GSK2334470

SKU: orb1305621

Description

GSK2334470 is a potent and selective small molecule inhibitor of PDK1, demonstrating an IC50 of approximately 10 nM in biochemical assays with minimal activity against related AGC kinases. This tool compound is used in vitro to investigate PI3K/PDK1 signaling pathways in cancer research and has been utilized in vivo to study metabolic regulation.

Research Area

Cell Biology

Key Properties

• CAS Number: 1227911-45-6
• MW: 462.6
• Purity: >98%
• Formula: C₂₅H₃₄N₈O
• SMILES: CNc1nc(cc(n1)-c1ccc2c(N)n[nH]c2c1)N1C[C@H](CC[C@H]1C)C(=O)NC1CCCCC1
• Target: Kinase
• Solubility: Soluble in DMSO (40 mg/ml)

Bioactivity

• Target IC50:
  PDK1:10 nM
• In Vivo:
  The efficacy of the PDK1 inhibitor (PDKi) GSK2334470 was assessed in newborn BrafV600E::Pten / mice through systemic administration of 4-HT. Administering PDK1 twice weekly significantly inhibited pigmented lesions and concurrent melanomagenesis, alongside a notable reduction (~80%) in lung metastases and lymph node metastases, as quantified by H&E staining and S100 immunostaining, respectively. This outcome mirrors the effects observed with the genetic deletion of Pdk1.
• Cell Research:
  GSK2334470 is dissolved in DMSO and diluted with appropriate medium before use. To study the inhibitory effect of GSK2334470 on mTOR-S6K pathway, non-resistant cells and the resistant sublines are treated with GSK2334470 at 5 μM for 1.5 and 12 h in 10 % FBS medium with/without MK-2206 (5 μM).

Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

GSK-470

Compound Identifiers

PubChem CID

46215815