| 名称 | CBL0137 hydrochloride |
| 描述 | CBL0137 hydrochloride (Curaxin-137 hydrochloride) is an inhibitor of the histone chaperone FACT, which also activates p53 and inhibits NF-κB with EC50 values of 0.37 and 0.47 μM, respectively. CBL0137 hydrochloride functionally inactivates the complex that promotes chromatin transcription (FACT), thereby driving effects on p53 and NF-κB and promoting cancer cell death, and when used in combination with cisplatin, CBL0137 hydrochloride has potent anticancer activity against SCLC. |
| 细胞实验 | Effects of CBLC137 (2 μM for 24 hours) on cell cycle in tumor (HT1080, RCC45, MiaPaca) and normal cells (Wi38, NKE-hTERT) are examined using FACS analysis of propidium iodide-stained cells. |
| 激酶实验 | MiaPaca2 and BxPC-3 cells are treated with CBL0137 hydrochloride for 4 or 24 h. Cells are harvested in 1× Cell Culture Lysis Reagent containing protease and phosphatase inhibitors. Lysates 5 to 20 μg are separated on SDS-PAGE gels and transferred to PVDF membranes. Blots are probed with antibodies specific for SSRP1, SPT16, RRM1, and RRM2. |
| 动物实验 | Animal Models: xenograft mouse models of cancer. Formulation: water. Dosages: 30 mg/kg. Administration: p.o. |
| 体外活性 | 方法：CBL0137 hydrochloride (Curaxin-137 hydrochloride) （0, 1，3,10μM，24h）处理的 HUVECs 和 HAEC 的细胞，使用 CCK-8 检测试剂盒检测细胞活力。
结果：超过1μM的 CBL0137 hydrochloride (Curaxin-137 hydrochloride) 会使HUVECs和HAEC的存活率降低。[1] |
| 体内活性 | 方法：ApoE−/−小鼠服用 CBL0137 hydrochloride (Curaxin-137 hydrochloride) （1mg/kg, 口服，三周），观察 CBL0137 hydrochloride (Curaxin-137 hydrochloride) 动脉粥样硬化小鼠模型的影响并进行了Westernblot实验。
结果：CBL0137 hydrochloride (Curaxin-137 hydrochloride) 可减轻部分结扎后颈动脉粥样硬化斑块的形成；CBL0137 hydrochloride (Curaxin-137 hydrochloride) 治疗下调了这些动脉中 p-YAP （Y357） 和 p-Src （Y416） 的蛋白质水平，以及炎症基因 MCP-1 和 VCAM-l。[1] |
| 存储条件 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. |
| 溶解度 | Ethanol : < 1 mg/mL (insoluble or slightly soluble)
10% DMSO+40% PEG300+5% Tween 80+45% Saline : 2 mg/mL (5.36 mM), Sonication is recommended.
H2O : 25 mg/mL (67.05 mM), Sonication is recommended.
DMSO : 36 mg/mL (96.55 mM), Sonication is recommended.
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| 关键字 | p53 | NF-κB | NFκB | NF-kB | NFkB | MDM-2/p53 | FACT | Curaxin-137 | Curaxin137 | Curaxin 137 | CBL-C-137 Hydrochloride | CBLC-137 | CBL-C137 | CBLC137 | CBL-C 137 Hydrochloride | CBLC 137 | CBL-0137 | CBL 0137 Hydrochloride | CBL 0137 |
| 相关产品 | Uridine | Lactose | Ethyl palmitate | 1,4-Naphthoquinone | Flubendazole | Glucosamine | Fumaric acid | Chitin | Kojic acid | Magnesium sulfate | Ethyl linoleate | N,N-Dimethylacetamide |
| 相关库 | 抑制剂库 | 抗癌活性化合物库 | 经典已知活性库 | 已知活性化合物库 | 临床失败化合物库 | 细胞凋亡化合物库 | 抗衰老化合物库 | NO PAINS 化合物库 | 免疫/炎症分子化合物库 | 药物功能重定位化合物库 | 抗癌临床化合物库 | 抗癌药物库 |