| Bioactivity | 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]. |
| Target | IC50: 1.7 μM (MALT1) |
| Invitro | 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. 0 --> MALT1-IN-13 相关抗体: Apoptosis Analysis[1] Cell Line: |
| 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: |
| Formula | C20H15BrClN3O3S2 |
| Molar Mass | 524.84 |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
| Reference | [1]. Liang X, et al., Development of Potent MALT1 Inhibitors Featuring a Novel "2-Thioxo-2,3-dihydrothiazolo[4,5-d]pyrimidin-7(6H)-one" Scaffold for the Treatment of B Cell Lymphoma. J Med Chem. 2024 Feb 22;67(4):2884-2906. [2]. Liang X, et al., Development of Potent MALT1 Inhibitors Featuring a Novel "2-Thioxo-2,3-dihydrothiazolo[4,5-d]pyrimidin-7(6H)-one" Scaffold for the Treatment of B Cell Lymphoma. J Med Chem. 2024 Feb 22;67(4):2884-2906. |