For research use only. Not for therapeutic Use.
<p style=/line-height:25px/>Y16 is an inhibitor of G-protein–coupled Rho GEFs; works synergistically with Rhosin/G04 in inhibiting LARG-RhoA interaction, RhoA activation, and RhoA-mediated signaling functions.<br>IC50 value:<br>Target: RhoA inhibitor<br>Y16 binds to this catalytic fragment of LARG with a Kd of ～76 ± 8 nM. Y16 was able to inhibit the GDP dissociation from RhoA catalyzed by LARG dose dependently without affecting the GEF reactions of Rac1 and Cdc42 catalyzed by TrioN and Intersectin, respectively. The N983A mutant lost the binding ability to Y16 with a Kd > 500 μM, whereas the K979A and E982A mutants showed a reduced affinity with Kd values of 0.47 and 2.1 μM, respectively. At 2.5 μM each, Rhosin and Y16 inhibited ～50% RhoA-GTP content, and at 5 μM each ～80% RhoA-GTP stimulated by serum, which were much more potent than the effect of Rhosin/G04 or Y16 acting alone (～80% inhibition at 30 μM). Even under a higher concentration of Y16 and Rhosin/G04 combination (50 μM each) when endogenous RhoA-GTP content was effectively suppressed, no effect on Rac1-GTP or Cdc42-GTP content in cells was observed. Although Rhosin/G04 or Y16 administration alone caused ～50% inhibition of RhoA activity at 10 μM, combined Rhosin/G04 and Y16 reached 70% inhibition of RhoA-GTP or the downstream p-MLC when each was at 2.5 μM.</p>
| Catalog Number | I003533 |
| CAS Number | 429653-73-6 |
| Molecular Formula | C24H20N2O3 |
| Purity | ≥95% |
| Target | MAPK/ERK Pathway |
| Solubility | 10 mM in DMSO |
| Storage | 3 years -20C powder |
| InChI | 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)/b22-15+ |
| InChIKey | ITMLWGWTDWJSRZ-PXLXIMEGSA-N |
| SMILES | O=C(/C1=CC2=CC=CC(OCC3=CC=CC(C)=C3)=C2)NN(C4=CC=CC=C4)C1=O |
| Reference | </br>1:Purification and characterization of a low-temperature hydroxylamine oxidase from heterotrophic nitrifier Acinetobacter sp. Y16. Zhang SM, Li WG, Zhang DY, Huang XF, Qin W, Sha CQ.Biomed Environ Sci. 2014 Jul;27(7):515-22. doi: 10.3967/bes2014.004. PMID: 25073910 Free Article</br>2:Ammonium removal by a novel oligotrophic Acinetobacter sp. Y16 capable of heterotrophic nitrification-aerobic denitrification at low temperature. Huang X, Li W, Zhang D, Qin W.Bioresour Technol. 2013 Oct;146:44-50. doi: 10.1016/j.biortech.2013.07.046. Epub 2013 Jul 18. PMID: 23911816 </br>3:Structural characterization and antioxidant properties of an exopolysaccharide produced by the mangrove endophytic fungus Aspergillus sp. Y16. Chen Y, Mao W, Tao H, Zhu W, Qi X, Chen Y, Li H, Zhao C, Yang Y, Hou Y, Wang C, Li N.Bioresour Technol. 2011 Sep;102(17):8179-84. doi: 10.1016/j.biortech.2011.06.048. Epub 2011 Jun 17. PMID: 21733681 </br>4:Inhibitory effects of costunolide isolated from Laurus nobilis on IgE-induced degranulation of mast cell-like RBL-2H3 cells and the growth of Y16 pro-B cells. Kim TJ, Nam KW, Kim B, Lee SJ, Oh KB, Kim KH, Mar W, Shin J.Phytother Res. 2011 Sep;25(9):1392-7. doi: 10.1002/ptr.3553. Epub 2011 Jun 14. PMID: 21674633 </br>5:Escherichia coli mutant Y16 is a double mutant carrying thermosensitive ftsH and ftsI mutations. Begg KJ, Tomoyasu T, Donachie WD, Khattar M, Niki H, Yamanaka K, Hiraga S, Ogura T.J Bacteriol. 1992 Apr;174(7):2416-7. PMID: 1551860 Free PMC Article |
