MPT0B392

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上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

MPT0B392 

MPT0B392 是一种口服活性的喹啉衍生物，作用于 c-Jun N末端激酶 (JNK) 和 apoptosis 的激活剂。MPT0B392 抑制微管蛋白聚合，通过激活 JNK 诱导细胞有丝分裂停滞，线粒体膜电位丧失和 caspases 裂解，最终导致细胞凋亡。MPT0B392 是一种新型微管解聚剂，可增强西罗莫司对耐药急性白血病细胞和多药耐药细胞系的细胞毒性。

MPT0B392

MPT0B392 Chemical Structure

CAS No. : 1346169-92-3

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生物活性

MPT0B392, an orally active quinoline derivative, induces c-Jun N-terminal kinase (JNK) activation, leading to apoptosis. MPT0B392 inhibits tubulin polymerization and triggers induction of the mitotic arrest, followed by mitochondrial membrane potential loss and caspases cleavage by activation of JNK and ultimately leads to apoptosis. MPT0B392 is demonstrated to be a novel microtubule-depolymerizing agent and enhances the cytotoxicity of sirolimus in sirolimus-resistant acute leukemic cells and the multidrug resistant cell line[1].

IC50 & Target[1]

JNK

 

Caspase

 

体外研究
(In Vitro)

MPT0B392 (B392) (0.001-0.1 μM; 24 and 48 hours) inhibits the cell viability of HL60, MOLT-4, and CCRF-CEM cells with IC50s of 0.02 μM, 0.03 μM and 0.02 μM, respectively[1].
MPT0B392 (0.1 μM; 48 hours) induces apoptosis in HL60 cancer cells[1].
MPT0B392 (0.1 μM for 6-48 hours; 0.01-0.1 μM for 24 and 48 hours) triggers cells arrest in the G2/M phase, followed by accumulation in subG1 phase in a concentration and time-dependent manner[1].
MPT0B392 (0.1 μM; 48 hours) increases the phosphorylation of Bcl-2, Mcl-1S and decreases in Mcl-1L[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay[1]

Cell Line: HL60 (acute promyelocytic leukemia), MOLT-4 (acute lymphoblastic leukemia), CCRF-CEM (acute lymphoblastic leukemia) cells
Concentration: 0.001, 0.003, 0.01, 0.03, 0.1 μM
Incubation Time: 24 and 48 hours
Result: Inhibited the cell viability.

Apoptosis Analysis[1]

Cell Line: HL60 cells
Concentration: 0.1 μM
Incubation Time: 48 hours
Result: Induced apoptosis in cancer cells.

Cell Cycle Analysis[1]

Cell Line: HL60 cells
Concentration: 0.1 μM or 0.01, 0.03, 0.1 μM
Incubation Time: 0.1 μM for 6-48 hours; 0.01-0.1 μM for 24 and 48 hours
Result: Triggered cells arrest in the G2/M phase, followed by accumulation in subG1 phase in a concentration and time-dependent manner.

Western Blot Analysis[1]

Cell Line: HL60 cells
Concentration: 0.1 μM
Incubation Time: 48 hours
Result: Increased the phosphorylation of Bcl-2, Mcl-1S and decreased in Mcl-1L.

体内研究
(In Vivo)

The effects of MPT0B392 (oral gavage; 50 mg/kg or 100 mg/kg for 12 or 14 days) shows relative potent anti-leukemia activity in a vivo xenograft model[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Severe combined immunodeficient (SCID) mice [1]
Dosage: 50 mg/kg or 100 mg/kg
Administration: Oral gavage; 12 or 14 days
Result: Resulted in significant tumor growth delay (83.3%) and tumor volume inhibition without loss of body weight.

分子量

404.44

Formula

C19H20N2O6S
CAS 号

1346169-92-3
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.
参考文献

  • [1]. Chao MW, et al. An oral quinoline derivative, MPT0B392, causes leukemic cells mitotic arrest and overcomes drug resistant cancer cells. Oncotarget. 2017 Apr,8(17):27772-27785.

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