ZINC69391

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。

ZINC69391 

ZINC69391 是一种特异的 Rac1 抑制剂,通过在 Rac1 表面掩蔽 Trp56 残基来干扰 Rac1-GEF 的相互作用。ZINC69391 干扰 Rac1 与 Dock180 的相互作用,降低 Rac1-GTP水平。ZINC69391 诱导细胞凋亡,具有抗增殖和抗转移作用。

ZINC69391

ZINC69391 Chemical Structure

CAS No. : 303094-67-9

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生物活性

ZINC69391, a specific Rac1 inhibitor, interferes with Rac1-GEF interaction by masking Trp56 residue on Rac1 surface. ZINC69391 interferes with the interaction of Rac1 with Dock180 and reduces Rac1-GTP levels. ZINC69391 induces apoptosis, and shows antiproliferative and antimetastatic effects[1][2][3].

体外研究
(In Vitro)

ZINC69391 inhibits growth of U937, HL-60, KG1A and Jurkat cells with IC50s ranging from 41 to 54 μM[1].
ZINC69391 (50-100 μM; 24 hours) augments the enzymatic activity of caspase 3 in a concentration dependent manner[1].
ZINC69391 (0-125 μM; 72h) reduces cell proliferation of human glioma cells[2].
ZINC69391 (50-100 μM; 48 hours) triggers cell cycle arrest[2].
ZINC69391 (50 μM; 24 hours) triggers apoptosis on human acute leukemic cells[1].

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

Cell Proliferation Assay[2]

Cell Line: U-87 MG, LN229 cells
Concentration: 0-125μM
Incubation Time: 72 hours
Result: Reduced cell proliferation in a concentration-dependent manner.

Cell Cycle Analysis[2]

Cell Line: LN229 cells
Concentration: 50, 100 μM
Incubation Time: 48 hours
Result: Resulted in a significant increased percentage of cells in the sub-G0/G1 phase in a concentration dependent manner.

Apoptosis Analysis[1]

Cell Line: HL-60, U937 and KG1A cell lines
Concentration: 50 μM
Incubation Time: 24 hours
Result: Led to a significant increase in apoptotic cells.

体内研究
(In Vivo)

ZINC69391 (25 mg/kg; i.p; daily for 21 days) impairs metastatic lung colonization in a syngeneic animal model[3].

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

Animal Model: Specific pathogen-free female BALB/c inbred mice (bearing F3II cells)[3]
Dosage: 25 mg/kg body weight
Administration: I.p; daily for 21 days
Result: Significantly reduced by about 60% the formation of total metastatic lung colonies.

分子量

309.29

Formula

C14H14F3N5

CAS 号

303094-67-9

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]. Cabrera M, et al. Pharmacological Rac1 inhibitors with selective apoptotic activity in human acute leukemic cell lines. Oncotarget. 2017;8(58):98509‐98523. Published 2017 Oct 4.

    [2]. Cardama GA, et al. Proapoptotic and antiinvasive activity of Rac1 small molecule inhibitors on malignant glioma cells. Onco Targets Ther. 2014;7:2021‐2033. Published 2014 Oct 30.

    [3]. Cardama GA, et al. Preclinical development of novel Rac1-GEF signaling inhibitors using a rational design approach in highly aggressive breast cancer cell lines. Anticancer Agents Med Chem. 2014;14(6):840‐851.

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