An inhibitor of the Rho GEF 12-RhoA protein-protein interaction
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Product Categories

Product Type

Biochemicals

Research Area

Cancer
Cell Migration & Metastasis

Y16

Item No. 42399

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
4-[[3-[(3-methylphenyl)methoxy]phenyl]methylene]-1-phenyl-3,5-pyrazolidinedione
CAS Number
429653-73-6
Molecular Formula
C24H20N2O3
Formula Weight
384.4
Purity
≥98%
Formulation (Request formulation change)
A solid
Solubility(Learn about Variance in Solubility)
DMSO: Sparingly Soluble: 1-10 mg/mL
SMILES
O=C1NN(C(C1=CC2=CC(OCC3=CC(C)=CC=C3)=CC=C2)=O)C4=CC=CC=C4
InChi Code
InChI=1S/C24H20N2O3/c1-17-7-5-9-19(13-17)16-29-21-12-6-8-18(14-21)15-22-23(27)25-26(24(22)28)20-10-3-2-4-11-20/h2-15H,16H2,1H3,(H,25,27)
InChi Key
ITMLWGWTDWJSRZ-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    5 mg

    $65

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    10 mg

    $117

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    25 mg

    $260

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    50 mg

    $455

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    Cayman Chemical
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    Product Description

    Y16 is an inhibitor of the protein-protein interaction between Rho guanine nucleotide exchange factor 12 (Rho GEF 12), also known as leukemia-associated Rho GEF (LARG), and RhoA.1 It binds to the DH-PH domain of Rho GEF 12 in a cell-free assay (Kd = 76 nM) and inhibits serum-induced phosphorylation of MLC and FAK, a marker of RhoA activity, in NIH3T3 cells when used at concentrations of 10 and 30 µM. Y16 (5-30 µM) inhibits cell growth, migration, invasion, and mammosphere formation in MCF-7 breast cancer cells.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Shang, X., Marchioni, F., Evelyn, C.R., et al. Small-molecule inhibitors targeting G-protein-coupled Rho guanine nucleotide exchange factors. Proc. Natl. Acad. Sci. USA 110(8), 3155-3160 (2013).