ROCK/HDAC-IN-1 (Compound 10h) serves as an orally effective inhibitor of ROCK/HDAC. This compound suppresses ROCK1/2 (IC50: 254.9 nM, 58.18 nM) and HDAC1/2/3/6/8 (IC50: 9.09, 8.03, 6.26, 0.41, 7.69 nM). It stimulates the activation of DAMPs, notably calreticulin (CRT) exposure and HMGB1 release, suggesting its potential as an inducer of immunogenic cell death (ICD). ROCK/HDAC-IN-1 exhibits antiproliferative effects against breast cancer cells (IC50: 0.37 µM for MDA-MB-231 cells), inhibits tumor growth, activates T cells, and shows no significant toxicity.
Molekulargewicht:
386.47
Formel:
C19H22N4O3S
Target-Kategorie:
ROCK|||Epigenetic Reader Domain|||HDAC
T201708
* Mehrwertsteuer und Versandkosten nicht enthalten. Irrtümer und Preisänderungen vorbehalten
