2. Apoptosis Stem Cell/Wnt
  3. Apoptosis Caspase β-catenin
  4. XIAP-CASP7 PPI-IN-1

XIAP-CASP7 PPI-IN-1 是一种可逆的XIAP: CASP7 抑制剂，能够特异性地破坏 XIAP 与 CASP7 的相互作用。XIAP-CASP7 PPI-IN-1 选择性诱导 MCF-7 和 caspase-3 低表达 (CASP3/DR) 三阴性乳腺癌细胞凋亡(apoptosis)。XIAP-CASP7 PPI-IN-1 通过下调 Paclitaxel (HY-B0015) 耐药的 MCF-7 细胞中的 β-连环蛋白及其相关的 ABC 转运蛋白，克服了化疗耐药性。XIAP-CASP7 PPI-IN-1 可用于研究乳腺癌。

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XIAP-CASP7 PPI-IN-1

XIAP-CASP7 PPI-IN-1 Chemical Structure

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XIAP-CASP7 PPI-IN-1 相关抗体

Top Publications Citing Use of Products

查看 Caspase 亚型特异性产品:

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Caspase 1 Caspase 2 Caspase 3 Caspase 4 Caspase 5 Caspase 6 Caspase 7 Caspase 8 Caspase 9 Caspase 10 Caspase 12 Caspase Caspase 11 Caspase-13

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Xiap-casp7 PPI-IN-1 is a reversible XIAP: CASP7 inhibitor with specifically disrupting the interaction between XIAP and CASP7. XIAP-CASP7 PPI-IN-1 selectively induce MCF-7 and other caspase-3 down-regulation (CASP3/DR) triple-negative breast cancer cell apoptosis. XIAP-CASP7 PPI-IN-1 overcomes chemoresistance via down-regulating β-catenin and its associated ABC transporters in Paclitaxel (HY-B0015)-resistant MCF-7 cells. XIAP-CASP7 PPI-IN-1 can be used for the study of breast cancer[1].

IC50 & Target[1]

Caspase-3

 

Caspase-7

 

Caspase-9

 

体外研究
(In Vitro)

XIAP-CASP7 PPI-IN-1 (Compound 643943) (0-50 μM, 4-24 h) 对 MCF-7 表现出最大细胞毒性作用，而这种毒性作用是通过凋亡信号介导的[1]。
XIAP-CASP7 PPI-IN-1 (0-0.5 nM μM, 24 h) 通过 Asp93 与 CASP7 结合，并从 XIAP: 释放活性 CASP7，从而诱导细胞死亡[1]。
XIAP-CASP7 PPI-IN-1 (1.25-5 μM μM, 24 h) 与抗癌药物具有协同作用，能有效使对 Paclitaxel 耐药的MCF-7细胞 (7TR) 对化疗敏感[1]。

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

XIAP-CASP7 PPI-IN-1 相关抗体:

Cell Cycle Analysis[1]

Cell Line: Paclitaxel-resistant MCF-7 cells (7TR)
Concentration: 1.25, 2.5 and 5 μM alone or with Staurosporine (STS) (HY-15141) and Doxorubicin (HY-15142A)
Incubation Time: 24 h
Result: Synergistically potentiated paclitaxel-induced G2M arrest and induced cell death.

Western Blot Analysis[1]

Cell Line: MCF-7
Concentration: 20 μM
Incubation Time: 24 h
Result: Detected CASP7 activity only, and no activation of CASP3.

Cell Cytotoxicity Assay[1]

Cell Line: MCF-7 cells
Concentration: 3.125, 6.25, 12.5, 25, 50 and 100 μM
Incubation Time: 24 h
Result: Exhibited the greatest cytotoxic effect on MCF-7 cells, with an EC50 of 8.48 μM.
Did not kill the normal breast MCF-10A cells at 100 μM.
Exhibited the EC50 values against BT-483, MDA-MB-468 and ZR-75-1 to be 4.1, 5.2, and 6.7 μM, respectively.

Western Blot Analysis[1]

Cell Line: paclitaxel-resistant MCF-7 cells (7TR)
Concentration: 1.25, 2.5 and 5 μM alone or with STS and Doxorubicin
Incubation Time: 24 h
Result: Decreased the level of cleaved β-catenin and certain ABC transporter.
体内研究
(In Vivo)

XIAP-CASP7 PPI-IN-1 (Compound 643943) (20 mg/kg, i.p., 1 天 1 次, 共 2 周) 在乳腺癌小鼠模型中具有抗肿瘤活性[1]。

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

Animal Model: MCF-7 and MDA-MB-468 induced xenograft model established in NOD/SCID mice[1]
Dosage: 20 mg/kg
Administration: Intraperitoneal injection (i.p.), once daily for 2 weeks
Result: Led to a significant reduced tumor volume and induced an increase for apoptosis in tumor tissues.
分子量

411.45

Formula

C25H21N3O3
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

XIAP-CASP7 PPI-IN-1 相关分类

  • 摩尔计算器

  • 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.

Keywords:

XIAP-CASP7 PPI-IN-1ApoptosisCaspaseβ-cateninBeta cateninQuinazolineCancer cellVEGFR2MCF-7 cellsInhibitorinhibitorinhibit

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