HDAC8-IN-3

HDAC8-IN-3 (compound P19) is a potent HDAC8 inhibitor with IC50 value of 9.3 μM and produces thermal stabilization. HDAC8-IN-3 has cytotoxicity and induces apoptosis in leukemic cell lines[1].

Signaling Pathways >> Apoptosis >> Apoptosis

Research Areas >> Cancer

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

Signaling Pathways >> Epigenetics >> HDAC

HDAC8:9.3 μM (IC50)

HDAC4:＞50 μM (IC50)

HDAC1:＞50 μM (IC50)

HDAC2:41 μM (IC50)

HDAC3:＞50 μM (IC50)

HDAC5:＞50 μM (IC50)

HDAC6:17 μM (IC50)

HDAC8:＞50 μM (IC50)

HDAC8-IN-3 (compound P19) (5-200 μM, 48 hours; HEK293T cells) has cytotoxicity in leukemic cell lines[1]. HDAC8-IN-3 (compound P19) (50 μM) inhibits glucose transporter 1 (GLUT1)-mediated glucose transport by down-regulating GLUT1 expression (IC50 = 28.2 μM)[1]. HDAC8-IN-3 (compound P19) (79.9 μM; 24 hours) can induce apoptotic death in the CEM cell line[1]. Cell Cytotoxicity Assay[1] Cell Line: K562, KCL22 and CEM leukemia cells. Concentration: 50 μM Incubation Time: 48 hours Result: Inhibited with IC50 values of 79.9, 85.4 and 43.2 μM for CEM, K562 and KCL22 cells, respectively. Apoptosis Analysis[1] Cell Line: CEM cells Concentration: 79.9 μM Incubation Time: 24 hours Result: The percentage of apoptotic cells was recorded as 60.97%.

[1]. Upadhyay N, et al. Discovery of novel N-substituted thiazolidinediones (TZDs) as HDAC8 inhibitors: in-silico studies, synthesis, and biological evaluation. Bioorg Chem. 2020 Jul;100:103934.