1. GPCR/G Protein
    Apoptosis
  2. Ras
    Apoptosis
  3. ZINC69391

ZINC69391 

Cat. No.: HY-102078
Handling Instructions

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.

For research use only. We do not sell to patients.

ZINC69391 Chemical Structure

ZINC69391 Chemical Structure

CAS No. : 303094-67-9

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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].

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.
Molecular Weight

309.29

Formula

C₁₄H₁₄F₃N₅

CAS No.

303094-67-9

SMILES

N=C(NC1=CC=CC=C1C(F)(F)F)NC2=NC(C)=CC(C)=N2

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Keywords:

ZINC69391ZINC 69391ZINC-69391RasApoptosisRac1-GEFinteractionDock180Rac1-GTPantiproliferativeantimetastaticacuteleukemiccellsmalignantgliomaInhibitorinhibitorinhibit

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ZINC69391
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HY-102078
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