About 31 results found for searched term "EN450" (0.071 seconds)
| Cat.No. | Name | Target |
|---|---|---|
| M42744 | EN450 | NF-κB |
| EN450 is a cysteine-reactive covalent molecular glue degrader targeting NF-κB. | ||
| M1669 | Regorafenib | VEGFR/PDGFR |
| BAY 73-4506 | ||
| Regorafenib (BAY 73-4506) is a novel oral multikinase inhibitor of c-KIT, VEGFR2, B-Raf with IC50s of 17, 40 and 69 nM respectively. | ||
| M2650 | Doxepin hydrochloride | Histamine Receptor |
| Doxepin hydrochloride is a potent and selective histamine receptor H1 antagonist. Doxepin hydrochloride is also a potent CYP450 inhibitor and significantly inhibits CYP450 2C19 and 1A2. | ||
| M2856 | MK-8745 | Aurora Kinase |
| MK-8745 is a potent and selective Aurora A inhibitor with IC50 of 0.6 nM, more than 450-fold selectivity for Aurora A over Aurora B. | ||
| M2929 | PF-4981517 | Cytochrome P450 (e.g. CYP17) |
| CYP3cide, PF-04981517 | ||
| PF-4981517 is a potent and selective inhibitor of CYP3A4 (P450) with IC50 of 0.03 μM, exhibits >500-fold selectivity over CYP3A5 and CYP3A7. | ||
| M2959 | Proadifen hydrochloride | Cytochrome P450 (e.g. CYP17) |
| SKF 525-A HCl | ||
| Proadifen hydrochloride is an inhibitor of the cytochrome P450 enzyme that blocks the metabolism of certain types of compounds. | ||
| M3058 | Terfenadine | Potassium Channel |
| (±)-Terfenadine; MDL-991 | ||
| Terfenadine is an antihistamine compound that is normally fully metabolized in the liver by the cytochrome P450 CYP3A4 subtype enzyme into the active form fexofenadine. | ||
| M3192 | TRAM-34 | Potassium Channel |
| Triarylmethane-34 | ||
| TRAM-34 is a selective and potent inhibitor of the intermediate-conductance Ca2+-activated K+ channel (IKCa1, KCa3.1) with Kd of 20 nM, 200- to 1500-fold selective over other ion channels, and does not block cytochrome P450. | ||
| M3341 | Selegiline hydrochloride | Monoamine Oxidase |
| Deprenyl hydrochloride | ||
| Selegiline (Deprenyl) hydrochloride is a potent, selective and irreversible inhibitor of MAO-B, with an IC50 of 51 nM. Selegiline hydrochloride exhibits 450-flod selectivity for MAO-B over MAO-A (IC50=23 μM). | ||
| M3582 | Racecadotril | Neprilysin (NEP) |
| Acetorphan | ||
| Racecadotril is a peripheral enkephalinase inhibitor with an IC50 of 4.5 μM.Racecadotril and its active metabolite, Thiorphan, inhibited the activity of purified NEP in the mouse brain with Ki's of 4500 and 6.1 nM.May be used in diarrhea related studies. | ||
| M4191 | Polygalaxanthone-III | Cytochrome P450 (e.g. CYP17) |
| Polygalaxanthone III was extracted from Polygala Tenuifolia Wild and had inhibitory effects on CYP450. Polygalaxanthone III inhibited the 6-hydroxylation of clozoxazone catalyzed by CYP2E1 with IC50 of 50.56μM. | ||
| M4414 | Gentiopicrin | Cytochrome P450 (e.g. CYP17) |
| Gentiopicroside is a natural iridoid glycoside that can inhibit the activity of P450 with IC50 and Ki values of 61 µM and 22.8 µM for CYP2A6, respectively. Gentiopicroside has anti-inflammatory and antioxidant activities. | ||
| M4532 | Rhodionin | AChR/AChE |
| Rhodionin was isolated from the roots of Rhodiola crenulata and is a specific non-competitive cytochrome P450 2D6 inhibitor with IC50 of 0.761 μM and Ki of 0.769 μM. Rhodionin effectively inhibited acetylcholinesterase (AChE) in a dose-dependent manner with an IC50 range of 57.50 to 2.43 μg/mL. Rhodionin had effective DPPH radical scavenging activity with IC50 of 19.49 μM. | ||
| M4935 | 3-Cyano-7-ethoxycoumarin | Cytochrome P450 (e.g. CYP17) |
| 3-Cyano-7-ethoxycoumarin is a fluorogenic cytochrome P-450 substrate that generates blue fluorescent product upon enzyme cleavage. | ||
| M5059 | Furafylline | Cytochrome P450 (e.g. CYP17) |
| Furafylline was a potent, non-competitive inhibitor of high affinity phenacetin O-deethylase activity of microsomal fractions of human liver, a reaction catalysed by P450IA2, with an IC50 value of 0.07 microM. | ||
| M5450 | Benzyl alcohol | Metabolite/Endogenous Metabolite |
| Benzenemethanol | ||
| Benzyl alcohol is an inhibitor of P450 enzyme. Benzyl alcohol mediated Toll-Like Receptor 4 to reduce the inflammatory response of liver injury in mice. Benzyl alcohol is used as a local anesthetic. Also, it is used in the manufacture of other benzyl compounds, as a pharmaceutic aid, and in perfumery and flavoring. | ||
| M5786 | Metyrapone | Metabolite/Endogenous Metabolite |
| Metapirone; Su-4885 | ||
| Metyrapone (Metapirone) is a potent and orally active 11β-hydroxylase inhibitor and an autophagy activator, also inhibits the production of aldosterone. Metyrapone (Metapirone) inhibits cytochrome P450-mediated ω/ω-1 hydroxylase activity and CYP11B1. | ||
| M5795 | Molidustat (BAY 85-3934) | HIF |
| BAY 85-3934 | ||
| Molidustat (BAY 85-3934) is a potent hypoxia-inducible factor prolyl hydroxylase (HIF-PH) inhibitor with IC50 of 480 nM, 280 nM, and 450 nM for PHD1, PHD2, and PHD, respectively. | ||
| M5925 | Regorafenib HCl | VEGFR/PDGFR |
| BAY73-4506 hydrochloride | ||
| Regorafenib (BAY 73-4506) is a multi-target inhibitor for VEGFR1, VEGFR2, VEGFR3, PDGFRβ, Kit, RET and Raf-1 with IC50 of 13 nM/4.2 nM/46 nM, 22 nM, 7 nM, 1.5 nM and 2.5 nM, respectively. | ||
| M6389 | 1-Aminobenzotriazole (ABT) | Cytochrome P450 (e.g. CYP17) |
| ABT; 3-Aminobenzotriazole; 1-Benzotriazolylamine; NSC 114498; NSC 656987 | ||
| 1-Aminobenzotriazole (ABT) is a cytochrome P450 inhibitor; inhibits 20-HETE synthesis. | ||
| M6723 | Fenofibrate | PPAR |
| Fenofibrate is a selective PPARα agonist with an EC50 of 30 μM. Fenofibrate inhibited cytochrome P450 subtype, with IC50 of 0.2, 0.7, 9.7, 4.8, and 142.1 μM for CYP2C19, CYP2B6, CYP2C9, CYP2C8, and CYP3A4, respectively. | ||
| M7822 | Gemfibrozil | PPAR |
| 吉非罗齐; CI-719 | ||
| Gemzil is a PPAR-α activator, which is a lipid-lowering agent. Gemfibrozil is also a nonselective inhibitor of P450, with Ki values of 5.8, 24,69 and 82 μM for CYP2C9, 2C19, 2C8 and 1A2, respectively. | ||
| M8186 | Stiripentol | Cytochrome P450 (e.g. CYP17) |
| BCX2600 | ||
| Stiripentol (BCX2600) can be used in the study of the third generation of antiepileptic drugs that enhance gaba energy neurotransmission. It's an inhibitor of cytochrome P450. | ||
| M8372 | Tienilic Acid | Others |
| Tienilic Acid (Ticrynafen) is a P450 inhibitor, a specific suicide substrate for CYP2C9 and CYP2C10. | ||
| M8694 | K-604 | Others |
| K-604 inhibits against acyl-coenzyme A (acyl-CoA):cholesterol O-acyltransferase-1 (ACAT1, SOAT1) activitiy in a selective (IC50 = 450 nM vs. | ||
| M8773 | Liarozole dihydrochloride | Others |
| Liarozole (R 75251, R75,251) is an orally active benzimidazole-based retinoic acid (RA) metabolism blocking agent (RAMBA) that targets multiple P450 enzymes, including aromatase (CYP19), 17-hydroxylase/17,20-lyas |
||
| M8796 | TCPOBOP | Others |
| TCPOBOP enhances the nuclear receptor CAR transactivation of cytochrome P450 (CYP), as dose-dependent direct agonist of CAR. | ||
| M9087 | FICZ | Aryl hydrocarbon Receptor |
| 6-Formylindolo[3,2-b]carbazole | ||
| FICZ is a potent aryl hydrogen receptor (AhR) agonist, with a Kd of 70 pM. FICZ acts by inducing transient expression of cytochrome P450-1A1 (CYP1A1) in vitro. | ||
| M9877 | Rhapontigenin | Cytochrome P450 (e.g. CYP17) |
| Protigenin | ||
| Rhapontigenin is a selective inactivator of cytochrome P450 1A1 with IC50 of 400 nM. | ||
| M9898 | TNO155 | Phosphatase |
| TNO-155；Batoprotafib | ||
| TNO155 is a first-in-class, selective, orally active wild-type SHP2 metamorphosis inhibitor with an IC50 value of 0.011 µM. tNO155 has good water solubility (0.736 mM), moderate lipophilicity (LogP=1.6), high lipophilic efficiency (>6), and no hERG inhibition (IC50 >30 μM) and no phototoxicity. Does not inhibit CYP450. | ||
| M10619 | Rhodiosin | AChR/AChE |
| Rhodiosin, isolated from the root of Rhodiola crenulata, is a specific non-competitive cytochrome P450 2D6 inhibitor with an IC50 of 0.420 μM and a Ki of 0.535 μM. Rhodiosin exhibits potent, dose-dependent inhibitory effects on acetylcholinesterase (AChE) with IC50 ranged from 57.50 to 2.43 μg/mL. | ||
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