| 名稱 | 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. |
| 細(xì)胞實(shí)驗(yàn) | 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. |
| 激酶實(shí)驗(yàn) | 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. |
| 動(dòng)物實(shí)驗(yàn) | Animal Models: xenograft mouse models of cancer. Formulation: water. Dosages: 30 mg/kg. Administration: p.o. |
| 體外活性 | 方法：CBL0137 hydrochloride (Curaxin-137 hydrochloride) （0, 1，3,10μM，24h）處理的 HUVECs 和 HAEC 的細(xì)胞，使用 CCK-8 檢測試劑盒檢測細(xì)胞活力。
結(jié)果：超過1μM的 CBL0137 hydrochloride (Curaxin-137 hydrochloride) 會(huì)使HUVECs和HAEC的存活率降低。[1] |
| 體內(nèi)活性 | 方法：ApoE?/?小鼠服用 CBL0137 hydrochloride (Curaxin-137 hydrochloride) （1mg/kg, 口服，三周），觀察 CBL0137 hydrochloride (Curaxin-137 hydrochloride) 動(dòng)脈粥樣硬化小鼠模型的影響并進(jìn)行了Westernblot實(shí)驗(yàn)。
結(jié)果：CBL0137 hydrochloride (Curaxin-137 hydrochloride) 可減輕部分結(jié)扎后頸動(dòng)脈粥樣硬化斑塊的形成；CBL0137 hydrochloride (Curaxin-137 hydrochloride) 治療下調(diào)了這些動(dòng)脈中 p-YAP （Y357） 和 p-Src （Y416） 的蛋白質(zhì)水平，以及炎癥基因 MCP-1 和 VCAM-l。[1] |
| 存儲條件 | 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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| 關(guān)鍵字 | 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 |
| 相關(guān)產(chǎn)品 | D-Psicose | Uridine | Sodium propionate | Ethyl palmitate | 1,4-Naphthoquinone | Flubendazole | Glucosamine | Fumaric acid | Kojic acid | Magnesium sulfate | Ethyl linoleate | N,N-Dimethylacetamide |
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