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

Heme Oxygenase-2-IN-1 (Compound 9) is a potent, selective inhibitor of heme oxygenase-2 (HO-2). The IC 50 values of Heme Oxygenase-2-IN-1 for HO-1 and HO-2 are 14.9 μM and 0.9 μM, respectively [1].

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

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

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.

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).

Nrf2 activator; inhibits Nrf2/Keap1 interaction. Induces upregulation of Nrf2 pathway downstream gene expression including heme-oxygenase 1. Suppresses LPS-induced TNF-α expression in THP-1 cells.

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.

Keap1-Nrf2-IN-9 (compound 11) is a potent inhibitor of the Keap1-Nrf2 protein−protein interaction (PPI) with an IC50 value of 0.575 µM. It enhances the expression of Nrf2 target genes, including heme oxygenase 1 (Hmox1), glutathione S-transferase P (GstP), and glutamate-cysteine ligase catalytic (Gclc) and modulatory (Gclm) subunits. Notably, Keap1-Nrf2-IN-9 is not cytotoxic to ARPE19 cells [1].

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.

Aniline-d5 is a deuterated compound of Aniline. Aniline has a CAS number of 62-53-3. Aniline has been reported to be toxic to the spleen via iron overload and induction of oxidative stress via Heme Oxygenase 1 up-regulation. Toxicity of this agent on the spleen is characterized by hyperplasia, fibrosis, and vascular congestion in rats. Studies suggest that this compound causes significant increase in both p-IKKα and p-IKKβ which in-turn increases NF-κB and AP-1 binding activity. In other experiments, Aniline displays a capacity to induce methemoglobinemia, glutathione depletion, membrane cytoskeletal changes, loss of circulating blood cells, and adversely affects blood stability.

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.

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.

Flavoglaucin exhibits significant inhibitory effects on PTP1B, the IC50 value of 13.4, micrometer; it also shows good binding affinity for human opioid or cannabinoid receptors. Flavoglaucin appears to be an antitumor promoter, it also has anti-inflammato

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.

Delmitide acetate (RDP58) is an orally active d-isomer decapeptide that exhibits potent anti-inflammatory properties. This compound suppresses the production of TNF-α, IFN-γ, and interleukin (IL)-12, while enhancing the activity of heme oxygenase 1. It is utilized in research related to ulcerative colitis [1] [2].

YS-49 (monohydrate) is an isoquinoline compound alkaloid that functions as a PI3K/Akt activator, specifically targeting a downstream effect of RhoA, to mitigate the activation of RhoA/PTEN in 3-methylcholanthrene-treated cells. It also prevents the angiotensin II (Ang II)-induced proliferation of vascular smooth muscle cells (VSMCs) by promoting the expression of heme oxygenase (HO)-1. Additionally, YS-49 exerts a significant positive inotropic effect by stimulating cardiac β-adrenoceptors, showcasing its multifaceted pharmacological activities [1] [2] [3].

TAT 14 acetate, a 14-mer peptide, is an Nrf2 activator with anti-inflammatory properties. TAT 14 acetate increases Nrf2 protein levels due to targeting the Nrf2 binding site on Keap1, but has no effect on Nrf2 mRNA expression.