Y16

Hersteller MedChem Express
Kategorie
Typ Inhibitors
Specific against other
Menge 5mg
ArtNr HY-12649-5mg
eClass 6.1 30220300
eClass 9.0 32160605
Lieferbar
Synonyms
Y-16
CAS No.
429653-73-6
Purity
>98%
MW
3844272
Formula
C24H20N2O3
Solubility
10 mM in DMSO
Biological Description
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.
IC50 value:
Target: RhoA inhibitor
Y16 binds to this catalytic fragment of LARG with a Kd of ca.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 uM, whereas the K979A and E982A mutants showed a reduced affinity with Kd values of 0.47 and 2.1 uM, respectively. At 2.5 uM each, Rhosin and Y16 inhibited ca.50% RhoA-GTP content, and at 5 uM each ca.80% RhoA-GTP stimulated by serum, which were much more potent than the effect of Rhosin/G04 or Y16 acting alone (ca.80% inhibition at 30 uM). Even under a higher concentration of Y16 and Rhosin/G04 combination (50 uM 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 ca.50% inhibition of RhoA activity at 10 uM, combined Rhosin/G04 and Y16 reached 70% inhibition of RhoA-GTP or the downstream p-MLC when each was at 2.5 uM.
Menge: 5mg
Lieferbar: In stock
Listenpreis: 132,50 €
Rabatt: -10,0%
Preis: 119,25 €
Sie sparen: 13,25 €
lieferbar

Vergleichen

Angebot anfordern

Fragen zum Produkt?
 
Schließen