HO-1 Inhibitor

Senkyunolide I is an orally active, blood-brain barrier-permeable metabolite of Z-ligustilide (HY-N0401A). Senkyunolide I is isolated from Ligusticum chuanxiong. Senkyunolide I upregulates p-Erk1/2 and Nrf2/HO-1, and inhibits Caspase 3. Senkyunolide I alleviates Apoptosis. Senkyunolide I increases the pain threshold in mice and reduces acetic acid-induced writhing responses in mice. Senkyunolide I improves neurological deficits, reduces infarct volume and alleviates cerebral edema in rats with focal cerebral ischemia-reperfusion injury. Senkyunolide I protects renal function and structural integrity in a mouse model of renal ischemia-reperfusion injury. Senkyunolide I is applicable to research related to focal cerebral ischemia-reperfusion injury, migraine, and renal ischemia-reperfusion injury.

Specneuzhenide (Nuezhenide) is an orally active phenol glycoside isolated from Ligustrum sinense. Specneuzhenide exhibits anti-inflammatory, antioxidant, antifibrotic, antitumor, hypoglycemic, as well as cartilage- and kidney-protective activities. Specneuzhenide inhibits fibrosis by activating the AMPK pathway (K_d = 62 µM), alleviates inflammation and oxidative stress by regulating multiple signaling pathways (NF-κB, Wnt/β-catenin and HO-1/Nrf-2), and upregulates podocyte proteins to comprehensively protect renal function. Specneuzhenide can be used in research related to cancer, rheumatoid arthritis, pulmonary fibrosis, diabetic nephropathy and osteoarthritis.

OB-24 is a selective small-molecule HO-1 inhibitor (IC₅₀ = 1.9 μM for HO-1 and IC₅₀ for HO-2 >100 μM). OB-24 possesses anti-tumor and anti-metastatic properties. OB-24 can be studies in research such as prostate cancer, melanoma, ovarian carcinoma and lung metastasis.

ME-344 is an Isoflavone. ME-344 increases mitochondrial ROS generation. ME-344 inhibits tubulin polymerization. ME-344 inhibits HO-1 and impacts its mitochondrial translocation. ME-344 induces Apoptosis through Caspase 3 activation. ME-344 synergizes with Vinblastine in leukemia cells. ME-344 displays anti-tumor activity against leukemia and lung tumor. ME-344 can be used in the research of lung cancer, acute myeloid leukemia, and HER2-negative breast cancer.

Quinocetone is an orally active animal feed additive used to increase the meat production of livestock and poultry. Quinocetone exhibits antibacterial activity against a variety of pathogenic microorganisms. Quinocetone exhibits tissue-specific (liver, lymphocyte) toxicity. Quinocetone induces autophagy in cells through the ATF6/DAPK1 pathway. Quinocetone activates the NF-κB and iNOS pathways, leading to cell apoptosis, hepatocyte vacuolar degeneration and fibrosis. Quinocetone can inhibit Nrf2/HO-1 and induce the generation of reactive oxygen species (ROS), leading to oxidative stress and DNA damage.

KCL-HO-1i is an orally active heme oxygenase-1 (HO-1) inhibitor (rat HO-1: IC₅₀ = 123 nM) and human HO-1: IC₅₀ = 128 nM). KCL-HO-1i targets immunosuppressive LYVE-1⁺ perivascular tumor-associated macrophages (PvTAMs) in the tumor microenvironment (TME), reduces PvTAM-mediated immune exclusion. KCL-HO-1i demonstrates synergistic anti-tumor efficacy with chemotherapy in MMTV-PyMT spontaneous breast cancer mice or C57Bl/6 mice bearing subcutaneous MN-MCA1 sarcomas. KCL-HO-1i can be used for the study of cancer.

QC-308 is a HO-1/HO-2 inhibitor, with an IC₅₀ of 0.27 μM against rat HO-1 and an IC₅₀ of 0.46 μM against rat HO-2. QC-308 inhibits the activities of rat HO-1 and HO-2 in carbon monoxide generation assays using spleen and brain microsomes, respectively. QC-308 also exhibits senolytic activity, reducing the survival rate of adipogenic progenitor cells in skeletal muscle fibers of senescent mice and human skeletal muscle myoblasts. QC-308 is applicable for senescence-related research.

QC-308 hydrochloride is a HO-1/HO-2 inhibitor, with an IC₅₀ of 0.27 μM against rat HO-1 and an IC₅₀ of 0.46 μM against rat HO-2. QC-308 hydrochloride inhibits the activities of rat HO-1 and HO-2 in carbon monoxide generation assays using spleen and brain microsomes, respectively. QC-308 hydrochloride also exhibits senolytic activity, reducing the survival rate of adipogenic progenitor cells in skeletal muscle fibers of senescent mice and human skeletal muscle myoblasts. QC-308 hydrochloride is applicable for senescence-related research.

Tricetinidin chloride is an antioxidant. Tricetinidin chloride protects rat renal cells against oxidative stress and DNA damage by reducing ROS production, increasing GSH levels, restoring mitochondrial membrane potential, and upregulating HO-1 expression. Tricetinidin chloride also inhibits the expression of IgE receptors on human mast cells. Tricetinidin chloride can be used in the research of inflammatory and allergic diseases.

Nrf-2/HMOX-1-IN-1 is a Nrf-2 and HMOX-1 inhibitor, as well as a Ferroptosis inducer. Nrf-2/HMOX-1-IN-1 inhibits GPX activity and upregulates p53 gene expression. Nrf-2/HMOX-1-IN-1 increases intracellular ROS and MDA levels, reduces GSH content, and elevates intracellular iron levels simultaneously. Nrf-2/HMOX-1-IN-1 exerts selective anticancer effects against breast cancer. Nrf-2/HMOX-1-IN-1 can be used in breast cancer-related research.