Merck, 5319780001, ATM Inhibitor, KU 60019

Name: ATM Inhibitor, KU 60019
Brand: Merck
SKU: 5319780001

Size:10 mg, ATM Inhibitor, KU 60019, KU-60019, KU60019, Ataxia Telangiectasia Mutate Kinase Inhibitor

Catalog Number: 5319780001

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Category

Phosphatase Inhibitors

Pack Size10 mg

CollectionsMerck Cell Culture Supplements & Reagents: Complete Solutions for Research & Bioproduction Merck Roche Life Science Products for PCR, RT‑PCR & Nucleic Acid Purification

Description

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)

Specifications

General

MDL number	MFCD18384974
UNSPSC Code	12352200
NACRES	NA.77
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
assay	≥98% (HPLC)
form	solid
potency	6.3 nM IC50
manufacturer/tradename	Calbiochem®
storage condition	OK to freeze
color	light beige
solubility	DMSO: 50 mg/mL
Quality Level	100
storage temp.	2-8°C

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