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CYP inhibition

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73

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1

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1

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10

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8

Isotope-Labeled Compounds

Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-W267897

    7-BFC

    Cytochrome P450 Others
    7-Benzyloxy-4-(trifluoromethyl)coumarin (7-BFC) is a coumarin fluorescent substrate. 7-Benzyloxy-4-(trifluoromethyl)coumarin is a substrate for cDNA-expressed CYP1A2 and CYP3A4 and is metabolized to 7-hydroxy-4-trifluoromethylcoumarin (HFC). 7-Benzyloxy-4-(trifluoromethyl)coumarin is used for rapid CYP isoform metabolism and inhibition screening studies .
    7-Benzyloxy-4-(trifluoromethyl)coumarin
  • HY-N0598

    20(S)-Ginsenoside F1

    Cytochrome P450 Endogenous Metabolite Cancer
    Ginsenoside F1, an enzymatically modified derivative of Ginsenoside Rg1, demonstrates competitive inhibition of CYP3A4 activity and weaker inhibition of CYP2D6 activity.
    Ginsenoside F1
  • HY-152118

    Cytochrome P450 Cancer
    CYP1B1-IN-4 is a 2,4-diarylthiazole compound with selectively CYP1B1 inhibition (IC50=0.2 nM). CYP1B1-IN-4 has little cytotoxicity and high stability in both human and rat liver microsomes .
    CYP1B1-IN-4
  • HY-W019847

    Cytochrome P450 Infection Metabolic Disease
    Azamulin is an irreversible, highly selective inhibitior of human CYP3Aa. Azamulin has CYP3A inhibition activity with IC50 values range from 0.03-0.24 μM. Azamulin can be used for the research of metabolism and antiinfection .
    Azamulin
  • HY-N0382
    Galangin
    Maximum Cited Publications
    16 Publications Verification

    Norizalpinin; 3,5,7-Trihydroxyflavone

    Cytochrome P450 Autophagy Cancer
    Galangin (Norizalpinin) is an agonist/antagonist of the arylhydrocarbon receptor. Galangin (Norizalpinin) also shows inhibition of CYP1A1 activity.
    Galangin
  • HY-175984

    LPL Receptor Inflammation/Immunology
    S1P1 agonist 7 is a potent, orally active, and β-arrestin-biased S1P1 agonist (EC50(G‑protein) = 12.7 nM and EC50(β‑arrestin) = 3.23 nM). S1P1 agonist 7 demonstrates potent immunomodulatory activity and a favorable safety profile. S1P1 agonist 7 exhibits excellent metabolic stability, minimal to moderate CYP inhibition, and S1P3-sparing selectivity. S1P1 agonist 7 shows pharmacokinetics, effectively reduces circulating lymphocytes, and significantly alleviates disease severity in experimental autoimmune encephalomyelitis (EAE) mouse models under both prophylactic and therapeutic regimens. S1P1 agonist 7 can be used for multiple sclerosis (MS) research .
    S1P1 agonist 7
  • HY-18569AR

    Indole-3-acetic acid sodium (Standard); 3-IAA sodium (Standard)

    Reference Standards Endogenous Metabolite Metabolic Disease
    Ginsenoside F1 (Standard) is the analytical standard of Ginsenoside F1. This product is intended for research and analytical applications. Ginsenoside F1, an enzymatically modified derivative of Ginsenoside Rg1, demonstrates competitive inhibition of CYP3A4 activity and weaker inhibition of CYP2D6 activity.
    3-Indoleacetic acid sodium (Standard)
  • HY-N0598R

    20(S)-Ginsenoside F1 (Standard)

    Reference Standards Cytochrome P450 Endogenous Metabolite Cancer
    Ginsenoside F1 (Standard) is the analytical standard of Ginsenoside F1. This product is intended for research and analytical applications. Ginsenoside F1, an enzymatically modified derivative of Ginsenoside Rg1, demonstrates competitive inhibition of CYP3A4 activity and weaker inhibition of CYP2D6 activity.
    Ginsenoside F1 (Standard)
  • HY-169217

    Cytochrome P450 Cancer
    CYP3A4-IN-4 (compound Δ,Λ-3), a Ru(II)−Ir(III) Conjugate, is a photoactive inhibitor of the major human drug metabolizing enzyme CYP3A4. CYP3A4-IN-4 containing the [Ru(tpy)(Me2bpy)] photocaging group showed an IC50 of 2.2 μM for inhibition of microsomal CYP3A4 under light conditions (λirr=530 nm, tirr=15 min). CYP3A4-IN-4 shows the phototherapeutic index (PI) for of 5.4 .
    CYP3A4-IN-4
  • HY-155456

    Cytochrome P450 Metabolic Disease
    CD-6 is a flavonoid CYP2A6 inhibitor (IC50: 1.566 μM). CYP2A6 inhibits the metabolism of nicotine to cotinine, resulting in an increase in the amount of nicotine available in the blood, leading to increased smoking behavior. CD-6 mediates CYP2A6 inhibition and can be used in research on smoking cessation or smoking-related diseases .
    CYP2A6-IN-1
  • HY-121161

    Cytochrome P450 Metabolic Disease
    (Rac)-Brassinazole, triazole-type compound, is a brassinosteroid (BR) biosynthesis inhibitor. (Rac)-Brassinazole increases inhibition of CYP90B in BR biosynthesis
    (Rac)-Brassinazole
  • HY-167872

    Cytochrome P450 Others
    Bifeprofen, a cytochrome P450 2C9 (CYP2C9) inhibitor, exhibits dose-dependent inhibition (75 μM, 50%) .
    Bifeprofen
  • HY-145786

    Cytochrome P450 Cancer
    Abiraterone decanoate is a potent Abiraterone proagent. Abiraterone decanoate provide a controlled release of Abiraterone and long-acting CYP17 inhibition with intramuscular (IM) delivery .
    Abiraterone decanoate
  • HY-19397

    Potassium Channel Cytochrome P450 Neurological Disease
    BMS-223131 (Compound 1) is a potent maxi-K potassium channel opener. BMS-223131 has a strong inhibitory effect on the CYP2C9 enzyme (IC50 = 1.7 μM) and also shows varying degrees of inhibition on other common CYP enzymes such as CYP1A2, CYP2C19, CYP2D6, and CYP3A4. BMS-223131 can enhance the outward current mediated by maxi-K, by promoting K + efflux to hyperpolarize the cell membrane and reducing Ca 2+ influx. BMS-223131 can be used for the research of neurological disease, such as stroke .
    BMS-223131
  • HY-15996B

    VT-464 (racemate)

    Cytochrome P450 Cancer
    Seviteronel racemate (VT-464 racemate) is the racemate form of Seviteronel (VT-464), which is a potent CYP17 lyase inhibitor(h-Lyase IC50=nM)inhibition.
    Seviteronel racemate
  • HY-125068

    Cytochrome P450 p38 MAPK Inflammation/Immunology
    RPR203494 is a potent inhibitor against CYP isozymes. RPR203494 shows inhibition against p38 kinase with an IC50 value of 9 nM and an EC50 value of 60 nM. RPR203494 demonstrates an inhibition of hepatic Cytochrome P450. RPR203494 is promising for research of rheumatoid arthritis (RA) .
    RPR203494
  • HY-N0382R

    Norizalpinin (Standard); 3,5,7-Trihydroxyflavone (Standard)

    Reference Standards Cytochrome P450 Autophagy Cancer
    Galangin (Standard) is the analytical standard of Galangin. This product is intended for research and analytical applications. Galangin (Norizalpinin) is an agonist/antagonist of the arylhydrocarbon receptor. Galangin (Norizalpinin) also shows inhibition of CYP1A1 activity.
    Galangin (Standard)
  • HY-10572A

    (R)-DMP 266; (R)-EFV; (R)-L-743726

    Reverse Transcriptase Infection
    (R)-Efavirenz ((R)-DMP 266) is a non-nucleoside reverse transcriptase inhibitor that acts by non-competitive inhibition of the viral enzyme. (R)-Efavirenz can be metabolized by CYP2B6 to 8-hydroxyefavirenz in a highly stereoselective manner. (R)-Efavirenz is promising to be a useful probe for the CYP2B6 active site and catalytic mechanisms .
    (R)-Efavirenz
  • HY-N0382S

    Isotope-Labeled Compounds Cytochrome P450 Autophagy Cancer
    Galangin- 13C3 is the 13C-labeled Galangin. Galangin (Norizalpinin) is an agonist/antagonist of the arylhydrocarbon receptor. Galangin (Norizalpinin) also shows inhibition of CYP1A1 activity.
    Galangin-13C3
  • HY-130353

    N-desethylamiodarone hydrochloride; LB 33020 hydrochloride

    Potassium Channel Autophagy Cardiovascular Disease
    Desethylamiodarone hydrochloride (N-desethylamiodarone hydrochloride) is a major active metabolite of Amiodarone. Desethylamiodarone hydrochloride is formed by CYP3A isoenzymes. Amiodarone is an antiarrhythmic agent for inhibition of ATP-sensitive potassium channel with an IC50 of 19.1 μM .
    Desethylamiodarone hydrochloride
  • HY-N0904
    Ginsenoside C-K
    5 Publications Verification

    Ginsenoside compound K; Ginsenoside K

    COX NO Synthase Cytochrome P450 Inflammation/Immunology
    Ginsenoside C-K, a bacterial metabolite of G-Rb1, exhibits anti-inflammatory effects by reducing iNOS and COX-2. Ginsenoside C-K exhibits an inhibition against the activity of CYP2C9 and CYP2A6 in human liver microsomes with IC50s of 32.0±3.6 μM and 63.6±4.2 μM, respectively.
    Ginsenoside C-K
  • HY-135560

    Nicotellin

    Cytochrome P450 Neurological Disease
    Nicotelline (Nicotellin) is a nicotine-related alkaloid, as well as a weak inhibitor of human cDNA-expressed cytochrome P-450 2A6 (CYP2A6). CYP2A6 mediates coumarin 7-hydroxylation, while Nicotelline fails to exhibit inhibition at 300 μM. Nicotelline can be used as a tracer and biomarker of particulate matter (PM) derived from tobacco smoke .
    Nicotelline
  • HY-15565
    APD668
    2 Publications Verification

    GPR119 Cytochrome P450 Potassium Channel Metabolic Disease
    APD668 is a potent, selective and orally active agonist of G-protein coupled receptor GPR119, with EC50s of 2.7 nM and 33 nM for hGPR119 and rGPR119, respectively. APD668 shows no significant inhibition of any of the five major CYP isoforms with the exception of CYP2C9 (Ki=0.1 μM). APD668 can be used for the research of steatohepatitis and diabetes .
    APD668
  • HY-155376

    mTOR Cancer
    mTOR inhibitor-14 (compound 14c) is a potent mTOR inhibitor. mTOR inhibitor-14 also shows minimal CYP2C8 inhibition. mTOR inhibitor-14 can inhibit tumor growth .
    mTOR inhibitor-14
  • HY-130353S

    Isotope-Labeled Compounds Potassium Channel Autophagy Cardiovascular Disease
    Desethyl Amiodarone-d4 (hydrochloride) is the deuterium labeled Desethylamiodarone hydrochloride. Desethylamiodarone hydrochloride (N-desethylamiodarone hydrochloride) is a major active metabolite of Amiodarone. Desethylamiodarone hydrochloride is formed by CYP3A isoenzymes. Amiodarone is an antiarrhythmic agent for inhibition of ATP-sensitive potassium channel with an IC50 of 19.1 μM .
    Desethyl Amiodarone-d4 hydrochloride
  • HY-144285

    CXCR HIV Inflammation/Immunology
    CXCR4 antagonist 4 is a potent, orally active CXCR4 antagonist (IC50=24 nM) with diminished CYP 2D6 activity, improved PAMPA permeability, potent inhibition of human immunodeficiency virus entry (IC50=7 nM) .
    CXCR4 antagonist 4
  • HY-15566
    APD597
    1 Publications Verification

    JNJ-38431055

    GPR119 Metabolic Disease
    APD597 (JNJ-38431055) is an orally active agonist of GPR119. APD597 exhibits reduced CYP2C9 inhibition with an IC50 of 5.8 μM. APD597 can be studied in research for type 2 diabetes .
    APD597
  • HY-50845
    Avagacestat
    2 Publications Verification

    BMS-708163

    γ-secretase Notch Cancer
    Avagacestat (BMS-708163) is a potent inhibitor of γ-secretase, with IC50s of 0.27 nM and 0.30 nM for Aβ42 and Aβ40 inhibition; Avagacestat (BMS-708163) also inhibits NICD (Notch IntraCellular Domain) with IC50 of 0.84 nM and shows weak inhibition of CYP2C19, with IC50 of 20 μM. Avagacestat can be used for Alzheimer disease research.
    Avagacestat
  • HY-15996

    VT-464

    Cytochrome P450 Androgen Receptor Cancer
    Seviteronel (VT-464) is a potent CYP17 lyase inhibitor(h-Lyase IC50=69 nM) and an AR antagonist. Seviteronel demonstrates both exceptional in vitro lyase/hydroxylase selectivity (~10-fold) and oral activity in a hamster model of androgen biosynthesis inhibition.
    Seviteronel
  • HY-134772

    STAT Cytochrome P450 Inflammation/Immunology
    AS1810722 is an orally active and potent STAT6 inhibitor with an IC50 of 1.9 nM. AS1810722 shows a good profile of CYP3A4 inhibition. AS1810722, a derivative of fused bicyclic pyrimidine, has the potential for allergic diseases such as asthma and atopic diseases research .
    AS1810722
  • HY-W130610R

    Liposome Reference Standards Akt mTOR Others
    Ginsenoside C-K (Standard) is the analytical standard of Ginsenoside C-K. This product is intended for research and analytical applications. Ginsenoside C-K, a bacterial metabolite of G-Rb1, exhibits anti-inflammatory effects by reducing iNOS and COX-2. Ginsenoside C-K exhibits an inhibition against the activity of CYP2C9 and CYP2A6 in human liver microsomes with IC50s of 32.0±3.6 μM and 63.6±4.2 μM, respectively.
    Stearamide (Standard)
  • HY-N0904R

    Ginsenoside compound K(Standard); Ginsenoside K (Standard)

    Reference Standards COX NO Synthase Cytochrome P450 Inflammation/Immunology
    Ginsenoside C-K (Standard) is the analytical standard of Ginsenoside C-K. This product is intended for research and analytical applications. Ginsenoside C-K, a bacterial metabolite of G-Rb1, exhibits anti-inflammatory effects by reducing iNOS and COX-2. Ginsenoside C-K exhibits an inhibition against the activity of CYP2C9 and CYP2A6 in human liver microsomes with IC50s of 32.0±3.6 μM and 63.6±4.2 μM, respectively.
    Ginsenoside C-K (Standard)
  • HY-130353R

    N-desethylamiodarone hydrochloride(Standard); LB 33020 hydrochloride (Standard)

    Reference Standards Potassium Channel Autophagy Cardiovascular Disease
    Desethylamiodarone (hydrochloride) (Standard) is the analytical standard of Desethylamiodarone (hydrochloride). This product is intended for research and analytical applications. Desethylamiodarone hydrochloride (N-desethylamiodarone hydrochloride) is a major active metabolite of Amiodarone. Desethylamiodarone hydrochloride is formed by CYP3A isoenzymes. Amiodarone is an antiarrhythmic agent for inhibition of ATP-sensitive potassium channel with an IC50 of 19.1 μM .
    Desethylamiodarone hydrochloride (Standard)
  • HY-146410

    Angiotensin Receptor Others
    AT2R antagonist 1 (compound 21) is a potent and high selective AT2R (angiotensin II AT2 receptor) ligand. AT2R antagonist 1 exhibits a fair AT2R affinity, with a Ki of 29 nM. AT2R antagonist 1 also inhibits common agent-metabolizing CYP enzymes. AT2R antagonist 1 shows high stability in human, rat and mouse liver microsomes .
    AT2R antagonist 1
  • HY-175804

    SARS-CoV Infection
    M2 ion channel blocker-2 (Compound 10) is a M2 channel blocker. M2 ion channel blocker-2 significantly blocks wild-type and mutant M2 (L27F and V27A) ion channels. M2 ion channel blocker-2 has potent antiviral activity against HCoV-229E (EC50: 4.7  μM in cytopathic effect) but not against influenza A virus. M2 ion channel blocker-2 has no significant inhibition of hERG and cytochrome P450 (CYP1A2, CYP2C19, and CYP3A4) activity .
    M2 ion channel blocker-2
  • HY-15565R

    GPR119 Cytochrome P450 Potassium Channel Metabolic Disease
    APD668 (Standard) is the analytical standard of APD668. This product is intended for research and analytical applications. APD668 is a potent, selective and orally active agonist of G-protein coupled receptor GPR119, with EC50s of 2.7 nM and 33 nM for hGPR119 and rGPR119, respectively. APD668 shows no significant inhibition of any of the five major CYP isoforms with the exception of CYP2C9 (Ki=0.1 μM). APD668 can be used for the research of steatohepatitis and diabetes .
    APD668 (Standard)
  • HY-141547

    Sodium Channel Cytochrome P450 Inflammation/Immunology
    Nav1.7-IN-8 is a potent blockage of NaV1.7 with high selectivity for the inhibition of NaV1.7 over the subtypes hNaV1.1 and hNaV1.5. Nav1.7-IN-8 inhibits CYP2C9 and CYP3A4 with an IC50 of 0.17 μM and 0.077 μM, respectively. Nav1.7-IN-8 displays significant analgesic effects in rodent models of acute and inflammatory pain .
    Nav1.7-IN-8
  • HY-135111

    Drug Metabolite Infection Metabolic Disease Cancer
    4-Desmethoxy Omeprazole is the active metabolite of Omeprazole. Omeprazole, a proton pump inhibitor (PPI), is available for treatment of acid-related gastrointestinal disorders. Omeprazole shows competitive inhibition of CYP2C19 activity with a Ki of 2 to 6 μM . Omeprazole also inhibits growth of Gram-positive and Gram-negative bacteria .
    4-Desmethoxy Omeprazole
  • HY-10779

    Factor Xa Cytochrome P450 Cardiovascular Disease
    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 .
    BMS-344577
  • HY-50845R

    γ-secretase Notch Cancer
    Avagacestat (Standard) is the analytical standard of Avagacestat. This product is intended for research and analytical applications. Avagacestat (BMS-708163) is a potent inhibitor of γ-secretase, with IC50s of 0.27 nM and 0.30 nM for Aβ42 and Aβ40 inhibition; Avagacestat (BMS-708163) also inhibits NICD (Notch IntraCellular Domain) with IC50 of 0.84 nM and shows weak inhibition of CYP2C19, with IC50 of 20 μM. Avagacestat can be used for Alzheimer disease research.
    Avagacestat (Standard)
  • HY-133116

    Adrenergic Receptor Neurological Disease
    4-Hydroxyatomoxetine is an active metabolite of Atomoxetine. 4-Hydroxyatomoxetine is metabolized by the enzyme cytochrome P450 2D6 (CYP2D6). Atomoxetine hydrochloride is a potent and selective noradrenalin re-uptake inhibitor (Ki values are 5 nM, 77 nM and 1451 nM for inhibition of radioligand binding to human NET, SERT and DAT respectively) .
    4-Hydroxyatomoxetine
  • HY-129923

    Cytochrome P450 Neurological Disease
    (R)-Omeprazole sodium is a gastric acid resistant compound with activity to inhibit gastric acid secretion. (R)-Omeprazole sodium is metabolized in vivo, and its metabolism is primarily affected by cytochrome P450 enzymes. The interaction between (R)-Omeprazole sodium and mannitol may affect its bioavailability in formulations. (R)-Omeprazole sodium exhibits reversible direct and metabolism-dependent inhibition of CYP2C19 .
    (R)-Omeprazole sodium
  • HY-B0113S
    Omeprazole-d3
    1 Publications Verification

    H 16868-d3

    Proton Pump Bacterial Autophagy Infection Metabolic Disease Cancer
    Omeprazole-d3 (H 16868-d3) is deuterium labeled Omeprazole. Omeprazole, a proton pump inhibitor (PPI), is available for treatment of acid-related gastrointestinal disorders. Omeprazole shows competitive inhibition of CYP2C19 activity with a Ki of 2 to 6 μM . Omeprazole also inhibits growth of Gram-positive and Gram-negative bacteria .
    Omeprazole-d3
  • HY-N1457
    Chrysosplenetin
    1 Publications Verification

    P-glycoprotein Cytochrome P450 Ferroptosis Metabolic Disease
    Chrysosplenetin is one of the polymethoxylated flavonoids in Artemisia annua L. (Compositae) and other several Chinese herbs. Chrysosplenetin inhibits P-gp activity and reverses the up-regulated P-gp and MDR1 levels induced by artemisinin (ART). Chrysosplenetin significantly augments the rat plasma level and anti-malarial efficacy of ART, partially due to the uncompetitive inhibition effect of Chrysosplenetin on rat CYP3A .
    Chrysosplenetin
  • HY-B0113A
    Omeprazole sodium
    5+ Cited Publications

    H 16868 sodium

    Proton Pump Autophagy Bacterial Phospholipase Infection Metabolic Disease Cancer
    Omeprazole sodium (H 16868 sodium), a proton pump inhibitor (PPI), is available for treatment of acid-related gastrointestinal disorders. Omeprazole sodium shows competitive inhibition of CYP2C19 activity with a Ki of 2 to 6 μM . Omeprazole sodium also inhibits growth of Gram-positive and Gram-negative bacteria . Omeprazole is a potent brain penetrant neutral sphingomyelinase (N-SMase) inhibitor (exosome inhibitor) .
    Omeprazole sodium
  • HY-W422288

    (Rac)-Ketoconazol; (Rac)-R 41400

    Fungal Cytochrome P450 Infection
    (Rac)-Ketoconazole ((Rac)-R 41400) is an antifungal imidazole compound with oral activity. (Rac)-Ketoconazole interferes with ergosterol synthesis by inhibiting cytochrome P450-dependent 14α-sterol demethylase (CYP51), a key enzyme on the fungal cell membrane, leading to membrane dysfunction and ultimately inhibition of fungal growth and reproduction. (Rac)-Ketoconazole is indicated for studies of fungal infections .
    (Rac)-Ketoconazole
  • HY-B0113
    Omeprazole
    5+ Cited Publications

    H 16868

    Proton Pump Autophagy Bacterial Phospholipase Infection Metabolic Disease Cancer
    Omeprazole (H 16868), a proton pump inhibitor (PPI), is available for treatment of acid-related gastrointestinal disorders. Omeprazole shows competitive inhibition of CYP2C19 activity with a Ki of 2 to 6 μM . Omeprazole also inhibits growth of Gram-positive and Gram-negative bacteria .Omeprazole is a potent brain penetrant neutral sphingomyelinase (N-SMase) inhibitor (exosome inhibitor) .
    Omeprazole
  • HY-147841

    HIV Reverse Transcriptase Infection
    HIV-1 inhibitor-41 (Compound B23) is an orally active non-nucleoside HIV-1 reverse transcriptase inhibitor with EC50 values of 20.8 nM and 50 nM against HIV-1 WT and mutant E138K strain, respectively. HIV-1 inhibitor-41 shows low hERG, no apparent CYP enzymatic inhibition and no acute toxicity .
    HIV-1 inhibitor-41
  • HY-144286

    CXCR Infection
    CXCR4 antagonist 3 (compound 12a) is a potent antagonist of CXCR4 with an IC50 of 11 nM. CXCR4 antagonist 3 is a congener of TIQ15. CXCR4 antagonist 3 demonstrates the best overall properties including CXCR4 antagonism, CYP 2D6 inhibition, metabolic stability, and permeability. CXCR4 antagonist 3 has the potential for the research of human immunodeficiency virus .
    CXCR4 antagonist 3
  • HY-157929

    Keap1-Nrf2 Inflammation/Immunology Cancer
    Keap1-Nrf2-IN-19 (compound 33) is an oral active Keap1-Nrf2 protein–protein interaction (PPI) inhibitor with the Kd value of 0.0014 μM. Keap1-Nrf2-IN-19 exhibits less than 50% inhibition at 30 μM against hERG and 10 μM against CYPs .
    Keap1-Nrf2-IN-19

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