Table 2.

Small molecular compounds that inhibit HSF1 activity.

Selective Compounds	Effect on HSF1	Mechanism of Action	References
KNK437	↓HSP expression	Unknown	[97]
KNK423	↓HSP expression	Unknown	[101]
“Compound 1”	↓HSF1 phosph. and HSP expression	Unknown	[103]
KRIBB11	↓HSF1-induced transcription	Binds to transactivation domain, prevents pTEFb recruitment	[54, 104–106]
Ly101-4b	↓HSF1 protein levels and HSP expression	Unknown	[108, 125]
Rohinitib (RHT)	↓HSE binding and HSP expression	Binds to DNA binding domain to prevent HSE binding	[83, 110]
PW3405	↓HSF1 phosph.	Unknown	[111]
CCT251236	↓HSP expression	Unknown	[112]
IHSF115	↓HSF1 binding to HSE and HSP expression	Binds DNA binding domain to prevent HSE binding	[113]
HSF1 RNA Aptamer	↓HSE binding and HSP expression	Binds DNA binding domain to prevent HSE binding	[114–117]
Natural Compounds
Quercetin	↓HSF1 phosph. and HSE binding	Unknown	[83, 118, 126]
Triptolide	↓HSP expression and transactivation	Inhibits HSF1-induced transcription activation	[83, 119, 120]
Rocaglamide A	↓HSE binding and HSP expression	Binds to DNA binding domain to prevent HSE binding	[83]