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方案
≥98% (HPLC)
质量水平
表单
solid
效能
6.3 nM IC50
制造商/商品名称
Calbiochem®
储存条件
OK to freeze
protect from light
颜色
light beige
溶解性
DMSO: 50 mg/mL
储存温度
2-8°C
SMILES字符串
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
一般描述
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.
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.
生化/生理作用
Cell permeable: yes
Primary Target
ATM
ATM
警告
Toxicity: Standard Handling (A)
重悬
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
其他说明
Biddlestone-Thorpe, L., et al. 2013. Clin. Cancer Res.19, 3189.
Golding, S., et al. 2009. Mol. Cancer Ther.8, 2894.
Golding, S., et al. 2009. Mol. Cancer Ther.8, 2894.
法律信息
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
储存分类代码
11 - Combustible Solids
WGK
WGK 3
闪点(°F)
Not applicable
闪点(°C)
Not applicable
法规信息
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