NVP-BAG956

SKU: orb1678991

Description

NVP-BAG956 is a potent small molecule inhibitor targeting multiple PI3K isoforms (α, β, γ, δ) and PDK1. It demonstrates cytotoxic effects against T-cell acute lymphoblastic leukemia (T-ALL) cell lines in vitro and serves as a valuable research tool for studying cancers such as melanoma.

Research Area

Signal Transduction

Key Properties

• CAS Number: 853910-02-8
• MW: 427.5
• Purity: 99.80%
• Formula: C₂₈H₂₁N₅
• SMILES: N#CC(C1=CC=C(C=C1)N2C(=NC=3C=NC=4C=CC(C#CC=5C=NC=CC5)=CC4C32)C)(C)C
• Target: PI3K
• Solubility: 10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (4.68 mM);DMSO:40 mg/mL (93.57 mM)

Bioactivity

• Target IC50:
  A2058 cells:290 nM|PI3Kγ:117 nM|PI3Kβ:446 nM|PDK1:240 nM|PI3Kα:56 nM|pAkt:67 nM|PI3Kδ:35 nM|VEGFR1:2.56 μM
• In Vitro:
  NVP-BAG956 inhibited PDK1 (IC50: 240 nM) and VEGFR1 (IC50: 2.56 μM). It also blocked the phosphorylation of PKB/Akt in A2058 cells with an IC50 of 67 nM.The inhibition of PKB/Akt phosphorylation was closely correlated with the reduction of A2058 cell proliferation, with an IC50 of 290 nM for NVP-BAG956.In the presence of NVP-BAG956, the A2058 cells were only able to exit from the G2-M phase, and thereafter stayed in the G1 phase. In addition, NVP-BAG956 significantly induced the expression of p27Kip1 in A2058 cells, but not in C32 cells.
• Cell Research:
  One day after plating (7×10^3 cells/cm2), melanoma cells (A2058, B16F1, B16F10, C32, HBL, Malme, Malme3M, NA8, SKMel2, SKMel23, A375, Hs294T, WM35, and 1205lu cells) are exposed to LY294002 (25 μM), Wortmannin (500 nM), NVP-BAG956 (1 μM), NVP-BBD130 (1 μM), NVP-BEZ235 (1 μM), and ZSTK474 (1 μM), and Rapamycin (100 nM). Compound concentrations are set 2 log units above the IC50 in vitro to ensure full PI3K inhibition, except for the μM inhibitor LY294002. Cells are trypsinized and counted, and the volume is quantified using a Casy Counter and Analyser. To determine the nuclear volume, cells are resuspended in CASYton containing 0.5% Triton X-100, followed by repetitive pipetting (8×), before volume measurements.

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

NVP-BAG 956, NVPBAG956, NVP-BAG956, NVP-BAG-956, NVP BAG956, BAG 956, BAG956, BAG-956, PI3K, PI3Kα, PI3Kβ, PI3Kδ, PI3Kγ

Compound Identifiers

PubChem CID

24882589