HDAC6-IN-10

HDAC6-IN-10 is a highly selective HDAC6 inhibitor with the IC50 of 0.73 nM. HDAC6-IN-10 has 144~10941-fold selectivity over other HDAC isoforms. HDAC6-IN-10 shows anti-proliferative activities against multiple myeloma cells[1].

Research Areas >> Cancer

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

Signaling Pathways >> Epigenetics >> HDAC

HDAC1:8020 nM (IC50)

HDAC4:5620 nM (IC50)

HDAC5:4370 nM (IC50)

HDAC6:0.73 nM (IC50)

HDAC7:752 nM (IC50)

HDAC8:513 nM (IC50)

HDAC9:2560 nM (IC50)

HDAC10:105 nM (IC50)

HDAC11:1800 nM (IC50)

HDAC6-IN-10 (Compound 21b) (0.1-10 μM; 24 h) treatment shows highly selective inhibition against HDAC6[1]. HDAC6-IN-10 (Compound 21b) (0-100 μM; 72 h) treatment shows anti-proliferative activities against two multiple myeloma cells RPMI-8226 and U266[1]. Western Blot Analysis[1] Cell Line: HCT-116 Concentration: 0.1, 1 and 10 μM Incubation Time: 24 hours Result: Showed a dose-dependent increase in the level of Ac-tubulin. Cell Proliferation Assay[1] Cell Line: RPMI-8226 and U266 cells Concentration: 0-100 μM Incubation Time: 72 hours Result: Showed antiproliferative activities against RPMI-8226 and U266 with the IC50s of 33.183 μM and 43.233 μM, respectively.

[1]. Xin Chen, et al. Novel 2, 5-diketopiperazine derivatives as potent selective histone deacetylase 6 inhibitors: Rational design, synthesis and antiproliferative activity. Eur J Med Chem. 2020 Feb 1;187:111950.