P450 1A1

By Targets:	Cytochrome P450 (17) Adenosine Receptor (1) Bacterial (2) BCRP (1) Drug Metabolite (1) Endogenous Metabolite (3) Fungal (1) GABA Receptor (1) Isotope-Labeled Compounds (1) Na+/K+ ATPase (2) NO Synthase (2) P-glycoprotein (1) PROTACs (1) Pyroptosis (1)
By Research Areas:	Cancer (11) Cardiovascular Disease (3) Infection (3) Inflammation/Immunology (4) Metabolic Disease (2) Neurological Disease (1)
Click Chemistry:	Alkynes (2)

Targets Recommended: Cytochrome P450

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-D0092

7-Ethoxy-4-methylcoumarin	Cytochrome P450	Others
7-Ethoxy-4-methylcoumarin is a coumarin derivative and can be used as a substrate probe of mammalian cytochromes P450 1A1, 2B4 and 2B6 .

HY-N2229

Rhapontigenin 1 Publications Verification
Rhapontigenin 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 .

HY-131452

1-Ethynylpyrene	Cytochrome P450	Cancer
1-Ethynylpyrene is an aryl acetylenic inhibitor of cytochromes P450 1A1, 1A2, and 2B1 with IC₅₀s of 0.18, 0.32, and 0.04 μM, respectively ^[1]. 1-Ethynylpyrene is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

HY-N2233

Rhapontigenin 3'-O-glucoside 1 Publications Verification
Rhapontigenin 3'-O-glucoside is a derivative of Rhapontigenin. Rhapontigenin is a potent inactivator of human P450 1A1 and is a good candidate for a cancer chemopreventive agent .

HY-Y0110

2-Naphthol

Endogenous Metabolite Others

2-Naphthol is a metabolite of naphthalene, catalyzed by cytochrome P450 (CYP) isozymes (CYP 1A1, CYP 1A2, CYP 2A1, CYP 2E1 and CYP 2F2).

2-Naphthol	Endogenous Metabolite	Others
2-Naphthol is a metabolite of naphthalene, catalyzed by cytochrome P450 (CYP) isozymes (CYP 1A1, CYP 1A2, CYP 2A1, CYP 2E1 and CYP 2F2).

HY-N10344

Glucoarabin	Others	Cancer
Glucoarabin is a bioactive glucosinolate. In Hepa1c1c7 cells, hydrolyzed Glucoarabin (hGSL 9) upregulates the phase II detoxification enzyme quinone reductase (NQO1), with no effect on cytochrome P450 (CYP) 1A1 activity .

HY-117532

PenCB PCB 118	Pyroptosis	Cancer
PenCB (PCB 118) could induces pyroptosis by priming and activating NFκB-dependent NLRP3 inflammasome. PCB 118 induces oxidative stress and pyroptosis are dependent on Aryl hydrocarbon receptor (AhR) activation and subsequent cytochrome P450 1A1 upregulation .

HY-Y0110S

2-Naphthol-d8	Endogenous Metabolite	Others
2-Naphthol-d₈ is the deuterium labeled 2-Naphthol[1]. 2-Naphthol is a metabolite of naphthalene, catalyzed by cytochrome P450 (CYP) isozymes (CYP 1A1, CYP 1A2, CYP 2A1, CYP 2E1 and CYP 2F2)[2].

HY-Y0110S1

2-Naphthol-d7	Endogenous Metabolite	Others
2-Naphthol-d₇ is the deuterium labeled 2-Naphthol[1]. 2-Naphthol is a metabolite of naphthalene, catalyzed by cytochrome P450 (CYP) isozymes (CYP 1A1, CYP 1A2, CYP 2A1, CYP 2E1 and CYP 2F2)[2].

HY-112734

4'-Methylchrysoeriol

Cytochrome P450 Cancer

4'-Methylchrysoeriol is a potent inhibitor of Cytochrome P450 enzymes, with an IC₅₀ of 19 nM for human P450 1B1-dependent EROD.

4'-Methylchrysoeriol	Cytochrome P450	Cancer
4'-Methylchrysoeriol is a potent inhibitor of Cytochrome P450 enzymes, with an IC₅₀ of 19 nM for human P450 1B1-dependent EROD.

HY-116050

17(S)-HETE	Cytochrome P450 Na+/K+ ATPase	Cardiovascular Disease Inflammation/Immunology
17S-HETE is arachidonic acid metabolite through cytochrome P-450 pathways. 17S-HETE serves as allosteric activator of the cytochrome **P450 1B1 and inhibitor of ATPase**, induces cardic hypertrophy .

HY-116196

17-HETE	Na+/K+ ATPase Cytochrome P450	Cardiovascular Disease Inflammation/Immunology
17-HETE is arachidonic acid metabolite through cytochrome P-450 pathways, which consists of 17R-HETE and 17S-HETE enantiomers. 17-HETE serves as allosteric activator of the cytochrome **P450 1B1 and inhibitor of ATPase**, induces cardic hypertrophy .

HY-114955

MTTC

Cytochrome P450 Others

MTTC is a 1,2,3-thiadiazole compound that exhibits mechanism-based inactivation, resulting in the inactivation of cytochrome P450 2E1 activity .

MTTC	Cytochrome P450	Others
MTTC is a 1,2,3-thiadiazole compound that exhibits mechanism-based inactivation, resulting in the inactivation of cytochrome **P450 2E1** activity .

HY-D0145

7-Ethoxyresorufin 1 Publications Verification Resorufin ethyl ether	Cytochrome P450 NO Synthase	Others
7-Ethoxyresorufin (Resorufin ethyl ether) is a fluorometric substrate and competitive inhibitor of cytochrome P450, especially *CYP1A1. 7-Ethoxyresorufin also inhibits NO synthase* .

HY-150557

CYP1B1-IN-1

Cytochrome P450 Cancer

CYP1B1-IN-1 (Compound 9e) is a selective cytochrome P450 1B1 (CYP1B1) inhibitor with an IC₅₀ of 0.49 nM .
HY-152196

CYP1B1-IN-5

Cytochrome P450 Cancer

CYP1B1-IN-5 (Compound 6q) is a potent and selective cytochrome P450 1B1 (CYP1B1) inhibitor with an IC₅₀ of 4.7 nM .
HY-150558

CYP1B1-IN-2

Cytochrome P450 Cancer

CYP1B1-IN-2 (compound 9j) is a potent and selective CYP1B1 (cytochrome P450 1B1) inhibitor, with an IC₅₀ of 0.52 nM .

CYP1B1-IN-1	Cytochrome P450	Cancer
CYP1B1-IN-1 (Compound 9e) is a selective cytochrome P450 1B1 (CYP1B1) inhibitor with an IC₅₀ of 0.49 nM .

CYP1B1-IN-5	Cytochrome P450	Cancer
CYP1B1-IN-5 (Compound 6q) is a potent and selective cytochrome P450 1B1 (CYP1B1) inhibitor with an IC₅₀ of 4.7 nM .

CYP1B1-IN-2	Cytochrome P450	Cancer
CYP1B1-IN-2 (compound 9j) is a potent and selective *CYP1B1* (cytochrome P450 1B1) inhibitor, with an IC₅₀ of 0.52 nM .

HY-128920

Phortress free base	Cytochrome P450	Cancer
Phortress free base (NSC 710305) is a P450 *CYP1A1*-activated antitumor prodrug with antitumor activity . Phortress free base leads to DNA damage and cell cycle arrest .

HY-111430

1-Ethynylnaphthalene	Cytochrome P450	Cancer
1-Ethynylnaphthalene is a selective inhibitor of cytochrome **P450 1B1**. 1-Ethynylnaphthalene is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

HY-N4205

Tetrahydropiperine	Cytochrome P450	Cancer
Tetrahydropiperine, a cyclohexyl analogue of piperine, is the first natural aryl pentanamide from Piper longum . Tetrahydropiperine (compound 14) inhibits the cytochrome P450 (CYP) isoform CYP1A1/arylhydrocarbon hydroxylase (AHH; IC₅₀=23 µM) .

HY-D0145S

7-Ethoxyresorufin-d5 Resorufin ethyl ether-d₅	Isotope-Labeled Compounds Cytochrome P450 NO Synthase	Others
7-Ethoxyresorufin-d₅ is deuterium labeled 7-Ethoxyresorufin. 7-Ethoxyresorufin (Resorufin ethyl ether) is a fluorometric substrate and competitive inhibitor of cytochrome P450, especially CYP1A1. 7-Ethoxyresorufin also inhibits NO synthase[1][2].

HY-147721

Dihydropteroate synthase-IN-1	Bacterial	Infection
Dihydropteroate synthase-IN-1 (compound 5g) is a potent dihydropteroate synthase (DHPS) inhibitor. Dihydropteroate synthase-IN-1 shows antimicrobial activities and antifungal activity. Dihydropteroate synthase-IN-1 inhibits cytochromes P450. Dihydropteroate synthase-IN-1 can bu used as diagnostic radio imaging material .

HY-147336

Desmethylazelastine	Drug Metabolite	Infection Cardiovascular Disease Metabolic Disease Inflammation/Immunology
Desmethylazelastine is a main active metabolite of Azelastine that is oxidatively metabolized by the cytochrome P450 enzyme system with a protein binding rate of 97% and an elimination half-life of 54 hours. Azelastine is an orally active, selective and high-affinity histamine H1-receptor antagonist. Azelastine can be used in studies of allergic rhinitis, asthma, diabetic hyperlipidemic and SARS-CoV-2 .

HY-147999

GlcN-6-P Synthase-IN-1	Bacterial Fungal Cytochrome P450	Infection
GlcN-6-P Synthase-IN-1 (Compound 4d) is a Glucosamine-6-phosphate (GlcN-6-P) synthase inhibitor with an IC₅₀ of 3.47 μM. GlcN-6-P Synthase-IN-1 exhibits significant antimicrobial activity. GlcN-6-P Synthase-IN-1 has good penetration in the CNS and is able to inhibit the cytochrome P450, CYP3A4 isoform .

HY-10965

Rolofylline KW-3902	Adenosine Receptor	Neurological Disease
Rolofylline (KW-3902) is a potent, selective adenosine A1 receptor antagonist that is under development for the treatment of patients with acute congestive heart failure and renal impairment. Rolofylline is metabolized primarily to the pharmacologically active M1-trans and M1-cis metabolites by cytochrome P450 (CYP₄₅₀) . Rolofylline is alleviating the presynaptic dysfunction and restores neuronal activity as well as dendritic spine levels in vitro, is an interesting candidate to combat the hypometabolism and neuronal dysfunction associated with Tau-induced neurodegenerative diseases .

HY-108347

CP-100356 hydrochloride 2 Publications Verification	P-glycoprotein BCRP	Metabolic Disease
CP-100356 hydrochloride is an orally active dual MDR1 (P-gp)/BCRP inhibitor, with an IC₅₀s of 0.5 and 1.5 µM for inhibiting MDR1-mediated Calcein-AM transport and BCRP-mediated Prazosin transport, respectively. CP-100356 hydrochloride is also a weak inhibitor of *OATP1B1* (IC₅₀=∼66 µM). CP-100356 hydrochloride is devoid of inhibition against MRP2 and major human P450 enzymes (IC₅₀>15 µM) .

HY-146393

PROTAC CYP1B1 degrader-1	PROTACs Cytochrome P450	Cancer
PROTAC CYP1B1 degrader-1 (Compound 6C), a α-naphthoflavone chimera derivative, is able to eliminate cytochrome P450 (CYP)1B1-mediated agent resistance via targeted *CYP1B1* degradation, with IC₅₀s of 95.1 and 9838.6 nM for CYP1B1 and CYP1A2, respectively. PROTAC CYP1B1 degrader-1 can be used for the research of CYP1B1-overexpressing prostate cancer .

HY-B0822S1

Fipronil-13C6	GABA Receptor Cytochrome P450	Inflammation/Immunology
Fipronil- ¹³C₆ is the ¹³C-labeled Fipronil. Fipronil is an insecticide that acts as a selective antagonist of insect GABA receptors (IC50s = 30 nM and 1,600 nM for cockroach and rat receptors, respectively). Fipronil also inhibits desensitizing and non-desensitizing glutamate-induced chloride currents in cockroach neurons (IC50s = 800 nM and 10 nM, respectively). Fipronil induces activity of the cytochrome P450 (CYP) isoforms CYP1A1/2, CYP2B1/2, and CYP3A1/2 in isolated rat liver microsomes.

Cat. No.	Product Name

HY-L034

Anti-Aging Compound Library	4352 compounds
Aging is a complex biological process characterized by functional decline of tissues and organs, structural degeneration, and reduced adaptability and resistance, all of which contribute to an increase in morbidity and mortality caused by multiple chronic diseases, such as Alzheimer's disease, cancer, and diabetes. Many theories, which fall into two main categories: programmed and error theories, have been proposed to explain the process of aging, but neither of them appears to be fully satisfactory. The programmed theories imply that aging relies on specific gene regulation, and the error theories emphasize the internal and environmental damages accumulated to living organisms. The damage theories proposed the nine hallmarks that were generally considered to contribute to the aging process: genomic instability, telomere attrition, epigenetic alterations, loss of proteostasis, deregulated nutrient-sensing, mitochondrial dysfunction, cellular senescence, stem cell exhaustion, and altered intercellular communication. MCE Anti-Aging Compound Library contains 4352 compounds, mainly targeting Sirtuin, mTOR, IGF-1R, AMPK, p53, Telomerase, Mitophagy, Mitochondrial Metabolism, COX, Cytochrome P450, Oxidase, etc. This library is a useful tool for anti-aging research.

Anti-Aging Compound Library

4352 compounds

Aging is a complex biological process characterized by functional decline of tissues and organs, structural degeneration, and reduced adaptability and resistance, all of which contribute to an increase in morbidity and mortality caused by multiple chronic diseases, such as Alzheimer's disease, cancer, and diabetes. Many theories, which fall into two main categories: programmed and error theories, have been proposed to explain the process of aging, but neither of them appears to be fully satisfactory. The programmed theories imply that aging relies on specific gene regulation, and the error theories emphasize the internal and environmental damages accumulated to living organisms. The damage theories proposed the nine hallmarks that were generally considered to contribute to the aging process: genomic instability, telomere attrition, epigenetic alterations, loss of proteostasis, deregulated nutrient-sensing, mitochondrial dysfunction, cellular senescence, stem cell exhaustion, and altered intercellular communication.

MCE Anti-Aging Compound Library contains 4352 compounds, mainly targeting Sirtuin, mTOR, IGF-1R, AMPK, p53, Telomerase, Mitophagy, Mitochondrial Metabolism, COX, Cytochrome P450, Oxidase, etc. This library is a useful tool for anti-aging research.

Cat. No.	Product Name	Type

HY-D0092

7-Ethoxy-4-methylcoumarin	Fluorescent Dyes/Probes
7-Ethoxy-4-methylcoumarin is a coumarin derivative and can be used as a substrate probe of mammalian cytochromes P450 1A1, 2B4 and 2B6 .

HY-D0145

7-Ethoxyresorufin 1 Publications Verification Resorufin ethyl ether	Chromogenic Substrates
7-Ethoxyresorufin (Resorufin ethyl ether) is a fluorometric substrate and competitive inhibitor of cytochrome P450, especially *CYP1A1. 7-Ethoxyresorufin also inhibits NO synthase* .

Cat. No.	Product Name	Category	Target	Chemical Structure

HY-Y0110

2-Naphthol	Monophenols Microorganisms Classification of Application Fields Source classification Other Diseases Phenols Endogenous metabolite Disease Research Fields	Endogenous Metabolite
2-Naphthol is a metabolite of naphthalene, catalyzed by cytochrome P450 (CYP) isozymes (CYP 1A1, CYP 1A2, CYP 2A1, CYP 2E1 and CYP 2F2).

HY-N4205

Tetrahydropiperine	Alkaloids Piperidine Alkaloids Classification of Application Fields Source classification Piperaceae Plants Disease Research Fields Piper nigrum Linn. Cancer	Cytochrome P450
Tetrahydropiperine, a cyclohexyl analogue of piperine, is the first natural aryl pentanamide from Piper longum . Tetrahydropiperine (compound 14) inhibits the cytochrome P450 (CYP) isoform CYP1A1/arylhydrocarbon hydroxylase (AHH; IC₅₀=23 µM) .

HY-N10344

Glucoarabin	Structural Classification Natural Products Classification of Application Fields Source classification Camelina sativa (L.) Crantz Glucosinolates Plants Brassicaceae Disease Research Fields Cancer	Others
Glucoarabin is a bioactive glucosinolate. In Hepa1c1c7 cells, hydrolyzed Glucoarabin (hGSL 9) upregulates the phase II detoxification enzyme quinone reductase (NQO1), with no effect on cytochrome P450 (CYP) 1A1 activity .

Cat. No.	Product Name	Chemical Structure

HY-Y0110S1

2-Naphthol-d7
2-Naphthol-d₇ is the deuterium labeled 2-Naphthol[1]. 2-Naphthol is a metabolite of naphthalene, catalyzed by cytochrome P450 (CYP) isozymes (CYP 1A1, CYP 1A2, CYP 2A1, CYP 2E1 and CYP 2F2)[2].

HY-Y0110S

2-Naphthol-d8
2-Naphthol-d₈ is the deuterium labeled 2-Naphthol[1]. 2-Naphthol is a metabolite of naphthalene, catalyzed by cytochrome P450 (CYP) isozymes (CYP 1A1, CYP 1A2, CYP 2A1, CYP 2E1 and CYP 2F2)[2].

HY-D0145S

7-Ethoxyresorufin-d5
7-Ethoxyresorufin-d₅ is deuterium labeled 7-Ethoxyresorufin. 7-Ethoxyresorufin (Resorufin ethyl ether) is a fluorometric substrate and competitive inhibitor of cytochrome P450, especially CYP1A1. 7-Ethoxyresorufin also inhibits NO synthase[1][2].

HY-B0822S1

Fipronil-13C6
Fipronil- ¹³C₆ is the ¹³C-labeled Fipronil. Fipronil is an insecticide that acts as a selective antagonist of insect GABA receptors (IC50s = 30 nM and 1,600 nM for cockroach and rat receptors, respectively). Fipronil also inhibits desensitizing and non-desensitizing glutamate-induced chloride currents in cockroach neurons (IC50s = 800 nM and 10 nM, respectively). Fipronil induces activity of the cytochrome P450 (CYP) isoforms CYP1A1/2, CYP2B1/2, and CYP3A1/2 in isolated rat liver microsomes.

Fipronil-13C6

Fipronil- ¹³C₆ is the ¹³C-labeled Fipronil. Fipronil is an insecticide that acts as a selective antagonist of insect GABA receptors (IC50s = 30 nM and 1,600 nM for cockroach and rat receptors, respectively). Fipronil also inhibits desensitizing and non-desensitizing glutamate-induced chloride currents in cockroach neurons (IC50s = 800 nM and 10 nM, respectively). Fipronil induces activity of the cytochrome P450 (CYP) isoforms CYP1A1/2, CYP2B1/2, and CYP3A1/2 in isolated rat liver microsomes.

Cat. No.	Product Name		Classification

HY-131452

1-Ethynylpyrene		Alkynes
1-Ethynylpyrene is an aryl acetylenic inhibitor of cytochromes P450 1A1, 1A2, and 2B1 with IC₅₀s of 0.18, 0.32, and 0.04 μM, respectively ^[1]. 1-Ethynylpyrene is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

HY-111430

1-Ethynylnaphthalene		Alkynes
1-Ethynylnaphthalene is a selective inhibitor of cytochrome **P450 1B1**. 1-Ethynylnaphthalene is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

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