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
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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 (compound #1) (1-50 µM; 2 h) dose-dependently inhibits EGF (HY-P7109)-stimulated Rac1 activation in CD18/HPAF cells, with an EC50 of 8.3 µM[1].
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 (0.001-100 µM; 1 h) dose-dependently blocks the binding of Rac1-GTP to the downstream effector protein PAK1, with an IC50 of 95 nM[1].
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. Further protocols information, click here.
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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.
Protocols
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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)