Y16
Y16 Basic information
- Product Name:
- Y16
- Synonyms:
-
- Y16
- 4-[[3-[(3-Methylphenyl)methoxy]phenyl]methylene]-1-phenyl-3,5-pyrazolidinedione
- Y16, >98%
- Y16, 429653-73-6
- 3,5-Pyrazolidinedione, 4-[[3-[(3-methylphenyl)methoxy]phenyl]methylene]-1-phenyl-
- Inhibitor,inhibit,Y-16,Y 16,Ras,Y16
- 4-(3-((3-Methylbenzyl)oxy)benzylidene)-1-phenylpyrazolidine-3,5-dione
- Y16, 10 mM in DMSO
- CAS:
- 429653-73-6
- MF:
- C24H20N2O3
- MW:
- 384.43
- Mol File:
- 429653-73-6.mol
Y16 Chemical Properties
- Density
- 1.273±0.06 g/cm3(Predicted)
- storage temp.
- 2-8°C
- solubility
- DMSO: soluble5mg/mL, clear (warmed)
- pka
- 8.84±0.20(Predicted)
- form
- powder
- color
- , faint yellow to dark orange
Y16 Usage And Synthesis
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 () |