HIF
Hypoxia inducible factors (HIFs) are heterodimeric proteins belonging to the basic helix-loop-helix-PAS (bHLH/PAS) family of transcription factors that mediate the primary transcriptional response to stress caused by hypoxia (accessible O2 level < 2%). HIFs are characterized by containing two subunits, including O2-labile α subunit (HIFα) and constitutively expressed β subnit (HIFβ). Mammalian HIFα consists of three isoforms, including HIF1α, HIF2α and HIF3α, which play an essential role in the regulation of HIF activity by O2 availability. Under normal O2 tension, HIFα is hydroxylated at the two conserved proline residues within the O2-dependent degradation (ODD) domain by prolylhydroxylase domain proteins (PHDs) and undergoes proteosomal degradation catalyzed by a complex formed by E3 ubiquitin ligase and the von Hippel-Lindau protein (pVHL); while, under hypoxia, HIFα stabilizes with PHDs being deactivated and hence induce transcription of genes with adaptive functions.
- C4887 2,4-DPDSummary: HIF-PH竞争性抑制剂,细胞通透性
- C4752 JNJ-42041935Summary: 缺氧诱导因子(HIF)脯氨酰羟化酶(PHD)抑制剂
- C4377 AdaptaquinSummary: HIF-脯氨酰羟化酶-2(PHD2)抑制剂
- C4321 Octyl-α-ketoglutarateSummary: 脯氨酰羟化酶(PHD)活化剂
- B6106 Daprodustat(GSK1278863)中文名: 达普司他Summary: HIF-脯氨酰羟化酶抑制剂
- B5851 FG2216Target: Pyruvate dehydrogenases (PDH)Summary: HIF-脯氨酰羟化酶抑制剂
- B1115 BAY 87-2243Target: Hypoxia Inducible Factors (HIFs)Summary: 有效的HIF-1选择性抑制剂
- A4506 DMOGTarget: Hypoxia-Inducible Factor Prolyl Hydroxylase Inhibitors (HIF-PHIs)Summary: 细胞通透的竞争性HIF-PH抑制剂
- A4509 PX 12Target: TrxSummary: Trx-1抑制剂
- A4507 KC7F2Summary: HIF-1α抑制剂