| Identification | Back Directory | [Name]
Y16 | [CAS]
429653-73-6 | [Synonyms]
Y16 Y16, >98% Y16, 429653-73-6 4-[[3-[(3-Methylphenyl)methoxy]phenyl]methylene]-1-phenyl-3,5-pyrazolidinedione 3,5-Pyrazolidinedione, 4-[[3-[(3-methylphenyl)methoxy]phenyl]methylene]-1-phenyl- | [Molecular Formula]
C24H20N2O3 | [MDL Number]
MFCD03083787 | [MOL File]
429653-73-6.mol | [Molecular Weight]
384.43 |
| Chemical Properties | Back Directory | [density ]
1.273±0.06 g/cm3(Predicted) | [storage temp. ]
2-8°C | [solubility ]
DMSO: soluble5mg/mL, clear (warmed) | [form ]
powder | [pka]
8.84±0.20(Predicted) | [color ]
, faint yellow to dark orange | [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) | [InChIKey]
ITMLWGWTDWJSRZ-UHFFFAOYSA-N | [SMILES]
N2(NC(=O)C(=Cc3cc(ccc3)OCc4cc(ccc4)C)C2=O)c1ccccc1 |
| Hazard Information | Back Directory | [Uses]
Y16 is a specific inhibitor of Leukemia-associated Rho guanine nucleotide exchange factor (LARG) with a Kd value of 76 nM. Y16 is active in blocking the interaction of LARG and related G-protein-coupled Rho GEFs with RhoA. Y16 shows no detectable effect on other diffuse B-cell lymphoma (Dbl) family Rho GEFs, Rho effectors, or a RhoGAP[1]. | [Biological Activity]
Y16 is an inhibitor of G protein-coupled Rho GEFs. It blocks the binding of LARG and Rho with a Kd of 80 nM. | [in vitro]
Y16 (10-30 μΜ; 24 hours; NIH 3T3 cells) could inhibit RhoA-GTP formation induced by serum dose dependently and is specific for RhoA. Y16 (10-30 μΜ; 24 hours ; NIH 3T3 cells) efficiently inhibits serum or SDF-1α-induced phospho-MLC and phospho-FAK formation, which are downstream of RhoA. Cell Viability Assay | Cell Line: | NIH 3T3 cells | | Concentration: | 10 μΜ, 30 μΜ | | Incubation Time: | 24 hours | | Result: | Inhibited RhoA-GTP formation induced by serum dose dependently and was specific for RhoA. | Western Blot Analysis | Cell Line: | NIH 3T3 cells | | Concentration: | 10 μΜ, 30 μΜ | | Incubation Time: | 24 hours | | Result: | Inhibited serum or SDF-1α-induced phospho-MLC and phospho-FAK formation, which were downstream of RhoA. | | [target]
| Target | Value | RhoGEFs () | table>[References]
[1] Shang X, et al. Small-molecule inhibitors targeting G-protein-coupled Rho guanine nucleotide exchange factors. Proc Natl Acad Sci U S A. 2013 Feb 19;110(8):3155-60. DOI:10.1073/pnas.1212324110 |
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Tags:429653-73-6
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