ZINC69391_product_DataBase

Bioactivity

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].

Invitro

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:

In Vivo

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

Name

ZINC69391

CAS

303094-67-9

Formula

C14H14F3N5

Molar Mass

309.29

Appearance

Solid

Transport

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Reference

[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.

PeptideDB

ZINC69391

CAS: 303094-67-9 F: C14H14F3N5 W: 309.29