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

CYP4Z1-IN-1 (compound 7c) 是一种有效的 CYP4Z1 抑制剂,IC50 为 41.8 nM。 CYP4Z1-IN-1 在体外和体内以浓度依赖性方式降低乳腺癌症干细胞标记物的表达、球体形成和转移能力以及肿瘤启动能力。

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CYP4Z1-IN-1 Chemical Structure

CYP4Z1-IN-1 Chemical Structure

CAS No. : 2760611-38-7

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Customer Review

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

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)

细胞效力
(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]
体外研究
(In Vitro)

CYP4Z1-IN-1 (compound 7c) 显示出对乳腺 CSC (癌症干细胞)的抗增殖活性,IC50 为 483 ± 2.5 nM[1]
CYP4Z1-IN-1 (0.8-51.2 μM, 24 h) 抑制乳腺癌细胞中干细胞标记物 (P-gp,
Oct3/4, Nanog, ALDH1A1, 和 Sox2) 的表达[1]
CYP4Z1-IN-1 (0.8-51.2 μM, 24-48 h) 可减弱乳腺癌细胞的迁移和侵袭能力[1]

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.
体内研究
(In Vivo)

CYP4Z1-IN-1 (compound 7c) (2000 mg/kg,口服,连续 7 天)对小鼠没有明显的毒性和体重减轻[1]
CYP4Z1-IN-1 (12.8 μM, 72 h处理MCF-7 and MDA-MB-231 cells,然后细胞皮下植入小鼠腹股沟乳腺) 可阻断乳腺癌细胞的肿瘤启动能力[1]

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

Formula

C13H18N2O3

CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

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

纯度 & 产品资料
参考文献
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  • 稀释计算器

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Help & FAQs
  • Do most proteins show cross-species activity?

    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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产品名称:
CYP4Z1-IN-1
目录号:
HY-152159
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