ac1 in 1

AC1-IN-1 is a selective inhibitor of adenylyl cyclase type 1 (AC1, IC50 = 0.54 µM).

IMPDHII/HDAC1-IN-1 (Compound C12) is an orally active dual inhibitor targeting IMPDHII and HDAC1, with IC50 values of 84.69 nM and 81.75 nM, respectively. It exhibits significant antitumor activity by inhibiting proliferation of K-562 cells (IC50 = 305.31 nM). By simultaneously targeting IMPDHII and HDAC1, this compound demonstrates a synergistic antitumor effect, suppressing tumor cell proliferation and inducing apoptosis. IMPDHII/HDAC1-IN-1 can be utilized in the study of cancers such as chronic myeloid leukemia (CML).

VEGFR2/HDAC1-IN-1 (compound 13) is a potent dual inhibitor of VEGFR-2 and HDAC, with IC50 values of 57.83 nM for VEGFR-2 and 9.82 nM for HDAC. It arrests the cell cycle at the S and G2 phases and induces apoptosis in HeLa cells, demonstrating an anti-angiogenic effect [1].

Casein kinase1δ-IN-29 (Compound 18) is an inhibitor that targets p38α and casein kinase 1 (CK1), exhibiting inhibitory effects on p38α, CK1δ, and CK1ε with IC50 values of 0.041 µM, 0.005 µM, and 0.447 µM, respectively. This compound causes cell cycle arrest at the subG1 phase and induces apoptosis in AC1-M88 cells.