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 |
VEGFR,PDGFR | 99%+ | ||||||||||||||||
| KU-0060648 |
++++
DNA-PK, IC50: 5 nM |
98% | |||||||||||||||||
| 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 | 414.48 |
| SMILES Code | O=C1N=C(N2CCOCC2)OC3=C(C4=C5C(C6=CC=CC=C6S5)=CC=C4)C=CC=C13 |
| MDL No. | MFCD30536366 |
| 别名 | |
| 运输 | 蓝冰 |
| InChI Key | SMMSWOMXOZLOPI-UHFFFAOYSA-N |
| Pubchem ID | 122705987 |
| 存储条件 |
In solvent -20°C: 3-6个月 -80°C: 12个月 Pure form Sealed in dry, 2-8°C |
| 溶解方案 |
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 以下溶解方案都请先按照体外实验的方式配制澄清的储备液,再依次添加助溶剂: ——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议现用现配,当天使用; 以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶
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