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.

p53:0.37 μM(EC50), NF-κB:0.47 μM(EC50), FACT:

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]

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]

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.

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.

Animal Models: xenograft mouse models of cancer. Formulation: water. Dosages: 30 mg/kg. Administration: p.o.