MC 1742

MC1742 is a potent HDAC inhibitor, with IC50s of 0.1 μM, 0.11 μM, 0.02 μM, 0.007 μM, 0.61 μM, 0.04 μM and 0.1 μM for HDAC1, HDAC2, HDAC3, HDAC6, HDAC8, HDAC10 and HDAC11, respectively. MC1742 can increase acetyl-H3 and acetyl-tubulin levels and inhibits cancer stem cells growth. MC1742 can induce growth arrest, apoptosis, and differentiation in sarcoma CSC[1].

Signaling Pathways >> Apoptosis >> Apoptosis

Research Areas >> Cancer

Signaling Pathways >> Cell Cycle/DNA Damage >> HDAC

Signaling Pathways >> Epigenetics >> HDAC

HDAC1:0.1 μM (IC50)

HDAC2:0.11 μM (IC50)

HDAC3:0.02 μM (IC50)

HDAC6:0.007 μM (IC50)

HDAC8:0.61 μM (IC50)

HDAC10:0.04 μM (IC50)

HDAC11:0.1 μM (IC50)

MC1742 (compound 1) (0.5 and 2 μM; 24 hours) increases acetylation in a dose-dependent manner, observable as punctuate nuclear staining of acetyl-histone H3[1]. MC1742 (0.5, 1 and 2 μM; 24, 48 and 72 hours) significantly induces apoptosis of all CSC cultures[1]. MC1742 (0.025-0.5 μM; 14 days) enhances bone nodule formation in a significant dose-dependent manner[1]. Immunofluorescence Cell Line: Sarcoma cancer stem cells[1] Concentration: 0.5 and 2 μM Incubation Time: 24 hours Result: Increased acetylation in a dose-dependent manner, observable as punctuate nuclear staining of acetyl-histone H3. Apoptosis Analysis Cell Line: Sarcoma cancer stem cells[1] Concentration: 0.5, 1 and 2 μM Incubation Time: 24, 48 and 72 hours Result: Significantly induced apoptosis of all CSC cultures. Cell Differentiation Assay Cell Line: Sarcoma cancer stem cells[1] Concentration: 0.025, 0.05, 0.1 and 0.5 μM Incubation Time: 14 days Result: Successfully enhanced bone nodule formation in a significant dose-dependent manner.

[1]. Di Pompo G, et al. Novel histone deacetylase inhibitors induce growth arrest, apoptosis, and differentiation in sarcoma cancer stem cells. J Med Chem. 2015;58(9):4073-4079.