Rac1-IN-1
Rac1-IN-1 is a potent Rac1 inhibitor with an IC50 of 95 nM and a Ki of 6.8 μM. Rac1-IN-1 blocks the binding of Rac1 to downstream PAK1 by targeting the nucleotide-binding site of Rac1, thereby specifically inhibiting Rac1 activation without affecting Cdc42/RhoA. Rac1-IN-1 can be used for research on pancreatic cancer.
For research use only. We do not sell to patients.
- CAS No.: 627042-19-7
- Formula: C19H14N2O5
- Molecular Weight:350.32
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biological Activity
Description
IC50 & Target
[1]|
Rac1 95 nM (IC50) |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| ASPC1 | EC50 |
19.1 μM
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Reduction of viability in human AsPC-1 pancreatic cancer cells after 7 days incubation by PrestoBlue assay.
Reduction of viability in human AsPC-1 pancreatic cancer cells after 7 days incubation by PrestoBlue assay.
|
28410221 |
| CAPAN-1 | EC50 |
21.7 μM
|
Reduction of viability in human Capan1 pancreatic cancer cells after 7 days incubation by PrestoBlue assay.
Reduction of viability in human Capan1 pancreatic cancer cells after 7 days incubation by PrestoBlue assay.
|
28410221 |
In Vitro
Rac1-IN-1 (25 µM; 24-120 h) inhibits the proliferation of Capan1, CD18/HPAF, and AsPC-1 pancreatic cancer cells[1].
Rac1-IN-1 (1-75 µM; 24-48 h) inhibits the migration and invasion of Capan1 and CD18/HPAF cells[1].
Rac1-IN-1 (1.6-100 µM; 7 days) reduced the viability of AsPC-1, Capan1, and CD18/HPAF pancreatic cancer cells with EC50 values of 19.1, 21.7, and 22.5 µM, respectively, without affecting HPNE normal pancreatic ductal cells[1].
Rac1-IN-1 (25-50 μM; 7 days) reduces cell colony formation in Capan1 cells.
Rac1-IN-1 (0.1-1000 µM; 1 h) dose-dependently displaced the nucleotide mant-GDP bound to Rac1 in an in vitro fluorescence polarization assay, with a Ki of 6.8 μM[1].
Rac1-IN-1 (50 µM; 2 h) selectively inhibits Rac1 activity, but not Cdc42 and RhoA, in CD18/HPAF cells[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 cells
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Concentration:50 µM
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Incubation Time:2 h
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Result:Inhibited Rac1 activity significantly.
Did not inhibit Cdc42 or RhoA activity.
Did not affect steady-state protein levels of Rac1, Cdc42, or RhoA.
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Cell Line:Capan1, CD18/HPAF cells
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Concentration:25 µM
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Incubation Time:24, 72, 120 h
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Result:Significantly inhibited the exponential proliferation of these pancreatic cancer cells over time.
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Cell Line:Capan1, CD18/HPAF cells
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Concentration:1, 10, 50, 75 μM
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Incubation Time:24 h, 48 h
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Result:Reduced the migration (wound closure) of pancreatic cancer cells in a dose-dependent manner, with >80% reduction observed at 75 μM in Capan1 cells at 48 h.
Chemical Information
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CAS No. 627042-19-7
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Molecular Weight 350.32
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Formula C19H14N2O5
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SMILES
O=C(C1=CC=C(C2=CC([N+]([O-])=O)=CC=C2)O1)NC3=CC=CC(C(C)=O)=C3
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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)