HDAC-IN-46

HDAC-IN-46 (compound 12c) is a potent HDAC inhibitor with an IC50 value of 0.21 μM and 0.021 μM for HDAC1 and HDAC6, respectively. HDAC-IN-46 upregulates p-p38, and downregulates Bcl-xL and cyclin D1 in MDA-MB-231 cells. HDAC-IN-46 induces significant G2 phase arrest and apoptosis. HDAC-IN-46 can be used for researching triple-negative breast cancer (TNBC)[1].

Signaling Pathways >> Apoptosis >> Apoptosis

Research Areas >> Cancer

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

Signaling Pathways >> Epigenetics >> HDAC

HDAC1:0.21 μM (IC50)

HDAC6:0.021 μM (IC50)

HDAC-IN-46 (compound 12c) has antiproliferative activity against MDA-MB-231, A549 and MCF-7 with IC50s of 88.46±10.5 μM, 83.34 ± 15.5 μM and 21.4±3.7 μM, respectively[1]. HDAC-IN-46 (5, 12.5 and 25 μM; 24 h) causes concentration-dependent upregulation of p-p38 and downregulation of Bcl-xL and cyclin D1 in MDA-MB-231 cells[1]. HDAC-IN-46 (12.5 and 25 μM; 48 h) induces significant G2 phase arrest and apoptosis[1]. Western Blot Analysis[1] Cell Line: MDA-MB-231 cells Concentration: 5, 12.5 and 25 μM Incubation Time: 24 h Result: Caused concentration-dependent upregulation of p-p38 and downregulation of Bcl-xL and cyclin D1. Cell Cycle Analysis[1] Cell Line: MDA-MB-231 cells Concentration: 12.5 and 25 μM Incubation Time: 48 h Result: Induced significant G2 phase arrest and apoptosis.

[1]. Wu B, et al. Pyrimethamine conjugated histone deacetylase inhibitors: Design, synthesis and evidence for triple negative breast cancer selective cytotoxicity. Bioorg Med Chem. 2020 Mar 15;28(6):115345.