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CYP1A1 Inhibitors

" in MedChemExpress (MCE) Product Catalog:

By Targets:	Apoptosis (1) Aryl Hydrocarbon Receptor (3) Checkpoint Kinase (Chk) (1) Cytochrome P450 (17) ERK (1) Fungal (1) GABA Receptor (2) Isotope-Labeled Compounds (1) NO Synthase (2)
By Research Areas:	Cancer (13) Infection (1) Inflammation/Immunology (1) Metabolic Disease (1) Neurological Disease (2)

Inhibitors & Agonists

Fluorescent Dye

Natural
Products

Isotope-Labeled Compounds

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-N2194

Bergamottin

5 Publications Verification

5-Geranoxypsoralen; Bergamotine; Bergaptin

Bergamottin is a potent and competitive CYP1A1 inhibitor with a K_i of 10.703 nM.
HY-101284

DMU2105

DMU2105 is a potent and specific CYP1B1 inhibitor, with IC₅₀s of 10 nM and 742 nM for CYP1B1 and CYP1A1, respectively.
HY-101285

DMU2139

DMU2139 is a potent and specific CYP1B1 inhibitor, with IC₅₀s of 9 nM and 795 nM for CYP1B1 and CYP1A1, respectively.

Bergamottin 5 Publications Verification 5-Geranoxypsoralen; Bergamotine; Bergaptin
Bergamottin is a potent and competitive *CYP1A1* inhibitor with a K_i of 10.703 nM.

DMU2105
DMU2105 is a potent and specific *CYP1B1* inhibitor, with IC₅₀s of 10 nM and 742 nM for CYP1B1 and CYP1A1, respectively.

DMU2139
DMU2139 is a potent and specific *CYP1B1* inhibitor, with IC₅₀s of 9 nM and 795 nM for CYP1B1 and CYP1A1, respectively.

HY-148595

Antitumor agent-88	Cytochrome P450	Cancer
Antitumor agent-88 exhibits potent antimitotic activity and arrests cell in the G2/M phase. Antitumor agent-88 disrupts the microtubule and the cytoskeleton in CYP1A1-expressing breast cancer cells. Antitumor agent-88 is also a competitive inhibitor of *CYP1A1* (K_i: 1.4 μM) .

HY-118216

Bitertanol Biloxazol	Fungal Cytochrome P450	Infection
Bitertanol (Biloxazol) is a potent antifungal agent. Bitertanol also is an *CYP1A1, CYP2B, and CYP3A* inducer in vivo and an *CYP1A* inhibitor in vitro .

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-N6264

26-Deoxyactein	Aryl Hydrocarbon Receptor ERK	Metabolic Disease
26-Deoxyactein is a constituent isolated from Cimicifuga racemosa, prevents TCDD-induced osteoblasts damage. 26-Deoxyactein inhibits increased AhR, CYP1A1 and ERK levels .

HY-134217

KYN-101	Aryl Hydrocarbon Receptor	Cancer
KYN-101 is a potent, selective and orally active AHR inhibitor. KYN-101 decreases the CYP1A1 mRNA expression. KYN-101 shows anti-cancer activity .

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-152079

CYP1B1-IN-3	Cytochrome P450	Cancer
CYP1B1-IN-3 is a potent and selective *CYP1B1* inhibitor with IC₅₀ values of 6.6, 347.3, >10000 nM for CYP1B1, CYP1A1, CYP1A2, respectively. CYP1B1-IN-3 inhibits cell migration and invasion. CYP1B1-IN-3 inhibits P-gp, AKT/ERK, FAK/SRC, and EMT pathways .

HY-N2625A

Harmalol hydrochloride	Cytochrome P450	Others
Harmalol hydrochloride, a beta carboline alkaloid, presents in several medicinal plants such as Peganum harmala. Harmalol hydrochloride, main metabolite of Harmaline, significantly inhibits the dioxin-mediated induction of CYP1A1 at the transcriptional and posttranslational levels. Harmalol hydrochloride possesses antioxidant and hydroxyl radical-scavenging properties .

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-N8382

Chalepensin	Cytochrome P450	Neurological Disease
Chalepensin, a furanocoumarin, is a competitive CYP2A6 inhibitor. Chalepensin also inhibits human CYP1A1, CYP1A2, CYP2A13, CYP2C9, CYP2D6, CYP2E1, and CYP3A4 to different extents .

HY-N2689

(R)-6',7'-Dihydroxybergamottin (R)-6′,7′-DHB	Cytochrome P450	Cancer
(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 .

HY-19340

TMS 5 Publications Verification (E)-2,3',4,5'-tetramethoxystilbene	Cytochrome P450	Cancer
TMS ((E)-2,3',4,5'-tetramethoxystilbene) is a selective and competitive *CYP1B1* inhibitor with an IC₅₀ of 6 nM and a K_i value of 3 nM. TMS shows a lesser extent inhibitory effect on CYP1A1 (IC₅₀=300 nM) and CYP1A2 (IC₅₀=3.1 μM). TMS is a methylated derivative of resveratrol and has anti-cancer activity .

HY-B0822

Fipronil
Fipronil is a broad-spectrum insecticide effective against Lepidoptera species as well as thrips, locusts, ants, cockroaches, fleas and ticks. Fipronil selectively inhibits GABA receptor with IC₅₀s of 30 nM and 1600 nM for cockroach and rat GABA receptors, respectively. Glutamate-gated chloride channels (GluCls), which are present in cockroaches but not in mammals, are sensitive to the blocking effect of Fipronil. Fipronil also induces apoptosis in HepG2 cells and promotes the expression of CYP1A1 and CYP3A4 mRNA in human hepatocytes .

HY-B0822R

Fipronil (Standard)	GABA Receptor Cytochrome P450 Apoptosis	Neurological Disease
Fipronil (Standard) is the analytical standard of Fipronil. This product is intended for research and analytical applications. Fipronil is a broad-spectrum insecticide effective against Lepidoptera species as well as thrips, locusts, ants, cockroaches, fleas and ticks. Fipronil selectively inhibits GABA receptor with IC₅₀s of 30 nM and 1600 nM for cockroach and rat GABA receptors, respectively. Glutamate-gated chloride channels (GluCls), which are present in cockroaches but not in mammals, are sensitive to the blocking effect of Fipronil. Fipronil also induces apoptosis in HepG2 cells and promotes the expression of CYP1A1 and CYP3A4 mRNA in human hepatocytes .

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.

HY-162051

CYP1B1-IN-6	Cytochrome P450	Cancer
CYP1B1-IN-6 (compound 19) is a fluorescence molecular probes which inhibits *CYP1B1* activity. CYP1B1-IN-6 can identify tumor sites in fluorescence imaging and photoacoustic imaging modes .

HY-157942

CYP1B1-IN-7	Cytochrome P450	Cancer
CYP1B1-IN-7 (compound 2a) is a selective inhibitor of CYP1B1 (IC₅₀: 75 nM). CYP1B1-IN-7 also reverses resistance (IC₅₀: 29 μM) and exhibits cytotoxicity in the CYP1B1-overexpressing MCF-7 cell line that is resistant to Docetaxel (HY-B0011) .

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-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 .
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-101284A

(E/Z)-DMU2105

Others Cancer

(E/Z)-DMU2105 is the E/Z isomer of DMU2105 (HY-101284). DMU2105 is a CYP1B1 inhibitor .

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-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-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 .

(E/Z)-DMU2105	Others	Cancer
(E/Z)-DMU2105 is the E/Z isomer of DMU2105 (HY-101284). DMU2105 is a CYP1B1 inhibitor .

HY-117102

ANI-7	Aryl Hydrocarbon Receptor Checkpoint Kinase (Chk)	Cancer
ANI-7 is an activator of aryl hydrocarbon receptor (AhR) pathway. ANI-7 inhibits the growth of multiple cancer cells, and potently and selectively inhibits the growth of MCF-7 breast cancer cells with a GI₅₀ of 0.56 μM. ANI-7 induces CYP1-metabolizing mono-oxygenases by activating AhR pathway, and also induces DNA damage, checkpoint Kinase 2 (Chk2) activation, S-phase cell cycle arrest, and cell death in sensitive breast cancer cell lines .

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 .

CYP1B1-IN-6	Fluorescent Dyes/Probes
CYP1B1-IN-6 (compound 19) is a fluorescence molecular probes which inhibits *CYP1B1* activity. CYP1B1-IN-6 can identify tumor sites in fluorescence imaging and photoacoustic imaging modes .

Cat. No.	Product Name	Category	Target	Chemical Structure

HY-N6264

26-Deoxyactein	Triterpenes Classification of Application Fields Terpenoids Source classification Ranunculaceae Metabolic Disease Plants Cimicifuga foetida Linn. Cimicifuga racemosa (L.) Nutt. Disease Research Fields	Aryl Hydrocarbon Receptor ERK
26-Deoxyactein is a constituent isolated from Cimicifuga racemosa, prevents TCDD-induced osteoblasts damage. 26-Deoxyactein inhibits increased AhR, CYP1A1 and ERK levels .

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-N2625A

Harmalol hydrochloride	Alkaloids Structural Classification Monophenols Classification of Application Fields Zygophyllaceae Source classification Peganum harmala Linn. Other Diseases Phenols Pyridine Alkaloids Plants Disease Research Fields	Cytochrome P450
Harmalol hydrochloride, a beta carboline alkaloid, presents in several medicinal plants such as Peganum harmala. Harmalol hydrochloride, main metabolite of Harmaline, significantly inhibits the dioxin-mediated induction of CYP1A1 at the transcriptional and posttranslational levels. Harmalol hydrochloride possesses antioxidant and hydroxyl radical-scavenging properties .

HY-N8382

Chalepensin	Structural Classification Natural Products Haloxylon ammodendron (C. A. Mey.) Bunge Source classification Amaranthaceae Plants	Cytochrome P450
Chalepensin, a furanocoumarin, is a competitive CYP2A6 inhibitor. Chalepensin also inhibits human CYP1A1, CYP1A2, CYP2A13, CYP2C9, CYP2D6, CYP2E1, and CYP3A4 to different extents .

HY-N2689

(R)-6',7'-Dihydroxybergamottin (R)-6′,7′-DHB	Structural Classification Natural Products Citrus × aurantium Linnaeus Source classification Rutaceae Plants	Cytochrome P450
(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 .

Cat. No.	Product Name	Chemical Structure

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.

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CYP1A1 Inhibitors

Inhibitors & Agonists

Fluorescent Dye

NaturalProducts

Isotope-Labeled Compounds

Natural
Products