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

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)

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
HBL1 GI50
0.69 μM
Compound: 10m
Synergistic antitumor activity against human HBL1 cells assessed as cell growth inhibition incubated for 72 hrs in presence of rapamycin by Cell Titer Glo assay
Synergistic antitumor activity against human HBL1 cells assessed as cell growth inhibition incubated for 72 hrs in presence of rapamycin by Cell Titer Glo assay
[PMID: 38349664]
HBL1 GI50
1.5 μM
Compound: 10m
Antiproliferative activity against human HBL1 cells assessed as cell growth inhibition incubated for 72 hrs by Cell Titer Glo assay
Antiproliferative activity against human HBL1 cells assessed as cell growth inhibition incubated for 72 hrs by Cell Titer Glo assay
[PMID: 38349664]
OCI-Ly1 GI50
> 25 μM
Compound: 10m
Antiproliferative activity against human OCI-Ly1 cells assessed as cell growth inhibition incubated for 72 hrs by Cell Titer Glo assay
Antiproliferative activity against human OCI-Ly1 cells assessed as cell growth inhibition incubated for 72 hrs by Cell Titer Glo assay
[PMID: 38349664]
TMD8 GI50
0.7 μM
Compound: 10m
Antiproliferative activity against human TMD8 cells assessed as cell growth inhibition incubated for 72 hrs by Cell Titer Glo assay
Antiproliferative activity against human TMD8 cells assessed as cell growth inhibition incubated for 72 hrs by Cell Titer Glo assay
[PMID: 38349664]
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
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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:
MALT1-IN-13
目录号:
HY-162268
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