| 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 | METHODS: HUVECs and HAECs cell treated with CBL0137 hydrochloride (Curaxin-137 hydrochloride) (0, 1, 3, 10 μM, 24 h) were tested for cell viability using the CCK-8 assay kit.
RESULTS CBL0137 hydrochloride (Curaxin-137 hydrochloride) above 1 μM reduced the survival rate of HUVECs and HAECs. [1] |
| 体内活性 | METHODS: ApoE−/− mice were treated with CBL0137 hydrochloride (Curaxin-137 hydrochloride) (1 mg/kg, oral, for three weeks) to observe the effects of CBL0137 hydrochloride (Curaxin-137 hydrochloride) on the atherosclerosis mouse model and perform Western blot experiments.
RESULTSCBL0137 hydrochloride (Curaxin-137 hydrochloride) can reduce the formation of atherosclerotic plaques in partially ligated carotid arteries;CBL0137 hydrochloride (Curaxin-137 hydrochloride) treatment downregulated the protein levels of p-YAP (Y357) and p-Src (Y416) in these arteries, as well as the inflammatory genes MCP-1 and VCAM-1. [1] |
| 存储条件 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| 溶解度 | Ethanol : < 1 mg/mL (insoluble or slightly soluble)
H2O : 25 mg/mL (67.05 mM), Sonication is recommended.
DMSO : 36 mg/mL (96.5 mM)
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| 关键字 | CBL0137 hydrochloride | Curaxin-137 | Nuclear factor-κB | CBL-C 137 Hydrochloride | inhibit | CBL0137 Hydrochloride | Inhibitor | CBL-0137 Hydrochloride | Curaxin137 | CBL-C137 | CBL 0137 | Nuclear factor-kappaB | NF-κB | CBLC 137 | MDM-2/p53 | CBL-0137 | CBL-0137 hydrochloride | Curaxin-137 Hydrochloride | CBL-C-137 Hydrochloride | CBL-C137 Hydrochloride | CBLC-137 | CBL 0137 Hydrochloride |
| 相关产品 | Rotenone | Sodium Houttuyfonate | Lidocaine | Diethylmaleate | Glucosamine | sodium lauroyl-α-hydroxyethyl sulfonate | Lidocaine hydrochloride | 5-Aminosalicylic Acid | Indole-3-carbinol | Diallyl disulfide | Caffeic Acid Phenethyl Ester | Sodium salicylate |
| 相关库 | 抗结直肠癌化合物库 | 经典已知活性库 | HIF-1化合物库 | 抗癌临床化合物库 | 药物功能重定位化合物库 | 抑制剂库 | 抗衰老化合物库 | 已知活性化合物库 | 抗癌药物库 | 抗癌活性化合物库 |
United States
