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- 详细信息
- 文献和实验
- 技术资料
- 保存条件:
Powder:2-8℃,2 years;Insolvent(母液):-20℃,6 months;-80℃,1 year
- 保质期:
Powder:2-8℃,2 years;Insolvent(母液):-20℃,6 months;-80℃,1 year
- 英文名:
ML367
- 库存:
现询
- 供应商:
北京索莱宝科技有限公司
- CAS号:
381168-77-0
- 规格:
25mg/10mg/5mg/50mg
| 规格: | 25mg | 产品价格: | ¥1590.0 |
|---|---|---|---|
| 规格: | 10mg | 产品价格: | ¥790.0 |
| 规格: | 5mg | 产品价格: | ¥490.0 |
| 规格: | 50mg | 产品价格: | ¥2240.0 |
| 基本信息 | |
| CAS | No.381168-77-0 |
| 英文名称 | ML367 |
| 分子式 | C19H12F2N4 |
| 分子量 | 334.32 |
| 溶解性 | Soluble in DMSO |
| 纯度 | ≥98% |
| 外观(性状) | Solid |
| 储存条件 | Powder:2-8℃,2 years;Insolvent(母液):-20℃,6 months;-80℃,1 year |
| SMILES | C1=CC=C2C(=C1)C(=NC(=N2)C3=CC=NC=C3)NC4=CC(=C(C=C4)F)F |
| InChIKey | LBPYNNJXARHGAG-UHFFFAOYSA-N |
| InChI | InChI=1S/C19H12F2N4/c20-15-6-5-13(11-16(15)21)23-19-14-3-1-2-4-17(14)24-18(25-19)12-7-9-22-10-8-12/h1-11H,(H,23,24,25) |
| PubChem CID | 921541 |
| 靶点 | ATAD5 |
| 通路 | Others |
| 背景说明 | ML367 是一种 ATPase 家族 AAA 结构域蛋白 5 (ATAD5) 稳定的有效抑制剂。ML367 阻断 DNA 的修复通路,抑制一般的 DNA 损伤反应。 |
| 生物活性 | ML367 is a potent inhibitor of ATPase family AAA domain-containing protein 5 (ATAD5) stabilization, acts as a probe molecule that has low micromolar inhibitory activity. ML367 blocks DNA repair pathways, suppresses general DNA damage responses including RPA32-phosphorylation and CHK1-phosphorylation in response to UV irradiation[1]. |
| In Vitro | Identification of pathway(s) that stabilize ATAD5 protein levels in response to DNA damage and inhibitors of these pathway(s) would be beneficial to understanding a novel mechanism involved in the DNA damage response and introduce a new therapeutic approach for sensitizing cancer cells, respectively. However, no chemical matter is currently known that perturbs ATAD5 function. To understand the biology of ATAD5 and to evaluate its therapeutic potential, we conducted a quantitative high throughput screening campaign and subsequent medicinal chemistry optimization in pursuit of small molecules that destabilize ATAD5. Herein, we detail the discovery of ML367, a probe molecule that has low micromolar inhibitory activity in the ATAD5 destabilizer screen run with 10 μM 5-fluorouridine (5-FUrd) as the DNA damaging agent. Interestingly, ML367 was found to block general DNA damage responses including RPA32-phosphorylation and CHK1-phosphorylation in response to UV irradiation.[1]Western Blot Analysis[1]:Cell Line:HEK293T cells;Concentration:0-40 μM in the presence or absence of 20 μM 5-Furd;Incubation Time:16 hours;Result:Inhibited the increased ATAD5 protein levels induced by 5-Furd. |
| 数据来源文献 | [1]. Rohde JM, et al. Discovery of ML367, inhibitor of ATAD5 stabilization. Probe Reports from the NIH Molecular Libraries Program. |
| 单位 | 瓶 |
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文献和实验直接IM―PCR (以rhIL-3的检测为例) 【试剂与配制】 TBS:20mmol/L Tris-HCl(pH7.4),150mmoI/L NaCL 封闭液:1.5% BSA (用TBS配制) 抗hIL-3单抗 生物素化羊抗鼠IgG 亲合素 DNA指示分子(生物素―AdAT) PCR反应液:5×PCR缓冲液10μl,dNTP 4μl,引物4μl,EP-DNA聚合酶0.5μl,蒸馏水31.5μl 【操作方法】 (1) 用TBS稀释rhIL-3至6.0μg
1 试剂 包被缓冲液:20mmol/L Tris-HCI(pH9.5),含150mmol/L NaCl和0.02%NaN3; 洗涤液:20mmol/L Tris-HCI(pH7.5),含150mmol/LNaCl0.1mmol/L EDTA和0.1%Tween20; 稀释液:20mmol/L Tris-HCI(pH7.5),含150mmol/L NaCl0.45%脱脂奶及变性鲑鱼精DNA (0.1mg/ml) 2 操作 1)包被 用包被缓冲液稀释抗原
免疫PCR(IM-PCR)注意事项 (1)固相载体的选择:主要取决于抗原在固相载体上的吸附程度。如果抗原吸附良好,可以进行IM-PCR。如果抗原吸附不良,则需选用双抗体夹心IM―PCR。另外选用的固相载体要和PCR仪器相匹配。一般用0.5ml的塑料反应管,也可以用微量滴定板。 (2)待检抗原的特异性抗体:这是决定本法特异性和敏感性的关键试剂,使用相应的McAb为宜。将抗体进行生物素标记后,可用于直接IM―PCR,或以生物素化的二抗
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