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

CYP4Z1-IN-1 (compound 7c) is a potent CYP4Z1 inhibitor, with an IC50 of 41.8 nM. CYP4Z1-IN-1 decreases the expression of breast CSCs stemness markers, spheroid formation, and metastatic ability as well as tumor-initiation capability in a concentration-dependent manner in vitro and in vivo.

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CYP4Z1-IN-1

CYP4Z1-IN-1 構造式

CAS 番号 : 2760611-38-7

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製品説明

CYP4Z1-IN-1 (compound 7c) is a potent CYP4Z1 inhibitor, with an IC50 of 41.8 nM. CYP4Z1-IN-1 decreases the expression of breast CSCs stemness markers, spheroid formation, and metastatic ability as well as tumor-initiation capability in a concentration-dependent manner in vitro and in vivo[1].

IC50 & Target

CYP4Z1

41.8 ± 1.4 nM (IC50)

CYP4F11

291.3 ± 46 nM (IC50)

CYP4F12

1598.3 ± 5 nM (IC50)

CYP2D6

>10 000 nM (IC50)

CYP2C9

>10 000 nM (IC50)

CYP3A4

>10 000 nM (IC50)

Cellular Effect
Cell Line Type Value Description References
MCF7 IC50
483 nM
Compound: 7c
Antiproliferative activity against human MCF7 cells assessed as cell growth inhibition incubated for 72 hrs by MTT assay
Antiproliferative activity against human MCF7 cells assessed as cell growth inhibition incubated for 72 hrs by MTT assay
[PMID: 36414390]
MDA-MB-231 IC50
483 nM
Compound: 7c
Antiproliferative activity against human MDA-MB-231 cells assessed as cell growth inhibition incubated for 72 hrs by MTT assay
Antiproliferative activity against human MDA-MB-231 cells assessed as cell growth inhibition incubated for 72 hrs by MTT assay
[PMID: 36414390]
体外実験

CYP4Z1-IN-1 (compound 7c) shows antiproliferative activity against breast CSCs (cancer stem cells), with an IC50 of 483 ± 2.5 nM[1].
CYP4Z1-IN-1 (0.8-51.2 μM, 24 h) suppresses the expression of stemness markers (P-gp, Oct3/4, Nanog, ALDH1A1, and Sox2) in breast cancer cells[1].
CYP4Z1-IN-1 (0.8-51.2 μM, 24-48 h) attenuates the migration and invasion ability of breast cancer cells[1].

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

Western Blot Analysis[1]

Cell Line: MCF-7 and MDA-MB-231 cells
Concentration: 0.8 μM, 3.2 μM, 12.8 μM, 51.2 μM
Incubation Time: 24 h
Result: Significantly suppressed the protein expression of stemness markers (P-gp, Oct3/4, Nanog, ALDH1A1, and Sox2) in MCF-7 cells in a concentration-dependent manner.
体内実験

CYP4Z1-IN-1 (compound 7c) (2000 mg/kg, orally, for 7 days) shows no evident toxicity and body weight loss in mice[1].
CYP4Z1-IN-1 (MCF-7 and MDA-MB-231 cells (12.8 μM, 72 h) implanted in the inguinal mammary gland of mice subcutaneously) blocks the tumor-initiating ability of breast cancer cells[1].

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

Animal Model: Mice[1]
Dosage: 2000 mg/kg
Administration: orally, for 7 days
Result: Showed that compound 7c was rather safe; no evident toxicity and body weight loss were observed.
Animal Model: BALB/c-nude mice (3-4 week old, female)[1]
Dosage: 12.8 μM
Administration: MCF-7 and MDA-MB-231 cells were pre-treated with 7c (12.8 μM) for 72 h and were then implanted in the inguinal mammary gland of mice subcutaneously
Result: Blocked the tumor-initiating ability of breast cancer cells.
分子量

250.29

分子式

C13H18N2O3

CAS 番号
SMILES

O=C(CCCC1=CC=C(C=C1)N/C=N/O)OCC

輸送条件

Room temperature in continental US; may vary elsewhere.

保管条件

Please store the product under the recommended conditions in the Certificate of Analysis.

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参考文献
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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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製品名:
CYP4Z1-IN-1
製品番号:
HY-152159
数量:
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