1. Metabolic Enzyme/Protease Apoptosis
  2. Cytochrome P450 Apoptosis
  3. CYP4Z1-IN-3

CYP4Z1-IN-3 is a selective CYP4Z1 inhibitor with a human IC50 of 55.3 nM. CYP4Z1-IN-3 inhibits breast cancer cell migration and induces apoptosis. CYP4Z1-IN-3 can be used for the research of breast cancer.

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CYP4Z1-IN-3

CYP4Z1-IN-3 Chemical Structure

CAS No. : 3106166-49-5

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Description

CYP4Z1-IN-3 is a selective CYP4Z1 inhibitor with a human IC50 of 55.3 nM. CYP4Z1-IN-3 inhibits breast cancer cell migration and induces apoptosis. CYP4Z1-IN-3 can be used for the research of breast cancer[1].

IC50 & Target[1]

CYP4Z1

55.3 nM (IC50)

In Vitro

CYP4Z1-IN-3 (Compound C8) (0.1-10 μM) potently inhibits CYP4Z1 enzyme activity in lysates from CYP4Z1-overexpressing HEK293T cells with an IC50 of 55.3 nM[1].
CYP4Z1-IN-3 exhibits high isoform selectivity for CYP4Z1 over human CYP2C9, CYP2C19, CYP2D6, and CYP3A4[1].
CYP4Z1-IN-3 (60 min) exhibits favorable metabolic stability in CD-1 mouse liver microsomes, with a half-life of 62.4 min and low intrinsic clearance[1].
CYP4Z1-IN-3 (3 h) shows excellent plasma stability in CD-1 mouse plasma, with a half-life exceeding 3.0 h, while it exhibits poor stability in human plasma[1].
CYP4Z1-IN-3 (0.01-100 μM; 48 h) does not exhibit significant cytotoxicity in MCF-7 breast cancer cells, MDA-MB-231 breast cancer cells, or normal MCF-10A mammary epithelial cells at concentrations up to 100 μM after 48 h of incubation[1].
CYP4Z1-IN-3 (0.5-12.5 μM) concentration-dependently reduces expression of stemness markers ALDH1A1, SOX2, and Nanog in CYP4Z1-expressing MCF-7 and MDA-MB-231 breast cancer cells, but not in CYP4Z1-negative 4T1 cells[1].
CYP4Z1-IN-3 (0.5-12.5 μM) concentration-dependently reduces the CD44+/CD24 breast cancer stem cell subpopulation in CYP4Z1-expressing MCF-7 and MDA-MB-231 cells, but not in CYP4Z1-negative 4T1 cells[1].
CYP4Z1-IN-3 (0.5-12.5 μM) dose-dependently suppresses mammosphere formation in CYP4Z1-expressing MCF-7 and MDA-MB-231 breast cancer cells, but not in CYP4Z1-negative 4T1 cells[1].
CYP4Z1-IN-3 (0.5-12.5 μM; 24-48 h) concentration-dependently inhibits the migratory capacity of CYP4Z1-expressing MCF-7 and MDA-MB-231 breast cancer cells in wound healing assays[1].
CYP4Z1-IN-3 (0.5-12.5 μM; 24-48 h) inhibits the invasive capacity of CYP4Z1-expressing MCF-7 and MDA-MB-231 breast cancer cells in Transwell assays[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Cytotoxicity Assay[1]

Cell Line: MCF-7, MDA-MB-231, MCF-10A cells
Concentration: 0.01 μM; 0.1 μM; 1 μM; 10 μM; 100 μM
Incubation Time: 48 h
Result: Showed no significant cytotoxicity in MCF-7, MDA-MB-231, or normal MCF-10A cells at concentrations up to 100 μM.

Cell Migration Assay [1]

Cell Line: MCF-7, MDA-MB-231 breast cancer cells
Concentration: 0.5 μM; 2.5 μM; 12.5 μM
Incubation Time: 24 h; 48 h
Result: Suppressed the migratory capacity of MCF-7 and MDA-MB-231 cells in a concentration-dependent and significant manner.

Cell Invasion Assay[1]

Cell Line: MCF-7, MDA-MB-231 breast cancer cells
Concentration: 0.5 μM; 2.5 μM; 12.5 μM
Incubation Time: 24 h; 48 h
Result: Inhibited the invasive capacity of CYP4Z1-expressing MCF-7 and MDA-MB-231 breast cancer cells in Transwell assays
In Vivo

CYP4Z1-IN-3 (Compound C8) (100-800 mg/kg; p.o.; single dose) does not cause acute toxicity in BALB/c mice[1].
CYP4Z1-IN-3 (10 mg/kg; i.v.; every three days for three week) reduces the number of lung metastatic nodules in a breast cancer lung metastasis model in BALB/c-nude mice without causing significant organ toxicity[1].
CYP4Z1-IN-3 attenuates the tumor-initiating capacity and stemness of breast cancer cells in immunodeficient mice, reducing tumor formation rate, tumor weight, stem cell frequency, stemness marker expression, and proliferation while increasing apoptosis[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: BALB/c (SPF-grade; male and female)[1]
Dosage: 100 mg/kg; 200 mg/kg; 400 mg/kg; 800 mg/kg
Administration: p.o.; single dose
Result: Showed no significant changes in body weight over 7 days.
Showed no significant changes in general health indicators over 7 days.
Animal Model: Balb/c-nude (female; 4–6 weeks old; injected intravenously with 5 × 106 MDA-MB-231 cells to establish a breast cancer lung metastasis model)[1]
Dosage: 10 mg/kg
Administration: i.v.; every three days for three week
Result: Reduced the number of lung metastatic nodules.
Exhibited no significant organ toxicity.
Molecular Weight

322.40

Formula

C19H22N4O

CAS No.
SMILES

CCCCNC(CC1=CC=C(C=C1)CN2C=NC3=C2C=CN=C3)=O

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Purity & Documentation
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    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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CYP4Z1-IN-3
Cat. No.:
HY-183756
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