Compound 401

SKU: orb1304029

Description

Compound 401 (2-morpholino-4H-pyrimido[2,1-a]isoquinolin-4-one) is a potent and selective small molecule inhibitor of DNA-PK with an IC50 of 0.28 μM, which additionally inhibits mTOR while sparing PI3K. It is a valuable chemical probe for studying DNA damage response and repair pathways in both cellular and animal models of cancer research.

Research Area

Molecular Biology, Pharmacology & Drug Discovery, Signal Transduction

Key Properties

• CAS Number: 168425-64-7
• MW: 281.31
• Purity: 99.76% (May vary between batches)
• Formula: C₁₆H₁₅N₃O₂
• SMILES: O=c1cc(nc2c3ccccc3ccn12)N1CCOCC1
• Target: DNA-PK
• Solubility: DMSO:5.45 mg/mL (19.37 mM)

Bioactivity

• Target IC50:
  DNA-PK:0.28 μM|mTOR:5.3 μM
• In Vitro:
  Compound 401 shows activity against mTOR (IC50 = 5.3 μM) but not p110α/p85α PI3K (IC50 > 100 μM). Treatment of cells with Compound 401 blocks the phosphorylation of sites modified by mTOR-Raptor and mTOR-Rictor complexes (ribosomal protein S6 kinase 1 Thr389 and Akt Ser473, respectively).
  Read more...

Storage & Handling

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

Alternative Names

Inhibitor, inhibit, 2-morpholino-4H-pyrimido[2,1-a]isoquinolin-4-one, DNA-dependent protein kinase, DNA-PK, DNAPK, Compound401, Compound-401, Compound 401

Compound Identifiers

PubChem CID

10039361