AKT inhibitor VIII

SKU: orb1304301

Description

AKT inhibitor VIII

Research Area

Cell Biology, Signal Transduction

Key Properties

• CAS Number: 612847-09-3
• MW: 551.64
• Purity: 98.65%
• Formula: C₃₄H₂₉N₇O
• SMILES: O=c1[nH]c2ccccc2n1C1CCN(Cc2ccc(cc2)-c2nc3cc4[nH]cnc4cc3nc2-c2ccccc2)CC1
• Target: Apoptosis,Akt
• Solubility: DMSO:255 mg/mL (462.26 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (3.63 mM)

Bioactivity

• Target IC50:
  Akt2:210 nM|Akt1:58 nM|Akt3:2119 nM
• In Vivo:
  In cell-based IPKA (C33A) assays, AKT inhibitor VIII suppresses Akt1/2 with IC50 values of 305 and 2086 nM, respectively. It significantly increases caspase-3 activity, inducing apoptosis in MCF7, HT29, and A2780 cells. In hepatocytes, it inhibits insulin's regulation of PEPCK and the expression of G6Pase and FOXO1 activity. Additionally, AKT inhibitor VIII enhances PAR-1-mediated platelet aggregation by blocking PKB. It inhibits cell growth in HCC827, NCI-H522, NCI-1651, and PC-9 cells with IC50 values of 4.7, 7.25, and 9.5 μM, respectively. When combined with gefitinib, the effects of suppressing cell growth and inducing apoptosis are enhanced.
• In Vitro:
  Akti-1/2 (50 mg/kg, i.p.) inhibits both basal and IGF-stimulated Akt1/2 phosphorylation in the lungs of mice.
• Cell Research:
  The cell growth inhibitory effect of AKTi-1/2 is studied using the 96 h sulforhodamine B assay (SRB). Drug concentrations that inhibited 50% of cell growth (IC50) are calculated for each compound in GraphPad Prism 6.0 using non-linear regression analysis and sigmoidal dose–response (variable slope) equation.(Only for Reference)

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

Akt, Akt1, AKT inhibitor VIII, Akt3, Akt2, AKTi-1/2, Apoptosis, inhibit, Inhibitor, Protein kinase B, PKB

Compound Identifiers

PubChem CID

135398501