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5.31978

ATM Inhibitor, KU 60019

Name: ATM Inhibitor, KU 60019
Brand: MM

Synonym(s):

ATM Inhibitor, KU 60019, KU-60019, KU60019, Ataxia Telangiectasia Mutate Kinase Inhibitor

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About This Item

Empirical Formula (Hill Notation):

C₃₀H₃₃N₃O₅S

CAS Number:

925701-46-8

Molecular Weight:

547.67

MDL number:

MFCD18384974

UNSPSC Code:

12352200

NACRES:

NA.77

Assay:

≥98% (HPLC)

Form:

solid

Quality level:

100

Storage condition:

OK to freeze, protect from light

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assay

≥98% (HPLC)

Quality Level

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

Related Categories

Bioactive Small Molecule Inhibitors

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)

Storage Class

11 - Combustible Solids

wgk

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable

Regulatory Information

新产品

This item has

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Global Trade Item Number

SKU	GTIN
5319780001	04055977287127

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