1. GPCR/G Protein MAPK/ERK Pathway Apoptosis
  2. Ras Apoptosis
  3. ZINC69391

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.

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ZINC69391 Chemical Structure

ZINC69391 Chemical Structure

CAS No. : 303094-67-9

Size Price Stock Quantity
Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
USD 286 In-stock
Solution
10 mM * 1 mL in DMSO USD 286 In-stock
Solid
5 mg USD 260 In-stock
10 mg USD 420 In-stock
25 mg USD 840 In-stock
50 mg USD 1300 In-stock
100 mg USD 2080 In-stock
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Based on 1 publication(s) in Google Scholar

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1 Publications Citing Use of MCE ZINC69391

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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].

MedChemExpress (MCE) 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.
In Vivo

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

MedChemExpress (MCE) 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.
Molecular Weight

309.29

Formula

C14H14F3N5

CAS No.
Appearance

Solid

Color

White to off-white

SMILES

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

Shipping

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
Solvent & Solubility
In Vitro: 

DMSO : 25 mg/mL (80.83 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.2332 mL 16.1661 mL 32.3321 mL
5 mM 0.6466 mL 3.2332 mL 6.4664 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 3.2332 mL 16.1661 mL 32.3321 mL 80.8303 mL
5 mM 0.6466 mL 3.2332 mL 6.4664 mL 16.1661 mL
10 mM 0.3233 mL 1.6166 mL 3.2332 mL 8.0830 mL
15 mM 0.2155 mL 1.0777 mL 2.1555 mL 5.3887 mL
20 mM 0.1617 mL 0.8083 mL 1.6166 mL 4.0415 mL
25 mM 0.1293 mL 0.6466 mL 1.2933 mL 3.2332 mL
30 mM 0.1078 mL 0.5389 mL 1.0777 mL 2.6943 mL
40 mM 0.0808 mL 0.4042 mL 0.8083 mL 2.0208 mL
50 mM 0.0647 mL 0.3233 mL 0.6466 mL 1.6166 mL
60 mM 0.0539 mL 0.2694 mL 0.5389 mL 1.3472 mL
80 mM 0.0404 mL 0.2021 mL 0.4042 mL 1.0104 mL
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ZINC69391 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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ZINC69391
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