NU7441, DNA-PK inhibitor (TBI4810)

Description

Product Details

Formal Name: 8-Dibenzothiophen-4-yl-2-morpholin-4-ylchromen-4-one

Alternate Names: Ku-57788

Molecular Formula: C₂₅H₁₉NO₃S

Formula Weight: 413.49

CAS Number: 503468-95-9

Purity: >98%

Formulation: powder

Solubility: Soluble in DMSO (up to 2 mg/ml with warming)

Storage: -20°C

Stability: ≥ 1 year.

Applications

DNA-PK inhibitor

Functions

Competitively inhibits DNA-dependent protein kinase (DNA-PK) (IC50 = 13 nM) over related kinases (IC50s 1.7 – 100 µM for mTOR, PI3K, ATM, and ATR). Sensitizes human colon cancer cells to etoposide and ionizing radiation through inhibition of double strand break repair of DNA. Enhances ionizing radiation-induced G2/M arrest of SUNE-1 cancer cells. Reverses acquired resistance to EGFR TK inhibitor osimertinib in a NSCLC line. Causes immunosuppression via reduction in cytokines and NFκB activity.

Application Procedures

First dissolved in DMSO (up to 2 mg/ml with warming), then diluted to aqueous buffer. Solutions in DMSO may be stored at -20° for up to 3 months.