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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