的非蛋白氨基酸,可抑制 HIF-prolyl hydroxylase-2 的活性。 | |||
T7802 | HIF/HIF Prolyl-Hydroxylase HIF | ||
M1001 是较弱的HIF-2α激动剂,直接与 HIF-2α PAS-B 结构域结合,Kd=667 nM,能够提高 HIF-2α-ARNT 复合体之间的稳定性。 | |||
T6961 | HIF/HIF Prolyl-Hydroxylase HIF Autophagy | ||
PX-478 是一种 HIF-1α 抑制剂,具有选择性、口服活性和血脑屏障渗透性。PX-478 具有抗肿瘤活性,还可以保护糖尿病中的胰腺 β 细胞功能,用于 2 型糖尿病的研究。 | |||
T1823 | HIF/HIF Prolyl-Hydroxylase | ||
IOX2 (IOX 2) 是特异性的脯氨酰羟化酶-2 抑制剂,IC50=22 nM。 | |||
T1613 | MAO HIF/HIF Prolyl-Hydroxylase | ||
Hydralazine hydrochloride (Apresoline) 是一种直接作用的血管舒张剂,可抗高血压。 | |||
T9627 | HIF/HIF Prolyl-Hydroxylase | ||
PHD-1-IN-1 是口服有效的缺氧诱导因子脯氨酰羟化酶结构域 1抑制剂,IC50为 0.034 μM。它与活性位 Fe2+具有独特的单齿结合相互作用,并诱导形成一个 “Arg367-out” 口袋。 | |||
T1939 | HIF/HIF Prolyl-Hydroxylase HIF Autophagy | ||
DMOG (Dimethyloxalylglycine) 是 α-酮戊二酸辅因子的拮抗剂,是一种 HIF 脯氨酰羟化酶抑制剂,可导致蛋白HIF-1α的积聚和稳定,诱导细胞自噬。它是一种促血管生成剂,在结肠炎和腹泻动物模型中起保护作用。 | |||
T3180 | HIF/HIF Prolyl-Hydroxylase | ||
JNJ-42041935 (HIF-PHD Inhibitor II) 是一种高效的,竞争性的、选择性的脯氨酰羟化酶PHD 抑制剂,抑制PHD1(pKi= 7.91±0.04),PHD2 (pKi= 7.29 ±0.05) 和 PHD3 (pKi= 7.65±0.09)。 | |||
T13289 | Cannabinoid Receptor HIF/HIF Prolyl-Hydroxylase PPAR | ||
EHP-101 (VCE-004.8) 是一种口服有效的特异性PPARγ和CB2受体双重激动剂,可抑制脯氨酰-羟化酶(PHDs) 并激活HIF 通路。它是一种半合成的多靶点大麻喹啉,可减弱脂肪生成并防止饮食诱导的肥胖,具有抗炎活性。 | |||
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。 |
目录号 | 产品名/同用名 | 种属 | 表达系统 | ||
---|---|---|---|---|---|
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.
|