Powder: -20°C for 3 years | In solvent: -80°C for 1 year
ML323 是一种有效的可逆的USP1-UAF1抑制剂,在Ub-Rho 测定实验中,IC50为 76 nM。在使用 K63 连接的双泛素 (di-Ub) 和单泛素化 PCNA 的正交凝胶测定中(Ub-PCNA)分别作为底物。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 269 | 现货 | ||
5 mg | ¥ 611 | 现货 | ||
10 mg | ¥ 996 | 现货 | ||
25 mg | ¥ 1,980 | 现货 | ||
50 mg | ¥ 3,820 | 现货 | ||
100 mg | ¥ 5,570 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 611 | 现货 |
产品描述 | ML323 is a reversible and effective USP1-UAF1 inhibitor in a Ub-Rho assay (IC50: 76 nM) and in orthogonal gel-based assays using K63-linked diubiquitin (di-Ub) (IC50: 174 nM 820 nM)and monoubiquitinated PCNA (Ub-PCNA) (IC50: 820 nM) as substrates, respectively. |
靶点活性 | USP1-UAF1:76 nM |
体内活性 | 在H596细胞和U2OS骨肉瘤细胞中,ML323以两个主要的DNA损伤应答途径(TLS 和 FA)为靶点,增强顺铂的细胞毒性。通过抑制H596细胞中USP1–UAF1活性,ML323抑制PCNA和ANCD2去泛素化。 |
激酶实验 | High-throughput screening: For HTS, USP1-UAF1 activity is monitored using ubiquitin-rhodamine 110 as a substrate, where hydrolysis of the amide bond between the C-terminal glycine of ubiquitin and rhodamine results in an increase in fluorescence. The assay is miniaturized to a 4 μL volume in a 1,536-well format and is used to screen approximately 402,701 compounds in quantitative HTS mode, with each compound tested over a range of four to five concentrations. The assay shows robust performance with an average Z'factor of 0.8 throughout the screen. |
细胞实验 | For the colony-forming assay, cells are seeded at a density of 300–500 cells per well in six-well plates and grown overnight. Cells are then treated with ML323 alone, cisplatin alone or a combination of cisplatin and ML323 (1:1 or 1:4) at the indicated concentrations. Cells treated with an equal volume of DMSO and saline are used as control. After 48 h of treatment, fresh growth medium is added, and cells are incubated for an additional 5-10 d to allow for colony formation. For UV combination treatment, the cells are treated with ML323 at the indicated concentrations or an equal volume of DMSO. After 48 h, the medium is removed, and cells are irradiated at 254 nm at the indicated dosage. Fresh growth medium is added, and the cells are incubated for an additional 5-10 d to allow for colony formation. The cells without UV irradiation but treated with ML323 or an equal volume of DMSO are used as controls and designated as 100%. After the formation of the colonies, cells are fixed with methanol and stained with 0.5% crystal violet. Colonies consisting of >50 cells are scored. The number of colonies is determined from triplicate plates. The dose-response curves are generated using GraphPad Prism and analyzed by using CalcuSyn to calculate the combination index, which is determined for the fraction of cells affected after the addition of fixed ratios of cisplatin and the USP1-UAF1 inhibitor. (Only for Reference) |
别名 | ML323 |
分子量 | 384.48 |
分子式 | C23H24N6 |
CAS No. | 1572414-83-5 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Ethanol: 38.5 mg/mL (100 mM)
DMSO: 38.5 mg/mL (100 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
Ethanol / DMSO | 1 mM | 2.6009 mL | 13.0046 mL | 26.0092 mL | 65.0229 mL |
5 mM | 0.5202 mL | 2.6009 mL | 5.2018 mL | 13.0046 mL | |
10 mM | 0.2601 mL | 1.3005 mL | 2.6009 mL | 6.5023 mL | |
20 mM | 0.13 mL | 0.6502 mL | 1.3005 mL | 3.2511 mL | |
50 mM | 0.052 mL | 0.2601 mL | 0.5202 mL | 1.3005 mL | |
100 mM | 0.026 mL | 0.13 mL | 0.2601 mL | 0.6502 mL |
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
ML-323 1572414-83-5 Cell Cycle/Checkpoint DNA Damage/DNA Repair Ubiquitination DUB Deubiquitinase ML323 Inhibitor inhibit DUBs ML 323 inhibitor