oxygenase-1

Heme Oxygenase-1-IN-1 (HO-1-IN-1) is a heme oxygenase 1 (HO-1) inhibitor (IC50: 250 nM).

HO-1-IN-1 hydrochloride is a heme oxygenase 1 (HO-1) inhibitor (IC50: 250 nM).

Zinc Protoporphyrin (Zn(II)-protoporphyrin IX) is an orally active, competitive inhibitor of heme oxygenase-1 (HO-1) that markedly attenuates the protective effects of Phloroglucinol (PG) against H2O2 and exhibits anti-cancer activity.

Heme Oxygenase-1-IN-2, a novel inhibitor of heme oxygenase-1 (HO-1), demonstrates potent antiproliferative activity in vitro with an IC50 value of 0.95 μM.

Heme Oxygenase-1-IN-3 (compound 4) serves as a potent and selective inhibitor of heme oxygenase-1 (HO-1) with a dissociation constant (Kd) of 141 nM, making it suitable for use in cancer and neurodegenerative disease research.

Heme Oxygenase-2-IN-1 (Compound 9) is a potent, selective inhibitor of heme oxygenase-2 (HO-2), with IC50 values of 14.9 μM for HO-1 and 0.9 μM for HO-2 [1].

Ketoprofen (RP-19583) is a propionic acid derivative and nonsteroidal anti-inflammatory drug (NSAID) with anti-inflammatory, analgesic, and antipyretic effects. It inhibits cyclo-oxygenase I and II, decreasing the formation of prostaglandin and thromboxane precursors. This reduction in prostaglandin synthesis, mediated by prostaglandin synthase, is responsible for its therapeutic effects. Additionally, Ketoprofen decreases thromboxane A2 formation via thromboxane synthase, inhibiting platelet aggregation.

Ibuprofen (Advil) is a propionic acid derivate and nonsteroidal anti-inflammatory drug (NSAID) with anti-inflammatory, analgesic, and antipyretic effects. Ibuprofen inhibits the activity of cyclo-oxygenase I and II, resulting in a decreased formation of precursors of prostaglandins and thromboxanes.

Sofalcone (SU-88), a gastric antiulcer agent in clinical use, is known to induce the expression of Heme oxygenase-1 (HO-1) in gastric epithelium.

Hemin (Hemin chloride) is a chlorinated iron-containing porphyrin, a heme oxygenase (HO)-1 inducer. Hemin has therapeutic activity in porphyrias by reducing heme deficiency in patients, thereby inhibiting δ-aminolevulinic acid synthetase activity through biochemical feedback.

Caffeic Acid Phenethyl Ester (Phenylethyl Caffeate) (CAPE) inhibits the activation of nuclear transcription factor NF-kappa B and may suppress p70S6K and Akt-driven signaling pathways, with antineoplastic, cytoprotective and immunomodulating activities. CAPE is the phenethyl alcohol ester of caffeic acid and a bioactive component of honeybee hive propolis. In addition, CAPE inhibits PDGF-induced proliferation of vascular smooth muscle cells through the activation of p38 mitogen-activated protein kinase (MAPK) and hypoxia-inducible factor (HIF)-1alpha and subsequent induction of heme oxygenase-1 (HO-1).

Aniline-d5 is a deuterated isotope marker of Aniline, which can be used for isotope tracing.Aniline induces toxicity to the spleen through iron overload and oxidative stress via heme oxygenase 1 up-regulation and is able to lead to a significant increase in p-IKKα and p-IKKβ, which in turn increases NF-κB and AP-1 binding activity.

OB 24 hydrochloride is a potent and selective heme oxygenase 1 (HO-1) inhibitor (IC50 values are 1.9 and >100 μM for HO-1 and HO-2 respectively), reduces protein carbonylation and reactive oxygen species formation in advanced prostate cancer cells (PCA). Inhibits cell proliferationin vitroand PCA tumor growth and lymph node/lung metastasesin vivo. Synergizes with Taxol.

Tin-protoporphyrin IX dichloride (SnPPIX dichloride) is an HO-1) inhibitor with antiviral activity that inhibits dengue and yellow fever viruses.

CP-312 (Cardioprotectant 312) is an antioxidant defense response activator that protects hiPSC-CM viability by acting through induction of heme oxygenase-1 and targeting the antioxidant response network by inducing HMOX1 expression.CP-312 protects human iPSC-derived cardiomyocytes from oxidative stress.

Bardoxolone (CDDO) is a synthetic oleanane triterpenoid that blocks the cellular synthesis of inducible nitric oxide synthase and inducible COX-2 in INF-γ-activated mouse macrophages with an IC50 value of 0.4 nM. By suppressing reactive oxygen and nitrogen species (ROS RNS) formation, it promotes the cellular control of ROS RNS levels that would lead to DNA damage associated with tumorigenesis. In various Y cell lines, Bardoxolone has been shown to specifically inhibit proliferation and induce apoptosis. Mechanism studies revealed that Bardoxolone is a ligand for peroxisome proliferator-activated receptor γ, and also that it induces genes regulated by Nrf2, including heme oxygenase-1 and eotaxin-1, which play a role in antioxidant response element signaling activity.

Carnosol is an Nrf2 activator, increasing Nrf2 levels and promoting heme oxygenase 1 (HMOX1) expression. It is a ribosomal S6 kinase (RSK2) inhibitor and can be used in gastric cancer-related research with an IC50 value of approximately 5.5 μM.

VK3-OCH3 (2-[(2-Methoxy)ethylthio]-3-methyl-1,4-na) is a selective antitumor agent via heme oxygenase (HO-1) related mechanisms; Vitamine K3 analogue.

HIF-PHD-IN-3 is a potent hiPSC-CM cardioprotective scaffold with potential inhibitory effects on HIF-PHD, regulates heme oxygenase-1, and can be used to study anaemia.

S-(+)-Ketoprofen ((S)-(+)-Ketoprofen) works by blocking the action of a substance in the body called cyclo-oxygenase. It belongs to a class of medicines called non-steroidal anti-inflammatory drugs (NSAIDs). Cyclo-oxygenase is involved in the production of chemicals in the body called prostaglandins. Prostaglandins are produced in response to injury or certain diseases and would otherwise go on to cause swelling, inflammation and pain. By blocking cyclo-oxygenase, S-(+)-Ketoprofen prevents the production of prostaglandins and therefore reduces inflammation and pain. Along with Peripheral analgesic action it possesses central analgesic action.S-(+)-Ketoprofen is a non-steroidal anti-inflammatory drug. It is manufactured by Menarini, under the tradename Keral. It is available in the UK, as S-(+)-Ketoprofen trometamol, as a prescription-only drug and in Latin America as Miracox, produced by Stein in Costa Rica. In Italy it is available as an over the counter-drug under the tradename Enantyum. In Lithuania it is available as over the counter-drug uder tradename Dolmen.

9-cis-β-Carotene, a precursor of retinal, is cleaved by beta-carotene oxygenase 1 (BCMO1) to produce 9-cis-retinal, which inhibits photoreceptor degeneration and restores retinal function in vivo.

Probucoldithiobisphenol (DTBP) is a derivative of Probucol. It stimulates the production of heme oxygenase 1 (HO-1) and exhibits antioxidant properties. In the Apoe− − mouse model, Probucol dithiobisphenol reduces aortic atherosclerotic lesions, and in a rabbit arterial injury model, it promotes arterial re-endothelialization and suppresses restenosis. This compound is orally active.

Nrf2 HO-1 Activator 3 (Compound C3a) is an activator of the Nrf2 signaling pathway that facilitates the translocation of Nrf2 into the nucleus and enhances the expression of heme oxygenase-1 (HO-1). In H9c2 cardiomyocytes subjected to H2O2 or high glucose stimulation, Nrf2 HO-1 Activator 3 inhibits the excessive expression of ROS and MDA, suppressing cell viability and colony formation, thereby exhibiting antioxidant activity.

CABP is a transition analog of ribulos-1, 5-diphosphate carboxylase/oxygenase (Rubisco).