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HIF Hypoxia-inducible factors

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.
M2558 DMOG DMOG (Dimethyloxaloylglycine) is an antagonist of α-ketoglutarate cofactor and inhibitor for HIF prolyl hydroxylase.
M5834 Oltipraz Oltipraz is a potent Nrf2 activator and a potent inducer of Phase II detoxification enzymes, most notably glutathione-S-transferase (GST).
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.
M14185 Oligomycin Oligomycin, an antifungal antibiotic, is an inhibitor of H+-ATP-synthase. Oligomycin blocks oxidative phosphorylation and the electron transport chain. Oligomycin inhibits HIF-1alpha expression in hypoxic tumor cells.
M42440 PHD-IN-2 PHD-IN-2 is a PHD antagonist (IC50: < 5 nM).
M42439 PHD-IN-1 PHD-IN-1 is a potent inhibitor of PHD2, with an IC50 value of ≤5 nM.
M42438 HIF-1 inhibitor-5 HIF-1 inhibitor-5 is a potent HIF-1 inhibitor with an IC50 of 2.38 μM.
M42437 7-Hydroxyneolamellarin A 7-Hydroxyneolamellarin A is a natural product that could be derived from sponge Dendrilla nigra.
M42436 PHD2-IN-1 PHD2-IN-1 is a potent and orally active inhibitor of HIF prolyl hydroxylase 2 (PHD2) with an IC50 of 22.53 nM.
M42435 GSK360A GSK360A is a potent and orally active HIF-PHD inhibitor with IC50 values of 10, 100, and 126 nM for PHD1, PHD2, and PHD3, respectively.
M42434 HIF-1α-IN-2 hydrochloride HIF-1α-IN-2 hydrochloride is an effective HIF-1α inhibitor with anticancer potencies (IC50s of 28 nM and 15 nM in MDA-MB-231 and MiaPaCa-2 cells, respectively).
M40742 Arylsulfonamide 64B Arylsulfonamide 64B is a HIF-1α/2α inhibitor that can be used in studies related to uveal melanoma.
M40741 PT-2567 PT-2567 is a HIF-2α inhibitor that can be used in studies related to pulmonary arterial hypertension.
M40740 PMG-301 PMG-301 is a HIF-2α inhibitor that can be used in studies related to kidney tumors.
M40739 K1299 K1299 is a HIF-2α inhibitor that can be used in studies related to renal cell carcinoma.
M40738 DFF332 DFF332 is a HIF-2α inhibitor that can be used in studies related to renal cell carcinoma.
M40737 AB-521 AB-521 is a HIF-2α inhibitor that can be used in studies related to hepatocellular carcinoma and renal cell carcinoma.
M40736 NKT2152 NKT2152 is a small molecule inhibitor of HIF-2α that can be used in studies related to renal cell carcinoma.
M31057 TAT-cyclo-CLLFVY TFA  TAT-cyclo-CLLFVY TFA is a cyclic peptide inhibitor of HIF-1 heterodimerization that inhibits hypoxia signaling in cancer cells. TAT-cyclo-CLLFVY TFA disrupts HIF-1α/HIF-1β protein-protein interaction with an IC50 of 1.3 μM.
M30728 TM6089  TM6089 is a unique Prolyl Hydroxylase (PHD) inhibitor which stimulates HIF activity without iron chelation and induces angiogenesis and exerts organ protection against ischemia. Local administration of TM6089 enhances angiogenesis, and oral administration stimulates HIF activity in transgenic rats expressing a hypoxia-responsive reporter vector.
M30650 M1002  M1002 is a hypoxia-inducible factor-2 (HIF-2) agonist, and can enhance the expression of HIF-2 target genes. M1002 shows synergy with prolyl-hydroxylase domain (PHD) inhibitors.
M30225 (Rac)-Arnebin 1 (Rac)-Arnebin 1 ((Rac)-β,β-Dimethylacrylalkannin) is the racemate of β,β-Dimethylacrylalkannin and/or β,β-Dimethylacrylshikonin. β,β-Dimethylacrylalkannin and β,β-Dimethylacrylshikonin are napthoquinones isolated from Arnebia nobilis. β,β-Dimethylacrylshikonin has anti-tumor activity.
M29928 1,4-DPCA  1,4-DPCA, a potent prolyl-4-hydroxylase inhibitor, is a collagen hydroxylation inhibitor in human foreskin fibroblasts with an IC50 of 2.4 µM. 1,4-DPCA inhibits prolyl-4-hydroxylases α isoforms stabilizes HIF-1α protein. 1,4-DPCA also inhibits factor inhibiting HIF (FIH) with an IC50 of 60 μM.
M28459 TAT-cyclo-CLLFVY  TAT-cyclo-CLLFVY is a cyclic peptide inhibitor of HIF-1 heterodimerization that inhibits hypoxia signaling in cancer cells. TAT-cyclo-CLLFVY disrupts HIF-1α/HIF-1β protein-protein interaction with an IC50 of 1.3 μM.




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