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303094-67-9

303094-67-9 structure
303094-67-9 structure
  • Name: ZINC69391
  • Chemical Name: ZINC69391
  • CAS Number: 303094-67-9
  • Molecular Formula: C14H14F3N5
  • Molecular Weight: 309.29
  • Catalog: Signaling Pathways Apoptosis Apoptosis
  • Create Date: 2020-08-07 20:19:00
  • Modify Date: 2024-01-17 16:12:20
  • 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].

Name ZINC69391
Description 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].
Related Catalog
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]. 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.
In Vivo ZINC69391 (25 mg/kg; i.p; daily for 21 days) impairs metastatic lung colonization in a syngeneic animal model[3]. 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.
References

[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.

Molecular Formula C14H14F3N5
Molecular Weight 309.29
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