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Merck

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.

Synonym(s):

Akt Inhibitor XIV, 4-Dodecyl-N-(1,3,4-thiadiazol-2-yl)benzenesulfonamide, PDK1 Inhibitor III, PHT-427

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About This Item

Empirical Formula (Hill Notation):
C20H31N3O2S2
CAS Number:
1191951-57-1
Molecular Weight:
409.61
UNSPSC Code:
12352200
Assay:
≥95% (HPLC)
Form:
solid
Quality level:
100
Storage condition:
OK to freeze

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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

storage temp.

2-8°C

Quality Level

100

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.

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Disclaimer

Toxicity: Standard Handling (A)

Storage Class

11 - Combustible Solids

wgk

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable

Certificates of Analysis (COA)

Search for Certificates of Analysis (COA) by entering the products Lot/Batch Number. Lot and Batch Numbers can be found on a product’s label following the words ‘Lot’ or ‘Batch’.

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