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
• UNSPSC-Code: 12352200
• NACRES: NA.77

Eigenschaften

• Assay: ≥98% (HPLC)
• Qualitätsniveau: 100
• Form: solid
• Wirksamkeit: 6.3 nM IC₅₀
• Hersteller/Markenname: Calbiochem^®
• Lagerbedingungen: OK to freeze; protect from light
• Farbe: light beige
• Löslichkeit: DMSO: 50 mg/mL
• Lagertemp.: 2-8°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+
• InChIKey: SCELLOWTHJGVIC-BGYRXZFFSA-N

Beschreibung

Allgemeine Beschreibung

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.

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.

Please note that the molecular weight for this compound is batch-specific due to variable water content. Please refer to the vial label or the certificate of analysis for the batch-specific molecular weight. The molecular weight provided represents the baseline molecular weight without water.

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. Wirkung

Cell permeable: yes

Primary Target
ATM

Warnhinweis

Toxicity: Standard Handling (A)

Rekonstituierung

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

Sonstige Hinweise

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

Rechtliche Hinweise

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

Sicherheitshinweise

• Lagerklassenschlüssel: 11 - Combustible Solids
• WGK: WGK 3
• Flammpunkt (°F): Not applicable
• Flammpunkt (°C): Not applicable