124032
Akt Inhibitor XIV
The Akt Inhibitor XIV, also referenced under CAS 1191951-57-1, controls the biological activity of Akt. This small molecule/inhibitor is primarily used for Phosphorylation & Dephosphorylation applications.
别名:
Akt Inhibitor XIV, 4-Dodecyl-N-(1,3,4-thiadiazol-2-yl)benzenesulfonamide, PDK1 Inhibitor III, PHT-427
InChI key
BYWWNRBKPCPJMG-UHFFFAOYSA-N
InChI
1S/C20H31N3O2S2/c1-2-3-4-5-6-7-8-9-10-11-12-18-13-15-19(16-14-18)27(24,25)23-20-22-21-17-26-20/h13-17H,2-12H2,1H3,(H,22,23)
assay
≥95% (HPLC)
form
solid
manufacturer/tradename
Calbiochem®
storage condition
OK to freeze
color
white
solubility
DMSO: 50 mg/mL
shipped in
ambient
Quality Level
General description
A cell-permeable thiadiazolyl compound that binds to PH (pleckstrin homology) domain (Kd = 40.8 µM, Ki = 2.4 µM) and acts as a competitive and reversible blocker of Akt translocation to the cellular membrane with selectivity over PDK1 (Kd = 90.1 µM, Ki = 5.5 µM). Inhibits pAkt-Ser473 (IC50 = 6.3, 8.6 and 10 µM in Panc-1, BxPC-3 and MiaPaCa-2 cells, respectively), and induces apoptosis at 20 µM (40% and 31%) and causes growth arrest (IC50 = 65 and 30 µM) in Panc-1 and MiaPaCa-2 cells, respectively. Further, suppresses tumor growth and regression in mouse xenograft model (125 mg/kg, i.p.) and reduces pGSK-3α-Ser21 and pGSK-3β-Ser9 and p70S6K-Thr389 levels.
Preparation Note
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.
Other Notes
Meuillet, E.J., et al. 2010. Mol. Cancer Ther. 9, 706.
Moses, S.A., et al. 2009. Cancer Res. 69, 5073.
Moses, S.A., et al. 2009. Cancer Res. 69, 5073.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Disclaimer
Toxicity: Standard Handling (A)
存储类别
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
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