ITSA-1 is an activator of histone deacetylase (HDAC), and counteract trichostatin A (TSA)-induced cell cycle arrest, histone acetylation, and transcriptional activation^[1]. IC50 & Target: HDAC^[1] In Vitro: ITSA1 (50 μM; A549 cells) treatment serves to revert the TSA-arrested population to a normal cell cycle distribution. ITSA1 is also able to effect cell cycle rescue over longer duration^[1].
ITSA1 (50 μM; 5 hours; A549 cells) treatment reduces the number of apoptosis in TSA-treated cells^[1].
ITSA1 (50 μM; 2 hours; A549 and murine ES cells cells) treatment suppresses TSA-induced histone acetylation. Importantly, suppression of acetylation levels is only observable when ITSA1 is added concurrent with or post TSA treatment^[1].
ITSA1 (50 μM; 30 minutes; murine ES cells cells) suppresses TSA-activated transcription in murine ES cells^[1]. In Vivo: ITSA-1 (0.5 mg/kg; intraperitoneal injection; 3 times/week; for 8 weeks; CBS^+/− mice) treatment balances deacetylation activity and suppresses IL-6 and TNF-α expression and thereby attenuated histone acetylationdependent infammatory signaling^[2].