Cytochrome P450 Inducer

1,2,3,6,7,8-Hexachlorodibenzofuran (1,2,3,6,7,8-HxCDF) is a dioxin-like polychlorinated dibenzofuran (PCDF). 1,2,3,6,7,8-Hexachlorodibenzofuran induces expression of the genes encoding aryl hydrocarbon hydroxylase (AHH) and ethoxyresorufin-O-deethylase (EROD) in H-4-II-E rat hepatoma cells (EC₅₀s = 1.47 and 1.24 nM, respectively). 1,2,3,6,7,8-Hexachlorodibenzofuran reduces weight, induces thymic atrophy, and induces the expression of genes encoding the cytochrome P450 (CYP) isoform CYP1A1 and 4-chlorobiphenyl hydroxylase in rats (EC₅₀s = 3.2, 0.9, 0.35, and 0.21 µmol/kg, respectively).

2,3,4,6,7,8-Hexachlorodibenzofuran (2,3,4,6,7,8-HxCDF) is a dioxin-like polychlorinated dibenzofuran (PCDF). 2,3,4,6,7,8-Hexachlorodibenzofuran induces expression of the genes encoding aryl hydrocarbon hydroxylase (AHH) and ethoxyresorufin-O-deethylase (EROD) in H-4-II-E rat hepatoma cells (EC₅₀s = 0.687 and 0.575 nM, respectively).

Perafensine (HR 459) is an antidepressant agent. Perafensine has cytochrome P450-inducing properties.

Desmethoxyyangonin (Standard) is one of the six major kavalactones found in the Piper methysticum (kava) plant. Desmethoxyyangonin (Standard) is a selective inhibitor of monoamine oxidase-B (MAO-B) (IC₅₀: 0.123  µM). Desmethoxyyangonin (Standard) exerts anti-inflammatory effects by inhibiting Jak2/STAT3 and IKK signaling pathways. Desmethoxyyangonin (Standard) induces CYP3A23 expression and leads to skeletal muscle relaxation.

1,2,3,4,7,8,9-Heptachlorodibenzofuran (1,2,3,4,7,8,9-HpCDF) is a compound that induces the expression of CYP1A1 and CYP1B1 genes in human peripheral blood lymphocytes, while also promoting the expression of the aryl hydrocarbon receptor repressor (AhRR). 1,2,3,4,7,8,9-Heptachlorodibenzofuran can increase ethoxyresorufin-O-deethylase (EROD) activity in isolated human peripheral blood lymphocytes in a concentration-dependent manner, which serves as a marker of CYP1A1 activity. Furthermore, 1,2,3,4,7,8,9-Heptachlorodibenzofuran exhibits immunosuppressive effects by reducing the number of splenic plaque-forming cells in mice and increasing aryl hydrocarbon hydroxylase (AHH) activity in liver microsomes of mice injected with sheep red blood cells. 1,2,3,4,7,8,9-Heptachlorodibenzofuran can be used in research in the fields of immunology, metabolic diseases, and environmental toxicology.

Bifendate (DDB), extracted from Schisandrae chinensis, is an orally active anti-HBV agent against chronic hepatitis B. Bifendate inhibits ATG5-dependent autophagy and attenuates oleic acid-induced lipid accumulation with anti-oxidant properties in vitro. Bifendate can decrease alanine transaminase (ALT) level in mice. Bifendate attenuates hepatic steatosis in cholesterol/bile salt- and high-fat diet-induced hypercholesterolemia in mice. Bifendate potently increases the activity of cytochrome proteins (CYPs) and reverse P-gp-mediated multi-drug resistance (MDR).

Mosapride (citrate) (Standard) is the analytical standard of Mosapride (citrate). This product is intended for research and analytical applications. Mosapride citrate is an orally active gastroenterokinetic compound. Mosapride citrate is a 5HT4 agonist. Mosapride citrate is a CYP inducer. Mosapride citrate has a concentration-dependent inhibitory effect on Kv4.3, and its IC50 value is 15.2 μM. Mosapride citrate can be used in the study of gastrointestinal diseases.

Thaspine acetate, an alkaloid, is a topoisomerase I and II inhibitor. Thaspine acetate induces cancer cell apoptosis. Thaspine acetate induces Bak and Bax activation, mitochondrial cytochrome c release and mitochondrial membrane permeabilization. Thaspine acetate can be isoalted from the cortex of the South American tree Croton lechleri.

Myrothecine A is a trichothecene mycotoxin found in M. roridum. Myrothecine A induces apoptosis, promotes the cytochrome c release, PARP-cleavage and phosphorylation of JNK, increases Bax and cleaved caspase-3, -5, and -8 levels. Myrothecine A has anticancer activities and promotes the maturation of DC cells in the microenvironment. Myrothecine A inhibits proliferation of A549, MCF-7, HepG2, and SMMC-7721 cancer cells with IC₅₀s of 95, 70, 60, and 25 µM, respectively.

3-Bromocarbazole-d₇ is the d₇-labeled 3-Bromocarbazole (HY-33798). 3-Bromocarbazole is an inhibitor of the aryl hydrocarbon receptor (AHR). 3-Bromocarbazole induces the mRNA expression of CYP1A1 and CYP1B1, with EC₅₀ values of 2500 nM and 1100 nM, respectively. 3-Bromocarbazole inhibits motor neuron axon length by downregulating the mRNA transcription levels of α1-tubulin, Gap43, Syn2a and shha in zebrafish larvae. 3-Bromocarbazole reduces central nervous system neurogenesis by downregulating the mRNA transcription levels of elavl3, nrd, mbp and gfap in zebrafish larvae. 3-Bromocarbazole induces developmental neurotoxicity and decreases body length in zebrafish larvae or embryos; at high concentrations, it also reduces hatching rate, and increases mortality and malformation rate. 3-Bromocarbazole can be used in studies related to developmental neurotoxicity and breast cancer.

Varilutamide (ONC1-13B) is an orally active androgen receptor (AR) inhibitor. Varilutamide shows a rat AR IC₅₀ of 7.9 μM, inhibits DHT-stimulated PSA expression and prostate cancer cell proliferation, suppresses tumor growth and PSA expression and weakly induces lower CYP3A activity. Varilutamide can be used for the research of castration-resistant prostate cancer and prostate cancer.

Bulleyaconitine A (Standard) is the analytical standard of Bulleyaconitine A. This product is intended for research and analytical applications. 0

Phortress (Standard) is the analytical standard of Phortress (HY-103223). This product is intended for research and analytical applications. Phortress is a high affinity AhR ligand that elicits antitumor activity by inducing transcription of CYP1A1.