I-BET151 is an inhibitor of bromodomain and extra-terminal domain (BET) proteins that selectively inhibits BET family members (BRD2, BRD3, BRD4, and BRDT). Over the past ten years, many studies have demonstrated the potential of I-BET151 in cancer treatment. Specifically, I-BET151 causes cell cycle arrest and inhibits tumor cell proliferation in some hematological malignancies and solid tumors, such as breast cancer, glioma, melanoma, neuroblastoma, and ovarian cancer. The anticancer activity of I-BET151 is related to its effects on NF-κB, Notch, and Hedgehog signal transduction pathway, tumor microenvironment (TME) and telomere elongation. Remarkably, the combination of I-BET151 with select anticancer drugs can partially alleviate the occurrence of drug resistance in chemotherapy. Especially, the combination of forskolin, ISX9, CHIR99021, I-BET151 and DAPT allows GBM cells to be reprogrammed into neurons, and this process does not experience an intermediate pluripotent state. The research on the anticancer mechanism of I-BET151 will lead to new treatment strategies for clinical cancer.

中文翻译：

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I-BET151 的抗癌作用，溴结构域和末端结构域蛋白的抑制剂。

I-BET151 是溴结构域和末端外结构域 (BET) 蛋白的抑制剂，可选择性抑制 BET 家族成员（BRD2、BRD3、BRD4 和 BRDT）。在过去十年中，许多研究证明了 I-BET151 在癌症治疗中的潜力。具体而言，I-BET151 会导致细胞周期停滞并抑制某些血液系统恶性肿瘤和实体瘤中的肿瘤细胞增殖，例如乳腺癌、神经胶质瘤、黑色素瘤、神经母细胞瘤和卵巢癌。I-BET151 的抗癌活性与其对 NF-κB、Notch 和 Hedgehog 信号转导通路、肿瘤微环境 (TME) 和端粒伸长的影响有关。值得注意的是，I-BET151与精选抗癌药物的联合应用可以部分缓解化疗耐药的发生。特别是毛喉素、ISX9、CHIR99021的组合，I-BET151 和 DAPT 允许 GBM 细胞重新编程为神经元，并且该过程不会经历中间多能状态。I-BET151抗癌机制的研究将为临床癌症带来新的治疗策略。