hif 2α in 2

HIF-2α agonist 2 is an HIF-2α agonist with an EC50 value of 1.68 μM for HIF-2α. HIF-2α agonist 2 can promote the stability of the ARNT A/B ring in the 3z structure of HIF-2a-ARNT complex without cytotoxicity to 786-o-Reha-Luc cells. HIF-2α agonist 2 can be used in the study of oxygen metabolism and is closely related to the occurrence of cancer.

HIF-2α-IN-2 is a hypoxia-inducible factor (HIF-2α) inhibitor with an IC50 of 16 nM in scintillation proximity assay (SPA).

HIF-2a translation inhibitor is a potent HIF-2α translation inhibitor with IC50=5 μM that inhibits constitutive and hypoxia-induced HIF-2α protein expression. Among them, HIF-2α-IN-4 associates the 5'UTR iron response element with oxygen sensing.

HIF-1/2α-IN-2 is a selective inhibitor targeting hypoxia-inducible factors 1α and 2α (HIF-1α and HIF-2α). It induces a state of cellular iron deficiency by inhibiting the activity of iron-sulfur cluster assembly protein 2 (ISCA2), thereby reducing HIF-2α synthesis and ultimately triggering ferroptosis. HIF-1/2α-IN-2 is widely used in research related to tumor biology, metabolic regulation, and ischemia.

HIF-2α-IN-3 is a HIF-2α alteration inhibitor with anti-tumor properties and may be used in the study of cardiovascular disease.

HIF-2α-IN-1 is a potent inhibitor of HIF-2α, with IC50 values below 500 nM.

HIF-2α agonist 3 (Compound 14d) is an orally active HIF-2α agonist with an EC50 value of 1.78 μM and is applicable in research on renal anemia.

PROTACHIF-1αdegrader-2 is a highly efficient and selective PROTAC degrader targeting HIF-1α. It facilitates the degradation of HIF-1α via the ubiquitin-proteasome pathway by promoting the formation of the HIF-1α/VHL ternary complex. This compound inhibits the proliferation, migration, and colony formation of HeLa cells while inducing apoptosis (apoptosis). Additionally, PROTACHIF-1αdegrader-2 reduces the expression of p-MEK and p-AKT in the MAPK and PI3K/AKT pathways. It is useful for cervical cancer research.

HIF-1α-IN-2 is a novel and highly potent HIF-1α inhibitor with anticancer and antitumor activity that inhibits the expression of HIF-1α and VEGF in a dose-dependent manner and inhibits cell migration.

HIF-2α-IN-6 (117) is a HIF-2α inhibitor [1].

HIF-1/2α-IN-1, an orally active compound, functions as an inhibitor of HIF-2α. Its inhibitory effect on HIF-2α activity is significant, with an IC 50 value of 0.92 μM. Furthermore, HIF-1/2α-IN-1 has the ability to decrease HIF-1α levels. This compound is particularly valuable for research on clear cell renal cell carcinoma (ccRCC) [1].

HIF-PHD-IN-2 (compound 25) is a highly effective PHD inhibitor with IC50 values below 100 nM for PHD1, PHD2, and PHD3 [1].

HIF-2α-IN-5 is a potent HIF-2α inhibitor with an IC50 of less than 50 nM [1].

HIF-2α-IN-7 is a hypoxia inducible factor 2α (HIF-2α) inhibitor. HIF-2α-IN-7 can inhibit HIF-2α with an EC 50 value of 6 nM. HIF-2α-IN-7 can be used for the research of various types of diseases including cancer , liver disease, inflammatory disease, pulmonary diseases and iron load disorders .

HIF-1α-IN-2 hydrochloride is a potent HIF-1α inhibitor exhibiting anticancer activity, with IC50 values of 28 nM in MDA-MB-231 cells and 15 nM in MiaPaCa-2 cells, effectively suppressing HIF-1α expression by inhibiting transcription and protein translation [1].

HIF-2α-IN-9 (compound 35r) is an HIF-2α inhibitor that effectively suppresses VEGF-A with an IC50 of 305 nM, modulates growth-promoting genes within tumor cells, and reactivates macrophage-mediated tumor immunity [1].

HIF-2α-IN-13 (18) acts as a HIF-2α inhibitor and exhibits an IC 50 value of 2.7 μM.

HIF-2α-IN-14 (18) acts as a HIF-2α inhibitor, exhibiting an IC 50 value of 0.27 μM.

HIF-2α-IN-15 (35) acts as a HIF-2α inhibitor and exhibits an inhibitory concentration (IC 50) of 0.41 μM.

HIF-2α-IN-10 (17) acts as a potent HIF-2α inhibitor, exhibiting an IC 50 value of 0.05 μM.

HIF-2α-IN-11 (1) serves as a potent inhibitor of HIF-2α, exhibiting an IC 50 value of 59.2 nM.

HIF-2α-IN-12 (9) acts as an inhibitor of HIF-2α, exhibiting an IC 50 value of 0.9 μM.

HIF-2α-IN-16 (48) acts as a HIF-2α inhibitor and demonstrates an IC 50 value of 0.091 μM.

PT2399 is a potent, selective, orally available HIF-2α antagonist that directly binds to the PAS B domain of HIF-2α (IC₅₀ = 6 nM). PT2399 exhibits antitumor activity. PT2399 specifically blocks the heterodimerization of HIF-2α and HIF-1β, thereby inhibiting the expression of downstream target genes such as VEGF and GLUT1, and exerts its antitumor effects.