heme oxygenase-1-in-2

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-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].

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.

12-Nitrolinoleate is a linoleic acid derivative that acts as an agonist of peroxisome proliferator-activated receptor γ (PPARγ). Formed via exposure to acidified nitrite, it is present in human red blood cells and plasma. This compound stimulates PPARγ-dependent gene expression, demonstrated in a reporter assay with MCF-7 cells expressing human PPARγ, with an EC50 of 0.045 µM. At 2.5 µM, 12-Nitrolinoleate reduces the secretion of IL-6, TNF-α, and chemokine (C-C motif) ligand 2 (CCL2) in THP-1 and RAW 264.7 macrophages, and it suppresses LPS-induced NF-κB transcriptional activity in RAW 264.7 macrophages. Additionally, it inhibits TNF-α-induced increases in vascular cell adhesion molecule-1 (VCAM-1) in human umbilical vein endothelial cells (HUVECs) and enhances heme oxygenase-1 (HO-1) levels in primary human aortic endothelial cells at concentrations of 1, 5, or 10 µM.

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.

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].

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

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