VE-821 is a novel ATR inhibitor. VE-821, sensitises tumour cells to DNA damage induced by radiation or chemotoxic drugs, by disrupting the DNA damage checkpoint and inhibiting DNA repair.Potent, selective ATP competitive ATR inhibitor (K i\xa0= 13 nM). Ex
Storage Temp
Store at -20°C
Shipped In
Ice chest + Ice pads
Grade
Moligand™
Action Type
INHIBITOR
Mechanism of action
Inhibitor of ATR serine/threonine kinase
Note
Wherever possible, you should prepare and use solutions on the same day. However, if you need to make up stock solutions in advance, we recommend that you store the solution as aliquots in tightly sealed vials at -20°C. Generally, these will be useable for up to one month. Before use, and prior to opening the vial we recommend that you allow your product to equilibrate to room temperature for at least 1 hour. Need more advice on solubility, usage and handling? Please visit our frequently asked questions (FAQ) page for more details.
Product Description
VE-821 is a potent and selective ATP competitive inhibitor of ATR with Ki/IC50 of 13 nM/26 nM in cell-free assays, shows inhibition of H2AX phosphorylation, minimal activity against PIKKs ATM, DNA-PK, mTOR and PI3Kγ.
Associated Targets(Human)
PRKDCTchemDNA-dependent protein kinase catalytic subunit (1 Activities)
1.Zhao Mengjie, Li Yanhui, Lu Chenfei, Ding Fangshu, Xu Miao, Ge Xin, Li Mengdie, Wang Zhen, Yin Jianxing, Zhang Junxia, Wang Xiefeng, Ge Zehe, Xiao Hong, Xiao Yong, Liu Hongyi, Liu Wentao, Cao Yuandong, Wang Qianghu, You Yongping, Wang Xiuxing, Yang Kun, Shi Zhumei, Qian Xu. (2023) PGC1α Degradation Suppresses Mitochondrial Biogenesis to Confer Radiation Resistance in Glioma. CANCER RESEARCH, 83 (7):(1094-1110). [PMID:36696363][10.1158/0008-5472.CAN-22-3083]
References
1.Reaper PM, Griffiths MR, Long JM, Charrier JD, Maccormick S, Charlton PA, Golec JM, Pollard JR. (2011) Selective killing of ATM- or p53-deficient cancer cells through inhibition of ATR.. Nat Chem Biol, 7 (7):(428-30). [PMID:21490603][10.1021/op500134e]
2.Zhao Mengjie, Li Yanhui, Lu Chenfei, Ding Fangshu, Xu Miao, Ge Xin, Li Mengdie, Wang Zhen, Yin Jianxing, Zhang Junxia, Wang Xiefeng, Ge Zehe, Xiao Hong, Xiao Yong, Liu Hongyi, Liu Wentao, Cao Yuandong, Wang Qianghu, You Yongping, Wang Xiuxing, Yang Kun, Shi Zhumei, Qian Xu. (2023) PGC1α Degradation Suppresses Mitochondrial Biogenesis to Confer Radiation Resistance in Glioma. CANCER RESEARCH, 83 (7):(1094-1110). [PMID:36696363][10.1158/0008-5472.CAN-22-3083]
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E1712148