ATM 选择性抑制剂 | 激活剂

目录号 产品名 产品描述 Selective / Pan IC50 / Ki
S8375 AZD0156

AZD0156是有效的、选择性的ATM激酶抑制剂,具有潜在的化疗/辐射增敏和抗肿瘤活性。

Selective
S8680 AZD1390

AZD1390 is a first-in-class orally available and CNS penetrant ATM inhibitor with an IC50 of 0.78 nM in cells and >10,000-fold selectivity over closely related members of the PIKK family of enzymes and excellent selectivity across a broad panel of kinases.

Selective ATM, IC50: 0.78 nM
S8729 AZ32

AZ32 is a specific inhibitor of the ATM kinase that possesses good BBB penetration in mouse with an IC50 value of <0.0062 μM for ATM enzyme. It shows adequate selectivity over ATR and also has high cell permeability.

Selective ATM, IC50: <0.0062 μM
S1570 KU-60019

KU-60019是一种改进的KU-55933类似物,在无细胞试验中作用于ATMIC50为6.3 nM,作用于ATM比作用于DNA-PK和ATR的选择性分别高270和1600倍,并且是高度有效的放射增敏剂。

Selective ATM, IC50: 6.3 nM
S1092 KU-55933 (ATM Kinase Inhibitor)

KU-55933 (ATM Kinase Inhibitor)是一种有效的,特异性ATM抑制剂,在无细胞试验中IC50/Ki为12.9 nM/2.2 nM,与DNA-PK, PI3K/PI4K, ATR和mTOR相比,对ATM具有高度选择性。

Selective ATM, IC50: 12.9 nM
S2758 Wortmannin (KY 12420)

Wortmannin是一种首次命名的PI3K抑制剂,在无细胞试验中IC50为3 nM,对 PI3K 家族的选择性较低。也会抑制自噬体的形成,并有效抑制DNA-PK/ATM,在无细胞试验中IC50为16 nM和150 nM。

Selective ATM, IC50: 150 nM
S2245 CP-466722

CP-466722是一种有效的,可逆的ATM抑制剂,不影响ATR,且抑制PI3K或PIKK家族成员。

Selective ATM, IC50: 410 nM
S8096 Mirin

Mirin是有效的Mre11–Rad50–Nbs1(MRN)复合体抑制剂,能够抑制Mre11相关的外切酶活性。

Selective
S8556 AZ31

AZ31 is a selective and novel ATM inhibitor with an IC50 of <0.0012 μM. It shows excellent selectivity over closely related enzymes (>500 fold selective over DNA-PK and PI3Kα and >1000 fold selective over mTOR, PI3Kβ and PI3Kγ).

Selective
S4157 Chloroquine diphosphate

Chloroquine Phosphate是一种4-氨基喹啉的抗疟疾和抗风湿药,也是一种ATM激活剂。

Selective
S3224 Cinobufagin

Cinobufagin (Cinobufagine), an active ingredient of Venenum Bufonis, inhibits tumor development. Cinobufagin increases ATM and Chk2 and decreases CDC25C, CDK1, and cyclin B. Cinobufagin inhibits PI3K, AKT and Bcl-2 while increases levels of cleaved caspase-9 and caspase-3. Thus, Cinobufagin induces cell cycle arrest at the G2/M phase and apoptosis.

Selective
S2817 Torin 2

Torin 2 是一种有效的选择性mTOR抑制剂,在p53−/− MEFs细胞系中IC50为0.25 nM;作用于mTOR比作用于PI3K选择性高800倍,并且改善了药代动力学性能。抑制ATM/ATR/DNA-PK,在PC3细胞系中EC50分别为28 nM/35 nM/118 nM。

Pan ATM, EC50: 28 nM
S7136 CGK 733

CGK 733是一种有效的ATM/ATR选择性抑制剂,IC50约为200 nM。

Pan ATM, IC50: 200 nM
S8050 ETP-46464

ETP-46464是一种有效的,选择性ATR抑制剂,IC50为25 nM。

Pan ATM, IC50: 545 nM