HDAC8-IN-17

HDAC8-IN-17 (compound 3r) (0-30 min) potently and time-dependently inhibits recombinant human HDAC8 enzyme, with an IC₅₀ of 0.08 μM after 30 min of pre-incubation^[1].
HDAC8-IN-17 (30 min) exhibits significantly higher selectivity for recombinant human HDAC8 than for HDAC1, HDAC2, HDAC3, and HDAC6; for HDAC1, the most potently inhibited off-target subtype, the selectivity reaches at least 72.5-fold^[1].
HDAC8-IN-17 (44.44-225 nM; 30 min) is a reversible non-competitive inhibitor of recombinant human HDAC8, which preferentially binds to the enzyme-substrate complex^[1].
HDAC8-IN-17 does not inhibit trypsin, confirming that its observed inhibitory activity is specific to HDAC8^[1].
HDAC8-IN-17 (0.4-11 μM; 24 h) selectively induces hyperacetylation of SMC3 in THP-1 cells, confirming its functional inhibitory effect on HDAC8 in a cellular context^[1].
HDAC8-IN-17 (72 h) inhibits the viability of human cancer cell lines Jurkat, THP-1, A549 and HCT116, with the strongest potency against THP-1 cells (GI₅₀ = 9 μM)^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.