1. Metabolic Enzyme/Protease NF-κB Apoptosis
  2. MALT1 Apoptosis
  3. MALT1-IN-13

MALT1-IN-13 (compound 10m) 是一种黏膜相关淋巴瘤转运蛋白 (MALT1)抑制剂,与 MALT1 蛋白酶共价且不可逆地结合抑制 MALT1 活性,IC50 为 1.7 μM。MALT1-IN-13 抑制 ABC-DLBCL 的增殖并诱导 ABC-DLBCL HBL1 的细胞凋亡 (apoptosis)。MALT1-IN-13 调节 mTOR 和 PI3K-Akt 通路。

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MALT1-IN-13 Chemical Structure

MALT1-IN-13 Chemical Structure

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Customer Review

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

MALT1-IN-13 (compound 10m) is inhibitor for mucosa-associated lymphoid tissue lymphoma translocation protein 1 (MALT1), which to binds MALT1 protease covalently and irreversibly, inhibits MALT1 with the IC50 of 1.7 μM. MALT1-IN-13 inhibits proliferation against ABC-DLBCL and induces apoptosis in ABC-DLBCL HBL1. MALT1-IN-13 regulates mTOR and PI3K-Akt pathways[1].

IC50 & Target

IC50: 1.7 μM (MALT1)

体外研究
(In Vitro)

MALT1-IN-13 (0-10 μM) 诱导 HBL1 细胞凋亡,抑制 ABC-DLBCL HBL1、TMD8 和 GCB-DLBCL OCI-LY1 细胞的增殖,GI50 分别为 1.5,0.7 和 >25 μM[1]
MALT1-IN-13 (0-10 μM) 下调 MALT1 和 NF-kB 通路的表达,上调 mTOR 和 PI3K-Akt 通路的表达,在 HBL1 细胞中发挥抗肿瘤作用[1]

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

Apoptosis Analysis[1]

Cell Line: ABC-DLBCL HBL1
Concentration: 0-10 μM
Incubation Time: 24 h
Result: Induced over 70% apoptosis in HBL1 cells with concentration of 5 μM.

Cell Proliferation Assay[1]

Cell Line: ABC-DLBCL HBL1, ABC-DLBCL TMD8 and GCB-DLBCL OCI-LY1
Concentration: 100 μM
Incubation Time: 72 h
Result: Inhibits proliferations of ABC-DLBCL HBL1, TMD8 and GCB-DLBCL OCI-LY1.

Apoptosis Analysis[1]

Cell Line: ABC-DLBCL HBL1 and ABC-DLBCL TMD8
Concentration: 0-10 μM
Incubation Time: 24 h
Result: Increased levels of cleaved PARP1 and caspase3. Decreased levels of IkBα and phosphorylated IkBα.
体内研究
(In Vivo)

MALT1-IN-13 (25 mg/kg,腹腔注射,12-14 天) 表现出具有 MALT1 蛋白酶特异性的抗肿瘤活性,抑制 HBL1/TMD8 异种移植 NCG 小鼠中的肿瘤生长[1]

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

Animal Model: HBL1/TMD8/OCI-LY1 xenografted NCG mice[1]
Dosage: 25 mg/kg
Administration: i.p., 12 days for HBL1 bearing NCG mice, 14 days for TMD8 bearing mice, 19 days for OCI-LY1 bearing mice
Result: Suppressed the HBL1 tumor growth and decreased the tumor weight with TGI of 55.9%.
Suppressed the TMD8 tumor growth and decreased the tumor weight with TGI of 69.9%.
分子量

524.84

Formula

C20H15BrClN3O3S2

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
  • 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.

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产品名称:
MALT1-IN-13
目录号:
HY-162268
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