234501

Compound 401

A cell-permeable pyrimido-isoquinolinone compound that acts as a potent, reversible, and ATP-competitive inhibitor of DNA-PK (IC₅₀ = 280 nM) with ~19-fold selectivity over mTOR (IC₅₀ = 5.3 µM).

• Synonym(s): Compound 401, 2-(Morpholin-1-yl)pyrimido[2,1-a]isoquinolin-4-one
• Empirical Formula (Hill Notation): C₁₆H₁₅N₃O₂
• CAS Number: 168425-64-7
• Molecular Weight: 281.31
• UNSPSC Code: 12352200

Properties

• Quality Level: 100
• Assay: ≥95% (HPLC)
• form: solid
• manufacturer/tradename: Calbiochem^®
• storage condition: OK to freeze; protect from light
• color: beige
• solubility: DMSO: 5 mg/mL
• shipped in: ambient
• storage temp.: 2-8°C
• InChI: 1S/C16H15N3O2/c20-15-11-14(18-7-9-21-10-8-18)17-16-13-4-2-1-3-12(13)5-6-19(15)16/h1-6,11H,7-10H2
• InChI key: BVRDQVRQVGRNHG-UHFFFAOYSA-N

Description

General description

A cell-permeable pyrimido-isoquinolinone compound that acts as a potent, reversible, and ATP-competitive inhibitor of DNA-PK (IC₅₀ = 280 nM) with ~19-fold selectivity over mTOR (IC₅₀ = 5.3 µM). Exhibits much reduced or no activity against 43 other commonly studied kinases, including PI 3-K, ATM, and ATR. Shown to induce apoptosis and inhibit mTOR-dependent growth in TSC1^-/- murine embryo fibroblasts.

Packaging

Packaged under inert gas

Warning

Toxicity: Standard Handling (A)

Reconstitution

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

Other Notes

Ballou, L.M., et al. 2007. J. Biol. Chem.282, 24463.
Griffin, R.J., et al. 2005. J. Med. Chem.48, 569.

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Safety Information

• Storage Class Code: 11 - Combustible Solids
• WGK: WGK 1
• Flash Point(F): Not applicable
• Flash Point(C): Not applicable