Item no. |
S2682-50 |
Manufacturer |
Selleckchem
|
CASRN |
1218777-13-9 |
Amount |
50 mg |
Category |
|
Type |
Inhibitors |
Specific against |
other |
ECLASS 10.1 |
32160490 |
ECLASS 11.0 |
32160490 |
UNSPSC |
12000000 |
Alias |
1218777-13-9 ' |
Similar products |
CAY10505 |
Available |
|
Administration |
Administered via p.o. |
Animal Models |
Wistar albino rats |
Cell lines |
Bone marrow cells |
Chemical Name |
(E)-5-((5-(4-fluorophenyl)furan-2-yl)methylene)thiazolidine-2, 4-dione |
Concentrations |
ca.10 mM |
Description |
CAY10505 is a PI3Kgamma inhibitor with IC50 of 30 nM. |
Dosages |
0.6 mg/kg |
IC50 |
30 nM, 30 nM, 30 nM, 30 nM, 30 nM, 30 nM |
In vitro |
CAY10505 selectively inhibits PI3Kgamma isoform, with an IC50 of 30 nM better than the PI3Kalpha, beta, and delta isoforms, with IC50 of 0.94, 20 and 20 uM, respectively. Tested against a panel of 80 other kinases including casein kinase 2, CAY10505 significantly inhibits only the unrelated casein kinase 2 (CK20) with an IC50 of 20 nM. CAY10505 also inhibits the phosphorylation of the PI3K substrate PKB/Akt in mouse macrophages with an IC50 of 228 nM. CAY10505 inhibits C5a-mediated PKB/Akt phosphorylation in Raw-264 macrophages, with an IC50 of 0.23 nM. In human monocytic cell line THP-1, MCP-1, binding to the GPCR chemokine receptor CCR2, strongly induces phosphorylation of PKB/Akt, which is effectively inhibited by 26 at IC50 values as low as 0.4 uM. CAY10505 inhibits MCP-1-mediated chemotaxis in wild-type primary monocytes in a concentration-dependent manner with an IC50 of 52 uM, as well as in the monocytic cell line THP-1 with an IC50 of 53 uM. [1] |
In vivo |
Oral administration of CAY10505 at 10 mg/kg results in moderate reduction of neutrophil recruitment by 35%, almost matching the result observed in PI3Kgamma-deficient mice. [1] Five weeks of deoxycorticosterone acetate salt (DOCA) administration are followed by 7 days of daily administration of PI3Kgamma inhibitor CAY10505 at a dose of 0.6 mg/kg (p.o.), which significantly improves acetylcholine-induced endothelium dependent relaxation, serum nitrate and (or) nitrite level, glutathione level, and the vascular endothelial lining in hypertensive rats. [2] |
Incubation Time |
3 hours |
Kinase Assay |
PI3Kgamma lipid kinase assay, A PI3Kgamma lipid kinase assay, based on the neomycin-coated scintillation proximity assay (SPA) bead technology, is performed in 384-well plates using ATP/[gamma33P]ATP and PtdIns as substrates. Kinase assays for IC50 value determinations of CAY10505 with PI3Kalpha, PI3Kbeta, and PI3Kdelta are carried out. |
Method |
Bone marrow cells are isolated, prepared, and stimulated. For in vitro chemotaxis, 107 5-day-derived BMDMs are suspended in 1 mL of medium containing 0.5% BSA and CAY10505 or DMSO and applied to the upper chamber of a transwell, 5 um pore size, chemotaxis plate. An amount of 600 uL of medium containing MCP-1/CCL2 and inhibitors or DMSO is added to the lower chamber. After 3 hours of incubation at 37 C and 5% CO2, the number of cells in the lower chamber is quantified with a Coulter. |
Molecular Weight (MW) |
289, 28 |
Picture ChemicalStructure Description |
CAY10505 Chemical Structure |
Picture Description 1 |
Data independently produced by Dr. Zhang, of Tianjin Medical University, , CAY10505purchased from Selleck, After starved in serum-free medium for 24h, A549 cells incubated with the indicated concentrations of CAY10505 for 3h, followed by 20-minute stimolation of 100ng/ml EGF. |
Solubility (25C) |
DMSO 58 mg/mL, Water <1 mg/mL, Ethanol <1 mg/mL |
Storage |
2 years -20CPowder, 2 weeks4Cin DMSO, 2 months-80Cin DMSO |
Note: The presented information and documents (Manual, Product Datasheet, Safety Datasheet and Certificate of Analysis) correspond to our latest update and should serve for orientational purpose only. We do not guarantee the topicality. We would kindly ask you to make a request for specific requirements, if necessary.
All products are intended for research use only (RUO). Not for human, veterinary or therapeutic use.