elk1

TD52 is an orally active inhibitor of cancerous inhibitor of PP2A (CIP2A). TD52 is an Erlotinib derivative and indirectly reduced CIP2A by disturbing Elk1 binding to the CIP2A promoter.

TAT-DEF-Elk-1 is a cell-penetrating peptide Elk-1 inhibitor.

TAT-DEF-Elk-1 acetate is a cell-penetrating peptide inhibitor of ERK1/2 kinase phosphorylated Elk-1 with antitumor and antidepressant activity.TAT-DEF-Elk-1 acetate inhibits the phosphorylation of Elk-1, inhibits Elk-1 nuclear TAT-DEF-Elk-1 acetate inhibits Elk-1 phosphorylation and Elk-1 nuclear translocation, and can be used to study depression.

Darizmetinib (HRX215, HRX-0215) is an MKK4 inhibitor. Inhibition of MKK4 leads to enhancement of the MKK7 and JNK1 signaling pathways, thereby activating the transcription factors ATF2 and ELK1, promoting cell proliferation and liver regeneration.

TD52 dihydrochloride (TD52 2HCl), a derivative of Erlotinib, is a potent and orally active inhibitor of protein phosphatase 2A (CIP2A). It exhibits strong anti-cancer properties by regulating the CIP2A/PP2A/p-Akt signaling pathway, resulting in the induction of apoptosis in triple-negative breast cancer (TNBC) cells. Mechanistically, TD52 dihydrochloride disrupts the binding of Elk1 to the CIP2A promoter, effectively reducing CIP2A levels. Notably, TD52 dihydrochloride demonstrates powerful anti-cancer activity while displaying less inhibition of p-EGFR.

TAT-DEF-Elk-1 TFA is a cell-penetrating peptide Elk-1 inhibitor, mimics and specifically interferes with the DEF domain of Elk-1. TAT-DEF-Elk-1 blocks Elk-1 phosphorylation and prevents Elk-1 nuclear translocation without interfering with ERK nor MSK1 act