Cytochrome P450 Inhibitor

Urotensin-II receptor antagonist-1 (compound 1) is a low oral bioavailability (F=0-3%, rat) selective human Urotensin II receptor antagonist, K_i=16 nM (test on HEK293 cells expressing recombinant human UT receptor). Urotensin-II receptor antagonist-1 inhibits cytochrome P450 (IC₅₀=0.75 μM, CYP2D6; 1.4 μM, CYP3A4), inhibits κ-opioid receptor (EC₅₀=3.2 μM), targets cardiac sodium channels (K_i=2.5 μM).

Vildagliptin carboxylic acid metabolite (M20.7) TFA is a potent P450 enzyme activity inhibitor.

ASN-001 is an orally active CYP-17A1 lyase inhibitor that selectively inhibits testosterone synthesis. ASN-001 has anticancer activity and can be used for research in the field of prostate cancer.

Aromatase-IN-5 (Compound 10) is a potent inhibitor of aromatase with an IC₅₀ value of 0.06 μM. Aromatase-IN-5 effectively blocks estrogen production. Aromatase-IN-5 inhibits the proliferation of breast cancer cell lines like MCF-7, arrests the cell cycle at the G1 phase, and induces apoptosis. Aromatase-IN-5 is promising for research of breast cancer.

CYP51-IN-26 is a CYP51 inhibitor with an IC₅₀ value of approximately 0.40 μM. CYP51-IN-26 eradicates C. auris biofilms. CYP51-IN-26 demonstrates significantly improved intracellular uptake in an accumulation assay. CYP51-IN-26 protects against C. auris infection in both G. mellonella and D. melanogaster models. CYP51-IN-26 can be used for research on fungal infections.

CYP51-IN-17 (compound 7a) is a potent CYP51 inhibitor with an IC₅₀ of 0.377 μg/mL. CYP51-IN-17 shows significant fungicidal activity against B. cinerea with an EC₅₀ of 0.326 μg/mL.

AR-C141990 (Compound 30) is a potent blocker of the monocarboxylate transporter MCT1 with a K_i of 4.8 nM. AR-C141990 (Compound 30) inhibits CYP3A4 and CYP2C9 with IC₅₀ values of 16 μM.

(Rac)-Tamsulosin (YM12617 (free base); (Rac)-LY253351 (free base)) is an isomer of Tamsulosin (HY-B0661). (Rac)-Tamsulosin is a sulfonamide phenethylamine derivative and a competitive antagonist of selective post-synaptic α₁-adrenoceptors. (Rac)-Tamsulosin inhibits CYP3A4 activity in a non-competitive, enantiomer-specific manner, with an IC₅₀ and K_i of 6.75 μM. (Rac)-Tamsulosin produces dose-dependent hypotension, preferentially antagonizing α₁-adrenoceptor-mediated pressor responses, and inhibits α₂-adrenoceptor-mediated pressor responses at high doses. (Rac)-Tamsulosin can be used in research related to various diseases such as metabolism.

COX-2/Aromatase-IN-1 is a potent dual inhibitor of COX-2 and aromatase. COX-2/Aromatase-IN-1 can simultaneously inhibit COX-2 and aromatase, significantly suppress inflammation and induce proliferation inhibition of breast cancer cells. COX-2/Aromatase-IN-1 exerts anti-breast cancer and anti-inflammatory effects in the MCF-7 breast cancer cell and carrageenan-induced rat paw edema model. COX-2/Aromatase-IN-1 can be used for the study of inflammation and breast cancer.

Anticancer agent 78 is a potent anticancer agent. Anticancer agent 78 shows cytotoxicity. Anticancer agent 78 exhibits anti-aromatase activity with an IC₅₀ value of 0.9 µM. Anticancer agent 78 has the potential for the research of breast cancer.

Galeterone (TOK-001) hydrochloride is a potent, orally active molecular glue degrader, which degrades androgen receptor (AR) and its splice variants (AR-Vs) and MAP kinase-interacting serine/threonine protein kinase Mnk1/2. Galeterone hydrochloride also functions as a CYP17 inhibitor (IC₅₀ = 47 nM). Galeterone hydrochloride induces cell apoptosis. Galeterone hydrochloride inhibits tumor growth in human prostate cancer xenograft mouse models. Galeterone hydrochloride can be used for castration resistant prostate cancer (CRPC) and pancreatic ductal adenocarcinoma (PDAC) research^[1][2].

CYP3A4-IN-1 (compound 5a) is a potent cytochrome P450 3A4 (CYP3A4) inhibitor with an IC₅₀ value of 0.085 µM.

Phenoxan is an inhibitor of cytochrome b and NADH: ubiquinone oxidoreductase. It exerts anti-HIV, antifungal, and cytotoxic effects by inhibiting the electron transport chain, the activity of HIV-1 Reverse Transcriptase, and viral replication. Phenoxan can be used in studies of HIV-1 infection and fungal infections.

CYP51/HDAC-IN-1 is a potent, orally active CYP51/HDAC dual inhibitor. CYP51/HDAC-IN-1 inhibits important virulence factors and down-regulated resistance-associated genes. CYP51/HDAC-IN-1 exhibits potent therapeutic effects for both tropical candidiasis and cryptococcal meningitis.

Caspase-3/7 activator 4 is a caspase-3 activator and caspase-7 activator. Caspase-3/7 activator 4 inhibits key enzymes in estrogen biosynthesis, including aromatase (IC₅₀ = 38.3 nM) and steroid sulfatase (IC₅₀ = 12.7 µM), and selectively suppresses COX-2 (IC₅₀ = 5.38 µM). Caspase-3/7 activator 4 shows strong antioxidant activity (DPPH: IC₅₀ = 16.26 µM). Caspase-3/7 activator 4 inhibits estrogen synthesis, suppresses estrogen availability, reduces prostaglandin production, increases caspase-3/7 expression, induces G0/G1 cell cycle arrest, induces apoptotic cell death, reduces circulating TNF-α and VEGFR-II levels, restores hepatorenal function markers and histoarchitecture, restores antioxidant defense enzyme activity, reduces lipid peroxidation, exerts antiproliferative activity against breast cancer cells, exerts antitumor activity in the Ehrlich ascites carcinoma models. Caspase-3/7 activator 4 can be used for the research of breast cancer, ehrlich ascites carcinoma.

Cloperidone hydrochloride acts as an inhibitor and substrate of CYP2C9, with an IC₅₀ of 17.7 μM. Cloperidone hydrochloride exhibits enhanced cytotoxicity in cells expressing CYP2C9. It can be used in the research of sedative/hypnotic-related diseases.

(R)-6',7'-Dihydroxybergamottin ((R)-6′,7′-DHB) is a competitive inhibitor of human and rat CYP1A1 activity with K_is of 55 μM and 1.72 μM, respectively. (R)-6',7'-Dihydroxybergamottin has the potential for cancer research.

Schisandrin A (Standard) is the analytical standard of Schisandrin A. This product is intended for research and analytical applications. Schisandrin A inhibits CYP3A activity with an IC₅₀ of 6.60 μM and Ki of 5.83 μM, respectively.

BMS-570520 is an orally bioavailable CCR3 antagonist with an IC₅₀ of 1.9 nM against hCCR3 and an IC₅₀ of 1300 nM against hCYP2D6. BMS-570520 inhibits CYP2D6, but shows low activity against off-target G protein-coupled receptors, biogenic amine transporters, and the hERG potassium channel. BMS-570520 regulates chemotaxis, calcium mobilization, and anti-inflammatory pathways. BMS-570520 can be used in research related to asthma, allergic rhinitis, and contact dermatitis.

GSK3β-IN-3 is an ATP-competitive GSK-3β inhibitor (IC₅₀ = 0.90 μM). GSK3β-IN-3 can reduce the phosphorylation level of tau protein in the BR5706 strain and reduce the deposition of Aβ aggregates in the CL2006 strain, and can be used to research Alzheimer's disease (AD).