YM-254890

Cyclic depsipeptide composed of unique amino acids differing from normal amino acids. Membrane permeable, potent and selective Galphaq family inhibitor. Inhibits the signal transduction of Galphaq, Galpha11 and Galpha14 (IC50=0.095µM) by blocking the exchange of GDP for GTP, preventing the activation of the G protein. Inhibits platelet aggregation induced by ADP. Shown to inhibit Galphaq-coupled GPCR signaling by inhibiting calcium mobilization and to have antithrombotic and thrombolytic effects. Might be used as a starting point for new approaches in cancer drug discovery. Galphaq signaling has been shown to regulate brown/beige adipocytes using the structurally similar specific Galphaq family inhibitor FR900359. It is suggested that inhibition of this pathway may be a novel therapeutic approach to combat obesity. The closely related compounds YM-254890 and FR900359 (UBO-QIC) are both potent and selective Galphaq family inhibitors and were for long time only restricted accessible. The commercial availability of YM-254890 might give further insights into Galphaq family signaling processes.

Price Not Available 1 mg YM-254890 Supplier Page
Catalog Number AG-CN2-0509-M001
Alternative Name(s) QS 3666A
Research Area Biochemicals, Cancer, Immunology, Metabolism, Natural Products
Molecular Formula C46H69N7O15
CAS# 568580-02-9
Purity >95%
Inchi InChI=1S/C46H69N7O15/c1-22(2)37(56)34(49-30(11)55)45(63)68-38(23(3)4)35-43(61)53(14)36(28(9)65-15)46(64)66-27(8)33(48-29(10)54)44(62)67-32(21-31-19-17-16-18-20-31)42(60)52(13)25(6)39(57)47-24(5)41(59)51(12)26(7)40(58)50-35/h16-20,22-24,26-28,32-38,56H,6,21H2,1-5,7-15H3,(H,47,57)(H,48,54)(H,49,55)(H,50,58)/t24-,26-,27+,28+,32+,33-,34-,35-,36-,37+,38+/m0/s1
Inchi Key QVYLWCAYZGFGNF-WBWCVGBTSA-N
SMILES O=C(N(C)C(C(N[C@H](C(N(C)[C@H](C(N[C@@H]([C@@H](C(C)C)OC([C@@H](NC(C)=O)[C@@H](C(C)C)O)=O)C1=O)=O)C)=O)C)=O)=C)[C@H](OC([C@@H](NC(C)=O)[C@@H](C)OC([C@@H](N1C)[C@@H](C)OC)=O)=O)CC2=CC=CC=C2
Size 1 mg
Supplier Page http://www.adipogen.com/ag-cn2-0509/ym-254890.html