BX-912

SKU: orb1307350

Description

BX-912 is a potent and selective cell-permeable inhibitor of PDK1 (IC50 = 12 nM), exhibiting over 10-fold selectivity against kinases such as C-Kit and PKC. It is a valuable chemical probe for studying the PI3K/PDK1/Akt signaling pathway in cancer research, enabling mechanistic investigations in both cellular and in vivo models.

Research Area

Cardiovascular Research, Cell Biology, Signal Transduction

Key Properties

• CAS Number: 702674-56-4
• MW: 471.35
• Purity: 99.34% (May vary between batches)
• Formula: C₂₀H₂₃BrN₈O
• SMILES: Brc1cnc(Nc2cccc(NC(=O)N3CCCC3)c2)nc1NCCc1cnc[nH]1
• Target: PKA,Chk,CDK,PDK,VEGFR,Apoptosis
• Solubility: H2O:< 1 mg/mL (insoluble or slightly soluble);10% DMSO+40% PEG300+5% Tween 80+45% Saline:3.3 mg/mL (7 mM);DMSO:87 mg/mL (184.58 mM);Ethanol:87 mg/mL (184.58 mM)

Bioactivity

• Target IC50:
  PDK1:12 nM
• In Vitro:
  BX-912 exhibits inhibitory effects on ChcK1 (IC50: 0.83 μM), PKA (IC50: 0.11 μM), c-kit (IC50: 0.85 μM), and KDR (IC50: 0.41 μM). In tumor cells, BX-912 blocks the PDK1/Akt signaling pathway, inhibiting adhesion-dependent growth in various tumor cells (e.g., PC-3 cells) or inducing apoptosis. The compound shows a 30-fold higher sensitivity to growth inhibition by BX-912 in cancer cell lines with elevated Akt activity in soft agar than in tissue culture plastics, consistent with the cell survival function of the PDK1/Akt signaling pathway, especially significant for non-adherent cells. BX-912 significantly inhibits PDK1 enzyme activity without affecting AKT2 activity (IC50 >10 μM), making it a direct inhibitor of PDK1. It notably increases the count of MDA-468 cells with 4N DNA content and arrests cells in the G2/M phase. BX-912 effectively suppresses cell growth (IC50: 0.32 μM) and is highly effective in inhibiting HCT-116 cell growth at 1 μM (inhibition rate of 96%).
• Cell Research:
  Cells such as MDA-468, MDA-453 are seeded at a low density (1.5-3 × 103 cells/well, 0.1 mL/well, 96-well plates) and are incubated overnight. BX912 treatments are made by adding 10 μL/well of the compound in 1% dimethyl sulfoxide and growth medium (final concentration of dimethyl sulfoxide, 0.1%), followed by brief shaking. Treated cells are incubated for 72 hours, and viability is measured by the addition of 10 μL of the metabolic dye WST-1. The WST-1 signal is read in a plate reader at 450 nm, and a no cell, or zero time cell, background is subtracted to calculate the net signal. (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

Apoptosis, BX 912, BX912, BX-912, Chk1, CDK2/CyclinE, Inhibitor, inhibit, VEGFR2 (KDR), PDK1, PDK-1, PKA

Compound Identifiers

PubChem CID

11754511