HIF/HIF Prolyl-Hydroxylase Hypoxia-inducible factors;HIFs;HIF-PH HIFs (Hypoxia-inducible factors) are transcription factors that respond to changes in available oxygen in the cellular environment, to be specific, to decreases in oxygen, or hypoxia. The HIF signaling cascade mediates the effects of hypoxia, the state of low oxygen concentration, on the cell. Hypoxia often keeps cells from differentiating. However, hypoxia promotes the formation of blood vessels, and is important for the formation of a vascular system in embryos, and cancer tumors. The hypoxia in wounds also promotes the migration of keratinocytes and the restoration of the epithelium. In general, HIFs are vital to development. In mammals, deletion of the HIF-1 genes results in perinatal death. HIF-1 has been shown to be vital to chondrocyte survival, allowing the cells to adapt to low-oxygen conditions within the growth plates of bones. HIF plays a central role in the regulation of human metabolism. Recently, several drugs that act as selective HIF prolyl-hydroxylase inhibitors have been developed. www.MedChemExpress.com 1 HIF/HIF Prolyl-Hydroxylase Inhibitors & Modulators Acriflavine AFP464 Cat. No.: HY-100575 Cat. No.: HY-16031 Bioactivity: Acriflavine is a fluorescent dye for labeling high molecular Bioactivity: AFP464, is an active HIF-1α inhibitor with an IC50 of 0.25 μM, weight RNA. It is also a topical antiseptic. also is a potent aryl hydrocarbon receptor (AhR) activator. Purity: 98.62% Purity: >98% Clinical Data: Launched Clinical Data: No Development Reported Size: 100 mg Size: 250 mg, 500 mg AKBA BAY 87-2243 (Acetyl-11-keto-β-boswellic acid) Cat. No.: HY-N0892 Cat. No.: HY-15836 Bioactivity: Acetyl-11-Keto-β-Boswellic Acid (AKBA) is an active Bioactivity: BAY 87-2243 is a highly potent and selective hypoxia-inducible triterpenoid compound from the extract of Boswellia serrate; a factor-1 ( HIF-1) inhibitor. novel Nrf2 activator. IC50 value: Target: Nrf2 activator in vitro: AKBA significantly reduced infarct volumes and apoptotic cells, and also increased neurologic scores by… Purity: 99.71% Purity: 99.41% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 5 mg, 10 mg 5 mg, 10 mg, 50 mg, 100 mg Chlorogenic acid Daprodustat (3-O-Caffeoylquinic acid; Heriguard; NSC-407296) Cat. No.: HY-N0055 (GSK1278863) Cat. No.: HY-17608 Bioactivity: Chlorogenic acid is a major phenolic compound in coffee and Bioactivity: Daprodustat (GSK1278863) is an orally active hypoxia-inducible tea. It plays several important and therapeutic roles such as factor prolyl hydroxylase inhibitor being developed for the antioxidant activity, antibacterial, hepatoprotective, treatment of anemia associated with chronic kidney disease. cardioprotective, anti-inflammatory, antipyretic, neuroprotective, anti-obesity, antiviral, anti-microbial,… Purity: 99.29% Purity: 99.39% Clinical Data: Phase 3 Clinical Data: Phase 3 Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 500 mg 5 mg, 10 mg, 50 mg, 100 mg Dencichin Desidustat (Dencichine; L-Dencichin; ODAP) Cat. No.: HY-N1477 Cat. No.: HY-103227 Bioactivity: Dencichin is a non-protein amino acid originally extracted Bioactivity: Desidustat is an inhibitor of HIF hydroxylase extracted from from Panax notoginseng, and can inhibit HIF-prolyl hydroxylase-2 patent WO 2014102818 A1, compound example 2. (PHD-2) activity. Purity: >98% Purity: 98.0% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 5 mg, 10 mg, 25 mg Size: 10mM x 1mL in DMSO, 1 mg, 5 mg, 10 mg, 50 mg, 100 mg DMOG EL-102 (Dimethyloxallyl Glycine) Cat. No.: HY-15893 Cat. No.: HY-16187 Bioactivity: DMOG (Dimethyloxallyl Glycine) is a cell-permeable and Bioactivity: EL102 is a inhibitor of HIF1α , Which can inhibit tubulin competitive inhibitor of HIF-1α prolyl hydroxylase (HIF-PH). polymerisation and decreased microtubule stability. Purity: 99.15% Purity: 99.07% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 50 mg, 100 mg, 200 mg, 500 mg 1 mg, 5 mg, 10 mg, 50 mg, 100 mg 2 Tel: 609-228-6898 Fax: 609-228-5909 Email: [email protected] Enarodustat ENMD-119 (JTZ-951) Cat. No.: HY-109057 (ENMD 1198; IRC 110160) Cat. No.: HY-16196 Bioactivity: Enarodustat is a potent and orally active factor prolyl Bioactivity: ENMD-119 is a 2-methoxyestradiol analogue with antiproliferative and antiangiogenic activity, and is suitable hydroxylase inhibitor, with an EC50 of 0.22 μM; Enarodustat has entered clinical trial for renal anemia. for inhibiting HIF-1α and STAT3 in human HCC cells. Purity: >98% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 250 mg, 500 mg Size: 1 mg, 5 mg, 10 mg, 20 mg FG-2216 Glucosamine hydrochloride (D-(+)-Glucosamine hydrochloride; (YM-311) Cat. No.: HY-15641 Chitosamine hydrochloride) Cat. No.: HY-N0733 Bioactivity: FG-2216 is a potent HIF-prolyl hydroxylase inhibitor with IC50 Bioactivity: Glucosamine (hydrochloride) is a natural product. IC50 value: of 3.9 uM for PDH2 enzyme; orally bioavailable and induced Target: In vitro: Glucosamine hydrochloride exhibited significant and reversible Epo induction in vivo. dose-dependent DPPH antioxidant activity [1]. Short-term (4 h) glucosamine hydrochloride treatment inhibited HIF-1α at the protein level, decreased phosphorylation of p70S6K and S6,… Purity: 99.31% Purity: 98.0% Clinical Data: No Development Reported Clinical Data: Launched Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in Water, 5 mg, 10 mg, 25 mg, 50 mg, 100 mg 50 mg GN44028 HIF-2α-IN-1 Cat. No.: HY-110266 Cat. No.: HY-19949 Bioactivity: GN44028 is a hypoxia inducible factor (HIF)-1 inhibitor, with an Bioactivity: HIF-2α-IN-1 is a HIF-2α inhibitor has an IC50 of less than 500 nM in HIF-2α scintillation proximity assay. IC50 of 14 nM. GN44028 inhibits hypoxia-induced HIF-1α transcriptional activity without suppressing HIF-1α mRNA expression, HIF-1α protein accumulation, or HIF-1α/HIF… Purity: 99.0% Purity: 99.45% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 5 mg 5 mg, 10 mg, 25 mg Hydralazine hydrochloride IDF-11774 Cat. No.: HY-B0464 Cat. No.: HY-111387 Bioactivity: Hydralazine Hydrochloride is a direct-acting vasodilator that Bioactivity: IDF-11774 is a novel hypoxia-inducible factor ( HIF) -1 is used as an antihypertensive agent. inhibitor with an IC50 of 3.65μM. IDF-11774 has been approved as a clinical candidate for a phase I study. Purity: 98.0% Purity: 98.04% Clinical Data: Launched Clinical Data: No Development Reported Size: 10mM x 1mL in Water, Size: 10mM x 1mL in DMSO, 100 mg, 500 mg 1 mg, 5 mg, 10 mg, 50 mg IOX2 JNJ-42041935 Cat. No.: HY-15468 Cat. No.: HY-12832 Bioactivity: IOX2 is a specific prolyl hydroxylase-2 ( PHD2) inhibitor Bioactivity: JNJ-42041935 is a potent, competitive and selective inhibitor with IC50 of 22 nM. of prolyl hydroxylase PHD; inhibits PHD1, PHD2, and PHD3 with pKi values of 7.91±0.04, 7.29 ±0.05, and 7.65±0.09, respectively. Purity: 98.41% Purity: 99.79% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 50 mg 5 mg, 10 mg www.MedChemExpress.com 3 KC7F2 LW6 Cat. No.: HY-18777 (HIF-1α inhibitor; LW8) Cat. No.: HY-13671 Bioactivity: KC7F2 is a potent HIF-1 pathway inhibitor and that its Bioactivity: LW6 is a novel HIF-1 inhibitor with an IC50 of 4.4 μM. potential as a cancer therapy agent warrants further study. Purity: 99.61% Purity: 98.0% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 50 mg, 100 mg 5 mg, 10 mg, 25 mg, 50 mg, 100 mg M1001 MK-8617 Cat. No.: HY-111547 Cat. No.: HY-101023 Bioactivity: M1001 is a weak agonist of HIF-2α, directly binds to the HIF-2α Bioactivity: MK-8617 is an orally active pan-inhibitor of hypoxia-inducible factor prolyl hydroxylase 1-3 ( HIF PHD1-3) with an IC of 1 PAS-B domain, with a Kd of 667 nM. M1001 enhances the 50 stabilities of HIF-2α-ARNT complex [1]. nM for PHD2. Purity: >98% Purity: 98.0% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 500 mg, 250 mg Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 25 mg, 50 mg, 100 mg, 200 mg ML228 Molidustat (CID-46742353) Cat. No.: HY-12754 (BAY 85-3934) Cat. No.: HY-12654 Bioactivity: ML228(CID-46742353) is an activator of the Hypoxia Inducible Bioactivity: Molidustat (BAY 85-3934) is a novel inhibitor of Factor (HIF) pathway; potently activate HIF in vitro as well hypoxia-inducible factor prolyl hydroxylase ( HIF-PH) with mean as its downstream target VEGF. IC50 values of 480 nM for PHD1, 280 nM for PHD2, and 450 nM for PHD3. Purity: 98.0% Purity: 98.33% Clinical Data: No Development Reported Clinical Data: Launched Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 50 mg, 100 mg 5 mg, 10 mg, 50 mg, 100 mg Oltipraz Oroxylin A (RP 35972; NSC 347901) Cat. No.: HY-12519 (Baicalein 6-methyl ether; 6-Methoxybaicalein) Cat. No.: HY-N0560 Bioactivity: Oltipraz has an inhibitory effect on HIF-1α activation in a Bioactivity: Oroxylin A is a natural active flavonoid with strong time-dependent manner, completely abrogating HIF-1α induction anticancer effects.