Chaetocin, a natural product from Chaetomium species, is a histone methyltransferase inhibitor with IC50 of 0.8 μM, 2.5 μM and 3 μM for dSU(VAR)3-9, mouse G9a and Neurospora crassa DIM5, respectively.

DIM5 (neurospora crassa):3 μM, G9a (mouse):2.5 μM, dSU(VAR)3-9:0.8 μM

在SL-2果蝇组织培养细胞中，Chaetocin抑制SU(VAR)3-9活性及Lys9位点上H3分子的二甲基化过程，并且抑制细胞生长。[1] 在人类肝癌细胞HepG2、Hep3B以及Huh7中，Chaetocin抑制由HIF-1介导的低氧反应。[2] Chaetocin还强效抑制广泛癌症细胞系的增殖与群落形成，其IC50值为2-10 nM。[3]

在Hepa 1c1c-7肿瘤携带的小鼠中，Chaetocin（0.25 mg/kg, i.p.）通过破坏HIF-1[alpha]介导的血管生成来抑制肿瘤生长。[2] 在SKOV3肿瘤携带的裸鼠中，Chaetocin治疗（0.25 mg/kg, i.p.）显著延缓肿瘤生长，且毒性较小。[3]

HeLa cells are transfected with 1 μg pcDNA or pcDNA-Trx. Twenty four h after transfection the cells are treated with either DMSO, 100 nM chaetocin or 100 nM doxorubicin for 24 h. The cells are then trypsinized and manually counted in trypan blue to exclude dead cells. For immunoblotting (24 h after transfections), cells are trypsinized, ished in cold PBS, and lysed in CelLytic lysis buffer containing protease inhibitors. Protein is analyzed by BCA assay and lysates are electrophoresed on 15% SDS-PAGE gels and transferred to nitrocellulose. Immunoblotting for thioredoxin and actin is then performed[2].