LTURM34 shows potent inhibition of DNA-PK (IC50 0.034 μM) with excellent selectivity over the Class I PI3K isoforms (IC50 all > 5 μM) and inhibits the proliferation of a wide range of tumor cell lines.
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产品名称 | DNA-PK ↓ ↑ | 其他靶点 | 纯度 | ||||||||||||||||
---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
PI-103 |
++
DNA-PK, IC50: 23 nM |
99%+ | |||||||||||||||||
CC-115 |
+++
DNA-PK, IC50: 0.013 μM |
mTOR | 98+% | ||||||||||||||||
Samotolisib | ✔ | 99%+ | |||||||||||||||||
NU 7026 |
+
DNA-PK, IC50: 0.23 μM |
PI3K | 98+% | ||||||||||||||||
PIK-75 HCl |
++++
DNA-PK, IC50: 2 nM |
99%+ | |||||||||||||||||
PP121 |
+
DNA-PK, IC50: 60 nM |
PDGFR,VEGFR | 99%+ | ||||||||||||||||
KU-0060648 |
++++
DNA-PK, IC50: 5 nM |
99% | |||||||||||||||||
KU-57788 |
+++
DNA-PK, IC50: 14 nM |
99%+ | |||||||||||||||||
LTURM34 |
++
DNA-PK, IC50: 0.034 μM |
98%+ | |||||||||||||||||
SF2523 |
+++
DNA-PK, IC50: 9 nM |
99%+ | |||||||||||||||||
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。 |
靶点 |
|
描述 | DNA-dependent protein kinase (DNA-PK) is a very large holoenzyme comprised of the p470 kDa DNA-PK catalytic subunit (DNA-PKcs) and the Ku heterodimer consisting of the p86 (Ku 80) and p70 (Ku 70) subunits. It is best known for its nonhomologous end joining (NHEJ) activity, which repairs double-strand DNA (dsDNA) breaks (DSBs)[1]. LTURM34 is a specific DNA-PK inhibitor with an IC50 value of 34 nM, and it exhibits 170-fold selectivity for DNA-PK over phosphoinositide 3-kinase (PI3K). The IC50s are 5.8 and 8.5 μM for PI3K β and δ, respectively[2]. LTURM34 was more consistently active against the selected cell lines compared with its analogues, but at best showed 54% inhibition against the HOP-92 non-small cell lung cancer line[2] |
作用机制 | Mechanism: LTURM34 could govern the strength of the interaction of the ring carbonyl with the Lys124 of DNA-PK as compared. |
计算器 | ||||
存储液制备 | 1mg | 5mg | 10mg | |
1 mM 5 mM 10 mM |
2.41mL 0.48mL 0.24mL |
12.06mL 2.41mL 1.21mL |
24.13mL 4.83mL 2.41mL |
CAS号 | 1879887-96-3 |
分子式 | C24H18N2O3S |
分子量 | 414.476 |
别名 | |
运输 | 蓝冰 |
存储条件 |
液体 -20°C:3-6个月-80°C:12个月 粉末 Sealed in dry,2-8°C |
溶解度 |
DMSO: 65 mg/mL(156.82 mM),配合低频超声助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO |
动物实验配方 |