PROTAC HDAC degrader-2

PROTAC HDAC degrader-2 (AP1) potently inhibits purified HDAC6 and HDAC10 enzymes with IC₅₀ values of 0.040 μM and 0.022 μM, respectively^[1].
PROTAC HDAC degrader-2 engages cellular CRBN in HEK293T cells stably expressing NanoLuc-CRBN with an IC₅₀ of 7.5 μM, an upper estimate due to autofluorescence interference^[1].
PROTAC HDAC degrader-2 (50 nM, 1 μM; up to 1440 min) shows high stability in human plasma at 1 μM, remaining above 85% intact for up to 1440 min^[1].
PROTAC HDAC degrader-2 (1-5 μM; 24 h) potently and selectively degrades HDAC6 and HDAC10 in MM.1S cells, with DC₅₀ values of 13 nM and 29 nM, respectively, and no off-target degradation of class I or class IIa HDAC subtypes at 1 μM for 24 h^[1].
PROTAC HDAC degrader-2 (1 μM; 24 h) does not induce histone H3 hyperacetylation and shows minimal effects on acetylated α-tubulin in MM.1S cells treated with 1 μM for 24 h, confirming its class IIb HDAC selectivity^[1].

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