Cytochrome P450 Inhibitor

CYP1B1-IN-3 is a potent and selective CYP1B1 inhibitor with IC₅₀ values of 6.6, 347.3, >10000 nM for CYP1B1, CYP1A1, CYP1A2, respectively. CYP1B1-IN-3 inhibits cell migration and invasion. CYP1B1-IN-3 inhibits P-gp, AKT/ERK, FAK/SRC, and EMT pathways.

Antitumor agent-87 is a potent antitumor agent. Antitumor agent-87 shows a high affinity for CYP1A1 with a K_i value of 0.23 µM. Antitumor agent-87 shows antiproliferative activity. Antitumor agent-87 induces cell cycle arrest at the G2/M phase. Antitumor agent-87 show antitumoral activity.

CYP4Z1-IN-3 is a selective CYP4Z1 inhibitor with a human IC₅₀ of 55.3 nM. CYP4Z1-IN-3 inhibits breast cancer cell migration and induces apoptosis. CYP4Z1-IN-3 can be used for the research of breast cancer.

Gamma-heptalactone (γ-Oenantholacton) is a selective cytochrome P450 2B6 (CYP2B6) inhibitor with an IC₅₀ of 2400 μM.

Bergapten-d₃ is deuterium labeled Bergapten. Bergapten is a natural anti-inflammatory and anti-tumor agent. Bergapten is inhibitory towards mouse and human CYP isoforms.

Fenofibrate (GMP) is Fenofibrate (HY-17356) produced by using GMP guidelines. GMP small molecules work appropriately as an auxiliary reagent for cell therapy manufacture. Fenofibrate is a selective PPARα agonist with an EC₅₀ of 30 μM. Fenofibrate also inhibits human cytochrome P450 isoforms, with IC₅₀s of 0.2, 0.7, 9.7, 4.8 and 142.1 μM for CYP2C19, CYP2B6, CYP2C9, CYP2C8, and CYP3A4, respectively.

R-116010 is a potent and selective retinoic acid (RA) metabolism inhibitor and can inhibit hydroxylase CYP26. R-116010 can enhance the anti-tumor effect of retinoic acid drugs. R-116010 can be used for the research of cancer, metabolic and neurological disease, such as neuroblastoma.

Proadifen-d₂ is the deuterium labeled Proadifen (HY-121789).

1,2-Dimethylnaphthalene is a CYP1A2 inhibitor with an IC₅₀ of 5.5 μM and a pIC₅₀ of 5.26.

(-)-(E) -guggulsterone (Standard) is the analytical standard for (-)-(E) -guggulsterone ((E)-Guggulsterone) (HY-N7781). (-)-(E)-Guggulsterone is an orally active natural stereoisomer of Guggulsterone (HY-107738). (-)-(E)-Guggulsterone is an antagonist for the Farnesoid X Receptor (FXR) with an IC₅₀ of 24.06 μM and possesses potent hypolipidemic properties. (-)-(E)-Guggulsterone suppresses dengue virus (DENV) replication by upregulating antiviral interferon responses by inducing HO-1 expression via Nrf2 activation. (-)-(E)-Guggulsterone exhibits antibacterial activities against Bacillus subtilis, Staphylococcus aureus and Pseudomonas aeruginosa. (-)-(E)-Guggulsterone has cardiac protective and antioxidant activities in rats.

CGP-45688 is an orally active non-steroidal aromatase inhibitor with an ED₅₀ of 30-100 μg/kg. CGP-45688 can reduce the level of estrogen in the body, thereby inhibiting the growth of estrogen-dependent tumors. CGP-45688 inhibits the growth of estrogen-dependent breast tumors in rat models. CGP-45688 disrupts the ovarian cycle and inhibits the weight of the uterus. CGP-45688 can be used for the study of breast cancer.

Conivaptan-d₄ (YM 087-d₄) is the deuterated-labeled Conivaptan (HY-18347). Conivaptan (YM 087 free base) is an orally active dual vasopressin V_1a/V₂ receptor antagonist with K_i values of 0.48 nM and 3.04 nM for vasopressin V_1a receptor and V₂ receptor, respectively. Conivaptan competitively and reversibly blocks vasopressin-mediated antidiuresis, vasoconstriction, and cellular hypertrophy, while inhibiting CYP3A4. Conivaptan inhibits vasopressin-induced intracellular calcium, cAMP, and mitogen-activated kinase activation in vascular smooth muscle cells and cardiomyocytes. Conivaptan induces water diuresis while improving hemodynamics in heart failure models, reducing left ventricular end-diastolic pressure, vascular resistance, and organ weight. Conivaptan is used for research on hyponatremia and congestive heart failure.

CYP1B1-IN-10 (Compound 15C) is a highly selective human cytochrome P450 1B1 (hCYP1B1) inhibitor (IC₅₀=0.11 μM). CYP1B1-IN-10 is promising for research of hormone-dependent tumors (e.g., breast and ovarian cancers).

K777 tosylate is a potent, orally active and irreversible cysteine protease inhibitor. K777 tosylate is also a potent CYP3A4 inhibitor with an IC₅₀ of 60 nM. K777 tosylate irreversibly inhibits Cruzain, the major cysteine protease of Trypansoma cruzi, and cathepsins B and L. K777 tosylate is a broad-spectrum antiviral by targeting cathepsin-mediated cell entry. K777 tosylate inhibits SARS-CoV and EBOV pseudovirus entry with IC₅₀ values of 0.68 nM and 0.87 nM, respectively.

DL-Acetylshikonin is a non-selective, reversible cytochrome P450 inhibitor with IC₅₀ values of 1.4-4.0 μM. DL-Acetylshikonin has anti-cancer and anti-inflammatory activities.

Debutyldronedarone-d7 (SR35021-d7) is the deuterated-labeled Debutyldronedarone (HY-12753). Debutyldronedarone (SR35021) is a Cytochrome P450 enzyme inhibitor and a Thyroid Hormone Receptor inhibitor, and it is a metabolite of Dronedarone (HY-A0016). Debutyldronedarone inhibits the binding of T3 to TRα1 and TRβ1. Debutyldronedarone reduces the incidence of reperfusion-induced ventricular fibrillation in anesthetized rats, while decreasing their heart rate and blood pressure. Debutyldronedarone can be used in studies related to ventricular fibrillation and atrial fibrillation.

Bifeprofen, a cytochrome P450 2C9 (CYP2C9) inhibitor, exhibits dose-dependent inhibition (75 μM, 50%).

BMS-344577 (Compound 22) is a potent and orally active factor Xa inhibitor (IC₅₀ = 4 nM, EC2xPT = 7 μM). BMS-344577 shows potent CYP3A4 inhibition activity (IC₅₀ = 0.3 μM). BMS-344577 can be used for the research of cardiovascular disease.

(S)-Desmethylcitalopram is the isomer of Desmethylcitalopram hydrochloride (HY-113739). Desmethylcitalopram (DCIT) hydrochloride is the active metabolite of Citalopram (HY-121203). Desmethylcitalopram has antidepressant effects. Desmethylcitalopram also inhibits cytochrome P450-2D6，-2C19 with IC₅₀s of 39.5 and 53.5 μM.

Aspergillusidone E is an aromatase inhibitor with an aromatase IC₅₀ of 1.0 μM. Aspergillusidone E exhibits cytotoxicity against cancer cells. Aspergillusidone E can be used in research related to various cancers such as breast cancer and liver cancer.