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HIF Hypoxia-inducible factors

Inhibitors

Cat.No.  Name Information
M1992 2-Methoxyestradiol 2-methoxyestradiol (2-ME2), an endogenous metabolite of 17β -estradiol (E2) with oral activity, is an apoptosis inducer and angiogenesis inhibitor with effective antitumor activity. Methoxyestradiol can also destabilize microtubules. Methoxyestradiol is a potent inhibitor of superoxide dismutase (SOD) and reactive oxygen species (ROS) that can induce autophagy in transformed cell line HEK293, cancer cell line U87 and HeLa.
M9066 PT2385 PT2385 is an orally active, selective inhibitor of hypoxia inducible factor (HIF)-2alpha, with a Ki value of less than 50 nM.
M11025 M1001 M1001 is a weaker HIF-2α agonist that binds directly to the HIF-2α PAS-B domain.Kd The value is 667 nM. The M1001 enhances stability between HIF-2α-ARNT complexes.
M11006 IOX4 IOX4 is a selective PHD2 inhibitor,IC50 With a value of 1.6 nM, HIFα expression is induced in cells and wild-type mice to permeate the blood-brain barrier. IOX4 competes with and displaces 2-oxoglutaric acid (2OG) at the PHD2 active site.
M10501 PT2399 PT2399 is a potent and orally available antagonist of HIF-2 with an IC50 of 6 nM, PT2399 selectively disrupts the heterodimerization of HIF-2α with HIF-1β.
M10436 Belzutifan (PT2977) Belzutifan (PT2977) is a second-generation orally active and selective HIF-2α inhibitor with an IC50 of 9 nM.
M10169 Vadadustat Vadadustat is a novel, oral hypoxia-inducible factor prolyl hydroxylase (HIF-PH) inhibitor.
M9842 ML228 ML228 is a potent the HIF pathway activator, with EC50 values of 1.23 and 1.4 μM for HRE gene reporter assay and HIF-1α nuclear translocation assay respectively.
M9675 Desidustat Desidustat is an inhibitor of HIF hydroxylase.
M9279 LW6 LW6 is a novel HIF-1alpha inhibitor, with an IC50 of 4.4 μM.
M9198 JTZ-951 Enarodustat (JTZ-951) is a potent and orally active factor prolyl hydroxylase inhibitor, with an EC50 of 0.22 μM.
M9066 PT2385 PT2385 is an orally active, selective inhibitor of hypoxia inducible factor (HIF)-2alpha, with a Ki value of less than 50 nM.
M8963 JNJ-42041935 JNJ-42041935 is a potent, competitive, reversible, and selective inhibitor of PHD with pKi values of 7.91±0.04, 7.29 ±0.05, and 7.65±0.09 for PHD1, PHD2, and PHD3, respectively.
M8924 Daprodustat Daprodustat (GSK1278863) is a novel, orally active inhibitor of hypoxia-induced factor prolyl hydroxylase (HIF-PHI). Reversible inhibition of HIF-PHD activity under normal partial oxygen pressure can temporarily inhibit HIF-α degradation and promote the expression of related hypoxia metabolism genes.
M8678 FG-2216 (BIQ) BIQ (FG-2216) is an orally available and potent inhibitor of prolyl-hydroxylase (PHD) with IC50 of 3.9 uM for PDH2 enzyme.
M7929 PX 12 PX-12 inhibits the thioredoxin redox system and HIF-1a activity.
M5834 Oltipraz Oltipraz is a potent Nrf2 activator and a potent inducer of Phase II detoxification enzymes, most notably glutathione-S-transferase (GST). Phase 3.
M5795 Molidustat (BAY 85-3934) Molidustat (BAY 85-3934) is a potent hypoxia-inducible factor prolyl hydroxylase (HIF-PH) inhibitor with IC50 of 480 nM, 280 nM, and 450 nM for PHD1, PHD2, and PHD, respectively.
M5276 MK-8617 MK-8617 is an orally active pan-inhibitor of Hypoxia-inducible factor prolyl hydroxylase 1−3 (HIF PHD1−3), inhibiting PHD1, 2, 3 with IC50s of 1.0, 1.0 and 14 nM, respectively.
M5146 PX-478 2HCl PX-478 2HCl is an orally active, and selective hypoxia-inducible factor-1α (HIF-1α) inhibitor.
M4869 BAY 87-2243 BAY87-2243 is a potent inhibitor of selective hypoxia-inducible facin-1 (HIF-1). Bay87-2243 induces iron death and necrosis in BRAFV600E melanoma cells by inhibiting the mitochondrial respiratory chain, resulting in ROS accumulation, lipid peroxidation, and GSH deletion.
M4460 Oroxylin-A Oroxylin A is an active flavonoid with strong anticancer effects.



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