Rac1-IN-2
Rac1-IN-2 is a small-molecule Rac1 inhibitor. Rac1-IN-2 inhibits Rac1-mediated signaling by blocking the binding of active Rac1 to PAK1 (IC50 = 88 nM), exhibits selectivity for Rac1 over Cdc42 and RhoA, and suppresses the proliferation, migration, clonogenicity, and viability of pancreatic cancer cells. Rac1-IN-2 can be used for research on pancreatic cancer.
For research use only. We do not sell to patients.
- CAS No.: 701223-06-5
- Formula: C23H20N2O2S
- Molecular Weight:388.49
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biological Activity
Description
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HPAF-II | EC50 |
22.4 μM
|
Inhibition of EGF-induced Rac1 activation in human CD18/HPAF pancreatic cancer cells assessed by PAK1 pull-down after 2 hrs incubation.
Inhibition of EGF-induced Rac1 activation in human CD18/HPAF pancreatic cancer cells assessed by PAK1 pull-down after 2 hrs incubation.
|
28410221 |
| ASPC1 | EC50 |
14.7 μM
|
Viability reduction against human AsPC-1 pancreatic cancer cells measured by PrestoBlue assay after 7 days incubation.
Viability reduction against human AsPC-1 pancreatic cancer cells measured by PrestoBlue assay after 7 days incubation.
|
28410221 |
| CAPAN-1 | EC50 |
24.2 μM
|
Viability reduction against human Capan1 pancreatic cancer cells measured by PrestoBlue assay after 7 days incubation.
Viability reduction against human Capan1 pancreatic cancer cells measured by PrestoBlue assay after 7 days incubation.
|
28410221 |
| HPAF-II | EC50 |
23.5 μM
|
Viability reduction against human CD18/HPAF pancreatic cancer cells measured by PrestoBlue assay after 7 days incubation.
Viability reduction against human CD18/HPAF pancreatic cancer cells measured by PrestoBlue assay after 7 days incubation.
|
28410221 |
In Vitro
Rac1-IN-2 (compound #6) (10 μM; 2 h) inhibits Rac1 activity in CD18/HPAF cells[1].
Rac1-IN-2 (1-50 μM; 2 h) inhibits EGF-induced Rac1 activation in CD18/HPAF cells with an EC50 of 22.4 μM[1].
Rac1-IN-2 (50 μM; 2 h) selectively inhibits Rac1 activity in CD18/HPAF cells without inhibiting Cdc42 or RhoA[1].
Rac1-IN-2 (25 μM; 24-120 h) inhibits the proliferation of Capan1 and CD18/HPAF cells[1].
Rac1-IN-2 (50 μM; 24-48 h) inhibits the migration of Capan1 and CD18/HPAF cells, with maximal wound closure inhibition of approximately 60% and 40%, respectively[1].
Rac1-IN-2 (50 μM; 1 h pre-incubation; 24 h migration) inhibits transwell migration of Capan1 and CD18/HPAF cells[1].
Rac1-IN-2 (7 days) reduces clonogenic survival of Capan1 cells, with little effect on HPNE normal pancreatic ductal cells[1].
Rac1-IN-2 (1.6-100 μM; 7 days) reduces the viability of AsPC-1, Capan1, and CD18/HPAF cells with EC50 values of 14.7, 24.2, and 23.5 μM, respectively[1].
Rac1-IN-2 (0.001-100 μM; 1 h) disrupts Rac1-PAK1 complex formation with an IC50 of 88 nM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:CD18/HPAF pancreatic cancer cells
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Concentration:10 μM
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Incubation Time:2 h
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Result:Inhibited Rac1 activity in CD18/HPAF cells.
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Cell Line:CD18/HPAF pancreatic cancer cells
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Concentration:50 μM
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Incubation Time:2 h
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Result:Inhibited Rac1 activity without inhibiting Cdc42 or RhoA activity.
Did not affect steady-state protein levels of Rac1, Cdc42, or RhoA.
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Cell Line:Capan1 and CD18/HPAF pancreatic cancer cells
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Concentration:25 μM
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Incubation Time:24, 72, and 120 h
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Result:Inhibited proliferation of Capan1 and CD18/HPAF cells.
Showed only a marginal decrease in CD18/HPAF cells at day 3.
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Cell Line:Capan1 and CD18/HPAF pancreatic cancer cells
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Concentration:50 μM
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Incubation Time:24, 48 h
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Result:Reduced migration of Capan1 and CD18/HPAF cells.
Inhibited wound closure by approximately 60% at 48 h.
Showed dose-dependent inhibition with maximum inhibition of ~60% in Capan1 cells and ~40% in CD18/HPAF cells.
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Cell Line:Capan1 and CD18/HPAF pancreatic cancer cells
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Concentration:50 μM
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Incubation Time:1 h pre-incubation; 24 h migration
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Result:Inhibited migration of both Capan1 and CD18/HPAF cells through the transwell barrier.
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Cell Line:AsPC-1, Capan1, and CD18/HPAF pancreatic cancer cells
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Concentration:1.6, 3.1, 6.3, 12.5, 25, 50, 100 μM
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Incubation Time:7 days at 37°C; 5 days
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Result:Reduced viability dose-dependently in all cell lines, with ~75% inhibition at 50 μM.
Reduced viability with EC50 values of 14.7 μM (AsPC-1), 24.2 μM (Capan1), and 23.5 μM (CD18/HPAF).
Chemical Information
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CAS No. 701223-06-5
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Molecular Weight 388.49
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Formula C23H20N2O2S
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SMILES
O=C(C=1SC=CC1)C2=CN(C=3C=CC=CC23)CC(=O)NC=4C=C(C=C(C4)C)C
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)