Akt-I-2 hydrochloride

CHF 233.00
In stock
SYN-1006-M0011 mgCHF 233.00
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More Information
Product Details
Synonyms AktI2
Product Type Chemical
Properties
Formula C23H21N3 . HCl
MW 339.4 . 36.5
CAS 473382-50-2
Purity Chemicals ≥95%
Appearance Solid.
Solubility Soluble in DMSO.
Declaration Manufactured by SynKinase.
Other Product Data Target: AKT | Kinase Group: AGC | Substrate: Serine-Threonine

Click here for Original Manufacturer Product Datasheet
Our product description may differ slightly from the original manufacturers product datasheet.
InChi Key NXSKOEXUDZHMAL-UHFFFAOYSA-N
Shipping and Handling
Shipping AMBIENT
Short Term Storage +4°C
Long Term Storage -20°C
Use/Stability Stable for at least 2 years after receipt when stored at -20°C.
Documents
MSDS Download PDF
Product Specification Sheet
Datasheet Download PDF
The compound (Akt-I-2) inhibited both Akt1 and Akt2 with IC(50) values of 2.7 and 21 µM respectively. It does not inhibit AKT3. The compound is a reversible inhibitor, and exhibits a linear mixed-type inhibition against ATP and peptide substrate. In addition to inhibiting kinase activity of AKT1 and AKT2 isoforms, AKT-I-1,2 blocked the phosphorylation and activation of AKT1 and AKT2 by PDK1 (phosphoinositide-dependent kinase 1). The inhibitor was found to be cell-active and to block phosphorylation of Akt at Thr308 and Ser473, reduce the levels of active Akt in cells, block the phosphorylation of known Akt substrates and promote TRAIL (tumour-necrosis-factor-related apoptosis-inducing ligand)-induced apoptosis in LNCap prostate cancer cells.
Product References
  1. Identification and characterization of pleckstrin-homology-domain-dependent and isoenzyme-specific Akt inhibitors: S.F. Barnett, et al.; Biochem. J. 385, 399 (2005)
  2. Rapid assembly of diverse and potent allosteric Akt inhibitors: Z. Wu, et al.; Bioorg. Med. Chem. Lett. 18, 2211 (2008)
  3. QSAR study of Akt/protein kinase B (PKB) inhibitors using support vector machine: X. Dong, et al.; Eur. J. Med. Chem. 44, 4090 (2009)
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