Activators & Inhibitors

Juglone (Regianin) is a natural naphthoquinone found in the black walnut (J. nigra) and other plants in the Juglandaceae family. Juglone also irreversibly inhibits peptidyl-prolyl cis/trans isomerases of the parvulin family, including human Pin1, yeast Ess1/Ptf1, and E. coli parvulin (Ki = 55.9 nM). Juglone also blocks transcription by RNA polymerases I, II, and III (IC50s = 2-7 μM) and attenuates kidney fibrosis in rats treated with unilateral ureteral obstruction, both through Pin1-independent mechanisms.

Sobetirome (IACS-010759) is a selective agonist of thyroid hormone receptor β (TRβ) and binds selectively to TRβ-1 (EC50: 0.16 μM).

KPT-6566 is a novel selective covalent pin1 inhibitor, KPT-6566 shows an IC50 of 640 nM and a Ki of 625.2 nM for PIN1 PPIase domain,and has anti-cancer activity.

GDC-0941, also known as Pictilisib, is a phosphatidylinositol 3-kinase (PI3K) inhibitor

Staurosporine is a potent inhibitor of many kinases including protein kinase C, protein kinase A, and protein kinase G. It also induces apoptosis in human neuroblastoma cell lines and chick embryonic neurons.

AZD2281, also known as Olaparib, is a poly(ADP-ribose) polymerase 1 (PARP1) inhibitor and an anti-cancer drug being tested in patients with mutations in the genes BRCA1 or BRCA2.

Rolipram is a selective, cell permeable inhibitor of cAMP-specific phosphodiesterase 4 (PDE4). PDE4 enzymes inactivate cyclic AMP (cAMP) via hydrolysis to 5'-AMP. Rolipram has two enantiomeric forms, R(-) and S(+). This product is the racemic mixture of the two enantiomers.

Soruberoylanilide Hydroxamic Acid (SAHA), or Vorinostat, is a histone deacetylase inhibitor and causes growth arrest and death of some transformed cells both in vitro and in vivo, with little or no toxic effects on normal cells.

Geldanamycin is an antibiotic and a potent antitumor compound. It inhibits pp60src tyrosine kinase, and it also binds specifically to heat shock protein Hsp90 and its GP96 homologue. It is known to inhibit protein maturation.