HIF/HIF Prolyl-Hydroxylase Modulator

THS-044 is a modulator of the formation of the HIF2α/ARNT heterodimer. THS-044 binding stabilizes the HIF2α PAS-B folded state (K_D = 2 μM), for regulating HIF2 activity in endogenous and pathological settings, and does not bind to HIF1α or ARNT PAS-B. THS-044 can be used for the study of diseases related to hypoxia.

Ceruloplasmin is a copper-binding ferroxidase and serum copper carrier. Ceruloplasmin promotes FPN1-mediated iron export by catalyzing ferrous iron oxidation, maintains the protein stability of ferroportin, and assists transferrin and lactoferrin in completing iron binding; it regulates HIF, AMPK, PPARα, and PGC1α, exerting antioxidant effects and inhibiting ferroptosis (Ferroptosis). Ceruloplasmin can be used in research on posthemorrhagic anemia, hemolytic anemia, neurodegenerative diseases, NAFLD, metabolic diseases, hereditary aceruloplasminemia, hepatocellular carcinoma, and ischemia-reperfusion injury.

VU 0364439 is a mGlu4 positive allosteric modulator with an EC₅₀ of 19.8 nM. VU 0364439 modulates the GRM4/CBX4/HIF-1α signaling pathway by enhancing GRM4-CBX4 interaction. VU 0364439 can be used for the research of parkinson’s disease.

Acetylarenobufagin is a steroidal hypoxia inducible factor-1 (HIF-I) modulator.