5.31978

ATM Inhibitor, KU 60019

• Synonym(e): ATM Inhibitor, KU 60019, KU-60019, KU60019, Ataxia Telangiectasia Mutate Kinase Inhibitor
• Empirische Formel (Hill-System): C₃₀H₃₃N₃O₅S
• CAS-Nummer: 925701-46-8
• Molekulargewicht: 547.67
• MDL number: MFCD18384974
• UNSPSC Code: 12352200
• NACRES: NA.77
• Assay: ≥98% (HPLC)
• Form: solid
• Storage condition: OK to freeze, protect from light

Eigenschaften

• assay: ≥98% (HPLC)
• Quality Segment: 100
• form: solid
• potency: 6.3 nM IC₅₀
• manufacturer/tradename: Calbiochem^®
• storage condition: OK to freeze, protect from light
• color: light beige
• solubility: DMSO: 50 mg/mL
• storage temp.: 2-8°C
• SMILES string: S1c2c(cccc2C5=CC(=O)C=C(O5)N6CCOCC6)Cc3c1ccc(c3)NC(=O)CN4C[C@H](O[C@H](C4)C)C
• InChI: 1S/C30H33N3O5S/c1-19-16-32(17-20(2)37-19)18-28(35)31-23-6-7-27-22(13-23)12-21-4-3-5-25(30(21)39-27)26-14-24(34)15-29(38-26)33-8-10-36-11-9-33/h3-7,13-15,19-20H,8-12,16-18H2,1-2H3,(H,31,35)/t19-,20+
• InChI key: SCELLOWTHJGVIC-BGYRXZFFSA-N

Beschreibung

General description

A cell permeable thioxanthene based compound that acts as a highly potent inhibitor of Ataxia telangiectasia mutate (ATM) kinase inhibitor (IC₅₀ = 6.3 nM). Displays about 270 and 1600-fold greater selectivity over DNA-PK and ATR kinase (IC₅₀ = 1.7 and >10 µM, respectively). Has only a trivial effect on 229 protein kinases when screened in a panel at 1 µM level. Shown to block Ser15 phosphorylation of p53 and basal and radiation-induced Ser473 phosphorylation of Akt in glioma cells. Blocks radiation-induced DNA damage response and radiosensitizes human glioma cells (U87 and U1242) and mouse glioma stem cells and inhibits glioma cell migration, invasion, and growth. Also radiosensitizes orthotopic glioma xenografts and significantly extends the survival of mice.

ATM kinase inhibitor, KU60019, is a cell permeable, potent inhibitor of ATM kinase inhibitor (IC₅₀ = 6.3 nM). Has 270 & 1600-fold higher selectivity over DNA-PK and ATR kinase.

Biochem/physiol Actions

Cell permeable: yes

Primary Target
ATM

Preparation Note

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

Other Notes

Biddlestone-Thorpe, L., et al. 2013. Clin. Cancer Res.19, 3189.
Golding, S., et al. 2009. Mol. Cancer Ther.8, 2894.

Legal Information

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

Disclaimer

Toxicity: Standard Handling (A)

Sicherheitshinweise

• Lagerklasse: 11 - Combustible Solids
• wgk: WGK 3
• flash_point_f: Not applicable
• flash_point_c: Not applicable