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SynKinase
Akt-I-2 hydrochloride
CHF 0.00
In stock
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| 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 |
Description
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
- Identification and characterization of pleckstrin-homology-domain-dependent and isoenzyme-specific Akt inhibitors: S.F. Barnett, et al.; Biochem. J. 385, 399 (2005)
- Rapid assembly of diverse and potent allosteric Akt inhibitors: Z. Wu, et al.; Bioorg. Med. Chem. Lett. 18, 2211 (2008)
- 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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