Cytochrome P450 Inhibitor
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Karanjin
0 ImagesKaranjin is an orally active furanoflavonoid which can be isolated from several Leguminosae. Karanjin exhibits evident anti-diabetic, anti-cancer, anti-inflammatory, antioxidant, anticolitis, anti-ulcer, anti-Alzheimer properties and multiple insect repellent/insecticidal, acaricide properties, suggesting the potential of Karanjin to be applied to relevant research.
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Levoketoconazole
0 ImagesSynonyms: (-)-Ketoconazole; (-)-Ketoconazol; (-)-R 41400Levoketoconazole ((-)-Ketoconazole) is the 2S,4R enantiomer derived from racemic Ketoconazole (HY-B0105). Levoketoconazole is a potent and orally active cortisol synthesis inhibitor. Levoketoconazole inhibits key steps in cortisol and testosterone synthesis by inhibiting CYP11B1, CYP11A1, and CYP17A1. Levoketoconazole can be used for research on endogenous Cushing’s syndrome.
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Rhapontigenin
0 ImagesRhapontigenin is a natural analog of resveratrol with anticancer, antioxidant, antifungal and antibacterial activities. Rhapontigenin is amechanism-based, potent and selective cytochrome P450 1A1 inactivator (IC50 = 400 nM). Rhapontigenin exhibits 400-fold and 23-fold selectivity for P450 1A1 over P450 1A2 and P450 1B1, respectively.
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BVT948
0 ImagesBVT948 is a protein tyrosine phosphatase (PTP) inhibitor which can also inhibit several cytochrome P450 (P450) isoforms and lysine methyltransferase SETD8 (KMT5A).
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Clomethiazole
0 ImagesChlormethiazole is an potent and orally active GABAA agonist. Chlormethiazole inhibits cytochrome P450 isoforms: CYP2A6 and CYP2E1 in human liver microsomes. Chlormethiazole is an anticonvulsant agent and has the potential for treating convulsive status epilepticus.
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Cedrol
0 ImagesCedrol is a potent competitive inhibitor of cytochrome P-450(CYP) enzyme. Cedrol plays an anticancer role by inducing cell cycle arrest and Caspase-dependent apoptosis. Cedrol acts as a neutrophil agonist that can desensitize cells to subsequent stimulation of N-formyl peptides. Cedrol prevents neuropathic pain caused by chronic contractile injury by inhibiting oxidative stress and inflammation. In addition, Cedrol has antibacterial, hair loss prevention and anti-anxiety properties.
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ADL-5859 hydrochloride
0 ImagesADL-5859 hydrochloride (compound 20) is a selective and orally active δ opioid receptor (DOR) agonist with an Ki and an EC50 value of 0.84 and 20 nM, respectively. ADL-5859 hydrochloride also shows inhibitory activity to hERG channel with an IC50 value of 78 μM. ADL-5859 hydrochloride can be used for the research of pain.
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Cecropin B
0 ImagesCecropin B has high level of antimicrobial activity and is considered as a valuable peptide antibiotic.
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Atazanavir sulfate
0 ImagesSynonyms: BMS-232632 sulfateAtazanavir (BMS-232632) sulfate is a highly selective and orally active HIV-1 protease inhibitor with blood-brain barrier permeability. Atazanavir sulfate is a substrate and inhibitor of CYP3A4, and an inhibitor of P-glycoprotein (P-gp). Atazanavir sulfate is also a SARS-CoV 3CLpro inhibitor with an IC50 of 3.49 μM. Atazanavir sulfate inhibits cardiac fibrosis, hyperlipidemia and induces malignant glioma death.
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Econazole
0 ImagesSynonyms: (±)-EconazolEconazole ((±)-Econazol) is an orally active imidazole antifungal agent, as well as a cytochrome P-450 inhibitor and a blocker of calcium and manganese ion uptake. Econazole is active against a variety of fungi and some Gram-positive bacteria, but has no significant activity against Gram-negative bacteria. Econazole can inhibit the synthesis of prostaglandins and can also induce liver damage.
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(R)-4-Benzyl-2-oxazolidinone
0 Images(R)-4-Benzyl-2-oxazolidinone is an oxazolidinone-type auxiliary that enables highly stereoselective asymmetric alkylation reactions. (R)-4-Benzyl-2-oxazolidinone is applied in the total synthesis of natural products and pharmaceutical preparations. Especially in pharmaceutical research and development, (R)-4-Benzyl-2-oxazolidinone not only serves as a key precursor for the synthesis of aromatase inhibitors, but also can be used in studies related to estrogen-dependent breast cancer.
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Galeterone
0 ImagesSynonyms: TOK-001; VN-124-1Galeterone (TOK-001) 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 also functions as a CYP17 inhibitor (IC50 = 47 nM). Galeterone induces cell apoptosis. Galeterone inhibits tumor growth in human prostate cancer xenograft mouse models. Galeterone can be used for castration resistant prostate cancer (CRPC) and pancreatic ductal adenocarcinoma (PDAC) research[1][2].
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Fadrozole hydrochloride
0 ImagesSynonyms: CGS 16949A; (Rac)-FAD286 hydrochlorideFadrozole hydrochloride (CGS 16949A) is a potent, selective and nonsteroidal inhibitor of aromatase with an IC50 of 6.4 nM.
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Piperonylic acid
0 ImagesPiperonylic acid is a natural molecule bearing a methylenedioxy function that closely mimics the structure of trans-cinnamic acid. Piperonylic Acid is a selective, mechanism-based inactivator of the trans-cinnamate 4-Hydroxylase. Piperonylic acid has anticancer, antioxidant and antibacterial activities.
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Feruloylputrescine
0 ImagesFeruloylputrescine is an oral active phenolamide found in citrus plants and formed through the decarboxylation of L-Arginine. Feruloylputrescine inhibits monooxygenase (cntA) and reductase (cntB) and trimethylamine production. Feruloylputrescine can be used for cardiovascular diseases research.
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MS-PPOH
0 ImagesMS-PPOH is a potent and selective cytochrome P450 (CYP) epoxygenase inhibitor. MS-PPOH inhibits CYP2C8 and CYP2C9 with IC50s of 15 and 11 μM, respectively. MS-PPOH is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
