parp;hdac

PARP-1 HDAC-IN-1 is an effective dual inhibitor of PARP-1 and HDAC6, with IC50 values of 68.90 nM and 510 nM, respectively. PARP-1 HDAC-IN-1 exhibits anti-cancer, anti-migration, and anti-angiogenesis activities.

PARP HDAC-IN-1 is a selective PARP and HDAC inhibitor with potential anticancer activity, inhibits PARP1, PARP2 and HDAC1, and may be used in the study of pancreatic cancer.

Compound A5b, also known as JMJD3 HDAC-IN-1, is a dual inhibitor that targets both JMJD3 (Jumonji domain-containing protein demethylase 3) and HADC1 (histone deacetylase, IC50 = 16 nM). It induces hypermethylation of histone H3K27 and hyperacetylation of H3K9, while also promoting apoptosis through the cleavage of caspase-7 and PARP. This compound has demonstrated the ability to effectively inhibit cancer cell cloning, migration, and invasion [1].

B102 (PARP HDAC-IN-1) is a dual inhibitor of PARP and HDAC, exhibiting IC50 values of 19.01 nM for PARP1, 2.13 nM for PARP2, 1.69 μM for HDAC1, and greater than 10 μM for HDAC6 in enzymatic assays. It possesses antiproliferative and antitumor properties and induces DNA damage and apoptosis in vitro.

DLC-50 is a dual inhibitor of PARP-1 and HDAC-1, exhibiting IC50 values of 1.2 nM and 31 nM respectively. It hinders the proliferation of cancer cells such as MDA-MB-436, MDA-MB-231, and MCF-7 with IC50 values of 0.3 μM, 2.7 μM, and 2.41 μM respectively. Additionally, DLC-50 induces apoptosis in MDA-MB-231 cells and causes cell cycle arrest at the G2 phase.