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CYP1A1-IN-2

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By Targets:	Cytochrome P450 (9) E3 Ligase Ligand-Linker Conjugates (1) Endogenous Metabolite (1) Environmental Pollutants (1) Fungal (2) Ligands for Target Protein for PROTAC (1) PROTAC Linkers (1) PROTACs (1) Reference Standards (2)
By Research Areas:	Cancer (9) Infection (2) Metabolic Disease (1)

Inhibitors & Agonists

Natural
Products

Art. -Nr.	Produktname	Target	Forschungsgebiete	Chemical Structure

HY-W017113

2-Mercaptobenzothiazole 1 Publications Verification	Environmental Pollutants Endogenous Metabolite	Metabolic Disease
2-Mercaptobenzothiazole is an activator of the aryl hydrocarbon receptor (AhR) , inhibiting thyroid hormone synthesis and dopamine beta-hydroxylase activity . 2-Mercaptobenzothiazole promotes bladder cancer cell invasion by altering the conformation of the AhR ligand binding domain (LBD), activating AhR transcription, and upregulating the mRNA and protein expression of target genes CYP1A1 and CYP1B1 . 2-Mercaptobenzothiazole inhibits thyroid peroxidase (TPO) with an IC₅₀ value of 11.5 μM, induces histological changes such as follicular cell hypertrophy in Xenopus laevis tadpoles, delaying metamorphosis . 2-Mercaptobenzothiazole increases chromosomal aberrations and sister chromatid exchanges (SCEs) in Chinese hamster ovary (CHO) cells, and enhances carcinogenicity in F344/N rats . 2-Mercaptobenzothiazole inhibits norepinephrine synthesis in mice and completely blocks the conversion of exogenous dopamine to norepinephrine in rat cardiomyocytes .

HY-N5132

(-)-Fenchone	Cytochrome P450	Others
(-)-Fenchone is a bicyclic monoterpene and serves as a substrate for human liver microsomal cytochrome P450 enzymes CYP2A6 and CYP2B6. (-)-Fenchone is not metabolized by human CYP1A1, CYP1A2, CYP1B1, CYP2C8, CYP2C9, CYP2C19, CYP2D6, CYP2E1, or CYP3A4 enzymes. (-)-Fenchone undergoes hydroxylation to produce 6-exo-hydroxyfenchone, 6-endo-hydroxyfenchone, and 10-hydroxyfenchone. During the metabolism of (-)-Fenchone, CYP2A6 may play a more important role than CYP2B6 .

HY-W007700

8-Bromooctanoic acid	PROTAC Linkers	Cancer
8-Bromooctanoic acid is a PROTAC linker, and can be used for synthesis of PROTAC CYP1B1 degrader-2 (HY-158429) .

HY-148595

*CYP1A1-IN-2*	Cytochrome P450	Cancer
CYP1A1-IN-2 (Compound 14) is a competitive inhibitor of *CYP1A1* (K_i: 1.4 μM). CYP1A1-IN-2 exhibits potent antimitotic activity and arrests cell in the G2/M phase. CYP1A1-IN-2 disrupts the microtubule and the cytoskeleton in CYP1A1-expressing breast cancer cells .

HY-103223

Phortress NSC 710305	Cytochrome P450	Cancer
Phortress is a high affinity AhR ligand that elicits antitumor activity by inducing transcription of CYP1A1 .

HY-159006

CYP1B1 ligand 3	Cytochrome P450	Cancer
CYP1B1 ligand 3 (Compound A1) is a selective inhibitor for cytochrome P450 enzyme CYP1B1 with an IC₅₀ of 11.9 nM. CYP1B1 ligand 3 can be utilized for the synthesis of PROTAC CYP1B1 degrader-2 (HY-158429) .

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-158430

*CYP1B1 ligand 2*	Ligands for Target Protein for PROTAC	Cancer
CYP1B1 ligand 2 is a target protein ligand of PROTAC CYP1B1 degrader-2 (HY-158429). CYP1B1 ligand 2 can be used to study lung cancer .

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-158431

(S,R,S)-AHPC-Me-8-bromooctanoic acid	E3 Ligase Ligand-Linker Conjugates	Cancer
(S,R,S)-AHPC-Me-8-bromooctanoic acid is an E3 ligase ligand-linker conjugate, and can be used for synthesis of PROTAC CYP1B1 degrader-2 (HY-158429) .

HY-158429

PROTAC CYP1B1 degrader-2	PROTACs Cytochrome P450	Cancer
PROTAC CYP1B1 degrader-2 (compound PV2) is a von Hippel-Landau (VHL) E3 ligase-based CYP1B1 degrader with the DC₅₀ of 1.0 nM at 24 h in A549/Taxol cells. PROTAC CYP1B1 degrader-2 inhibits growth, migration, and invasion of A549/Taxol cell(Sturcture Note:(Blue: VHL ligand (HY-112078), Black: linker (HY-W007700), Pink: CYP1B1 ligand (HY-159006) .

HY-118216R

Bitertanol (Standard) Biloxazol (Standard)	Reference Standards Fungal Cytochrome P450	Infection
Bitertanol (Standard) is the analytical standard of Bitertanol. This product is intended for research and analytical applications. 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-103223R

Phortress (Standard) NSC 710305 (Standard)	Reference Standards Cytochrome P450	Cancer
Phortress (Standard) is the analytical standard of Phortress (HY-103223). This product is intended for research and analytical applications. Phortress is a high affinity AhR ligand that elicits antitumor activity by inducing transcription of CYP1A1 .

Art. -Nr.	Produktname	Category	Target	Chemical Structure

HY-W017113

2-Mercaptobenzothiazole 1 Publications Verification	Structural Classification Natürliche Produkte Classification of Application Fields Metabolic Disease Endogenous metabolite Disease Research Fields Source Classification	Environmental Pollutants Endogenous Metabolite
2-Mercaptobenzothiazole is an activator of the aryl hydrocarbon receptor (AhR) , inhibiting thyroid hormone synthesis and dopamine beta-hydroxylase activity . 2-Mercaptobenzothiazole promotes bladder cancer cell invasion by altering the conformation of the AhR ligand binding domain (LBD), activating AhR transcription, and upregulating the mRNA and protein expression of target genes CYP1A1 and CYP1B1 . 2-Mercaptobenzothiazole inhibits thyroid peroxidase (TPO) with an IC₅₀ value of 11.5 μM, induces histological changes such as follicular cell hypertrophy in Xenopus laevis tadpoles, delaying metamorphosis . 2-Mercaptobenzothiazole increases chromosomal aberrations and sister chromatid exchanges (SCEs) in Chinese hamster ovary (CHO) cells, and enhances carcinogenicity in F344/N rats . 2-Mercaptobenzothiazole inhibits norepinephrine synthesis in mice and completely blocks the conversion of exogenous dopamine to norepinephrine in rat cardiomyocytes .

HY-N5132

(-)-Fenchone	Structural Classification Other Monoterpenes Classification of Application Fields Terpenoids Other Diseases Umbelliferae Plants Vernonia Schreb. Disease Research Fields Source Classification	Cytochrome P450
(-)-Fenchone is a bicyclic monoterpene and serves as a substrate for human liver microsomal cytochrome P450 enzymes CYP2A6 and CYP2B6. (-)-Fenchone is not metabolized by human CYP1A1, CYP1A2, CYP1B1, CYP2C8, CYP2C9, CYP2C19, CYP2D6, CYP2E1, or CYP3A4 enzymes. (-)-Fenchone undergoes hydroxylation to produce 6-exo-hydroxyfenchone, 6-endo-hydroxyfenchone, and 10-hydroxyfenchone. During the metabolism of (-)-Fenchone, CYP2A6 may play a more important role than CYP2B6 .

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BODIPY 493/503 purchased from MedChemExpress. Usage Cited in: Nat Commun. 2025 Feb 1;16(1):1241. [Abstract]

MedchemExpress Validation 01

Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature. Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature. Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.

BODIPY 493/503 purchased from MedChemExpress. Usage Cited in: Nat Commun. 2025 Feb 1;16(1):1241. [Abstract]

MedchemExpress Validation 01

MedchemExpress Validation 03

Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred

MedchemExpress Validation 04

MedchemExpress Validation

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CYP1A1-IN-2

Inhibitors & Agonists

NaturalProducts

Natural
Products