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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 Chemical Structure
CAS No. : 303094-67-9
| 规格 |
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是否有货 |
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| 100 mg |
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询价 |
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| 250 mg |
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询价 |
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| 500 mg |
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询价 |
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* Please select Quantity before adding items.
| 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].
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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].
上海金畔生物科技有限公司 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. |
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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].
上海金畔生物科技有限公司 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. |
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| 运输条件 |
Room temperature in continental US; may vary elsewhere.
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| 储存方式 |
Please store the product under the recommended conditions in the Certificate of Analysis.
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| 参考文献 |
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[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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