Chetomin (BRN0077366) is an inhibitor of HIF-1 by weaken transcription of HIF-1, disrupting the binding of HIF-1α and HIF-2α to p300 at low nanomolar concentrations.

HIF-1（缺氧诱导因子1）是一种转录因子，能够响应细胞环境氧气的变化[2]。Chetomin通过破坏HIF-1与其转录共激活因子p300的相互作用，选择性地抑制HIF-1活性。通过Chetomin抑制HIF-1，有效降低了缺氧依赖的转录，并使缺氧的HT 1080人类成纤维细胞瘤细胞体外辐射敏化[1]。Chetomin减轻了恶性胶质瘤细胞系U251 mg（DMF10：1.35和1.18）和U343 mg（DMF10：1.78和1.48）的缺氧诱导的放射抗性[3]。使用Chetomin针对HIF-1，消除了缺氧诱导因子-1α的分化抑制效应[4]。

在体内异种移植模型中，联合使用chetomin和forskolin显著抑制恶性胶质瘤的生长[4]。Che-M（装载chetomin的胶束）在斑马鱼中显著抑制胚胎血管生成、肿瘤诱导的血管生成和肿瘤生长。在小鼠模型中，Che-M抑制肿瘤生长并延长皮下CT26肿瘤模型中的生存期[5]。

In RT-PCR and clonogenic survival experiments, chetomin is added in a concentration of 150 nM to fully supplemented medium four hours before treatment with hypoxia. HT 1080 cells are then transferred to the hypoxic workstation (0.1% O2, 12 h) or to the well-humidified incubator (12 hours) without changing medium. HT1080 cells are thus treated for 16 hours with chetomin (150 nM) prior to radiation treatment. (Only for Reference)