HSF1 Inhibitor

Rocaglamide (Roc-A) is isolated from the genus Aglaia and can be used for coughs, injuries, asthma and inflammatory skin diseases. Rocaglamide is a potent inhibitor of NF-κB activation in T-cells. Rocaglamide is a potent and selective heat shock factor 1 (HSF1) activation inhibitor with an IC₅₀ of ~50 nM. Rocaglamide inhibits the function of the translation initiation factor eIF4A. Rocaglamide also has anticancer properties in leukemia.

KRIBB11 is an inhibitor of Heat shock factor 1 (HSF1), with IC₅₀ of 1.2 μM.

NXP800 (CCT361814) is a potent and orally active heat shock factor 1 (HSF1) pathway inhibitor. NXP800 has the potential for cancer research.

HSF1-IN-2 (Compound 0048) is a HSF1 inhibitor. HSF1-IN-2 is applicable to cancer research.

Ly101-4B is an apoptosis inducer and multi-target inhibitor with antiproliferative, antitumor and cycytotoxic effects. Ly101-4B reduces HSF1 expression, inhibits microRNA-214 synthesis, downregulates HSP27, HSP70 and HSP90 expression, while suppressing E2F-dependent transcriptional activity and downregulating its target genes. Ly101-4B induces caspase 3/7-mediated apoptosis by reducing DNA synthesis, inhibiting the cell cycle and G1/S phase transition, without affecting RNA synthesis or inducing necrosis. Ly101-4B is selective for pancreatic ductal adenocarcinoma cells with different genotypes and varying degrees of E2F dependence. Ly101-4B can be used in research related to epithelial ovarian cancer and pancreatic ductal adenocarcinoma.

HSF1-IN-3 is a heat shock transcription factor 1 (HSF1) inhibitor with a K_d value of 23.8 μM against HSF1-DBD. HSF1-IN-3 inhibits the proliferation of cancer cells and induces their apoptosis, with stronger activity in androgen-dependent prostate cancer cells. HSF1-IN-3 reduces the expression of HSP70 and HSP90, downstream effectors of HSF1, and attenuates HSE-driven transcriptional activity. HSF1-IN-3 can be used in the research of cancers such as prostate cancer and leukemia.