Description: Selective inhibitor of Rac1-GEF interaction; antioncogenic
Chemical Name:N6-[2-[[4-(Diethylamino)-1-methylbutyl]amino]-6-methyl-4-pyrimidinyl]-2-methyl-4,6-quinolinediamine trihydrochloride
Purity: ≥99% (HPLC)
Biological Activity
Technical Data
Solubility
Calculators
Datasheets
References
Biological Activity
Selective inhibitor of Rac1-GEF interaction. Prevents Rac1 activation by Rac-specific guanine nucleotide exchange factors (GEFs) TrioN and Tiam1 (IC50 ~ 50 μM) without affecting Cdc42 or RhoA activation. Inhibits Rac1-mediated cell functions and is reported to reverse tumor cell phenotyes in prostate cancer cells.
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The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.
Solubility Data
Solvent
Max Conc. mg/mL
Max Conc. mM
Solubility
DMSO
53.1
100
water
53.1
100
Preparing Stock Solutions
The following data is based on the product molecular weight 530.97. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.
Concentration / Solvent Volume / Mass
1 mg
5 mg
10 mg
1 mM
1.88 mL
9.42 mL
18.83 mL
5 mM
0.38 mL
1.88 mL
3.77 mL
10 mM
0.19 mL
0.94 mL
1.88 mL
50 mM
0.04 mL
0.19 mL
0.38 mL
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Product Datasheets
Certificate of Analysis / Product Datasheet
Safety Datasheet
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References
References are publications that support the products' biological activity.
Gaoet al (2004) Rational design and characterization of a Rac GTPase-specific small molecule inhibitor. Proc.Natl.Acad.Sci.USA 101 7618 PMID: