HSF1A is an activator of Heat shock transcription factor 1 (HSF1).

Rocaglamide（Roc-A）从大青属植物中提取，用于治疗咳嗽、损伤、哮喘和炎症性皮肤病。罗卡格拉酰胺是T细胞中NF-κB激活的强效抑制剂，并且是选择性热休克因子1（HSF1）激活的抑制剂，IC50约为50 nM。它还抑制翻译起始因子eIF4A的功能，并具有抗白血病的抗癌特性。

Geniposidic Acid is a naturally occuring iridoid glucoside HSF1 inducer, with anti-inflammatory and anti-cancer agent.

CCT251236 is a HSF1 pathway inhibitor with IC50 value of 19nM for inhibition of HSF1-mediated HSP72 induction, and a tight-binding ligand of pirin with Kd value of 44nM. It displays efficacy in a human ovarian carcinoma xenograft model.