Akt-I-2 hydrochloride
| Code | Size | Price |
|---|
| SYN-1006-M100 | 100 mg | Enquire |
Quantity:
| SYN-1006-M050 | 50 mg | Enquire |
Quantity:
| SYN-1006-M001 | 1 mg | £238.00 |
Quantity:
| SYN-1006-M005 | 5 mg | £461.00 |
Quantity:
| SYN-1006-M010 | 10 mg | £719.00 |
Quantity:
Prices exclude any Taxes / VAT
Overview
Regulatory Status: RUO
Shipping:
-20°C
Documents
Further Information
Alternate Names/Synonyms:
AktI2
Appearance:
Solid.
CAS:
473382-50-2
EClass:
32160000
Form (Short):
liquid
InChi:
InChI=1S/C23H21N3.ClH/c1-23(2,24)18-14-12-17(13-15-18)22-21(16-8-4-3-5-9-16)25-19-10-6-7-11-20(19)26-22;/h3-15H,24H2,1-2H3;1H
InChiKey:
NXSKOEXUDZHMAL-UHFFFAOYSA-N
Long Description:
Chemical. CAS: 473382-50-2. Formula: C23H21N3 . HCl. MW: 339.4 . 36.5. 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.
Molecular Formula:
C23H21N3 . HCl
Molecular Weight:
339.4 . 36.5
Package Type:
Plastic Vial
Product 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.
Purity:
>95%
Solubility Chemicals:
Soluble in DMSO.
Transportation:
Non-hazardous
UNSPSC Category:
Protein Kinase Modulators
UNSPSC Number:
12352200
Use & Stability:
Stable for at least 2 years after receipt when stored at -20°C.
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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