HDAC Degrader

HDAC6 degrader-1 is the PROTAC degrader for HDAC6 with a DC₅₀ of 3.8 nM in cell MM.1S.

PROTAC HDAC6 degrader 3 (Compound 4) is a selective inhibitor and degrader for HDAC6 with an IC₅₀ of 686 nM and a DC₅₀ of 171 nM. PROTAC HDAC6 degrader 3 promotes the acetylation of α-tubulin. (Pink: ligand for target protein (HY-171141); Blue: ligand for E3 ligase VHL (HY-150803))

PROTAC HDAC degrader-2 TFA is the trifluoroacetate salt of PROTAC HDAC degrader-2. PROTAC HDAC degrader-2 is a selective IIb HDACs PROTAC degrader, with DC₅₀s of 13 nM for HDAC6, 29 nM for HDAC10, respectively. PROTAC HDAC degrader-2 exhibits low cytotoxicity against hematological and solid cancer cell lines. PROTAC HDAC degrader-2 can be used for the chemical knockdown of class IIb HDACs.

HDAC6 ligand-5 is a binding ligand of HDAC6 and can be used to synthesize PROTACs such as PROTAC HDAC6 degrader 5.

Tubastatin A-C6-NHBoc is a conjugate of a target protein ligand and a linker, which can be used to synthesize PROTACs, such as PROTAC HDAC degrader-2 (HY-174444).

HDAC6 ligand-linker conjugate 1 is a conjugate of HDAC6 ligand and linker, which can be used to synthesize PROTACs such as PROTAC HDAC6 degrader 5 (HY-174401).

HDAC1 Degrader-1 (compound 1a) is an HDAC1 degrader with anticancer activity. HDAC1 Degrader-1 significantly reduces HDAC1 levels in MM.1S multiple myeloma cells.

YX862 is a selective HDAC8 PROTAC degrader and induces the degradation of HDAC8 with maximum degradation ＞ 95% at 250 nM in MDA-MB-231 cells.

PRO-HD1 is a PROTAC HDAC6 degrader. PRO-HD1 degrades HDAC6 in A549 cells, and inhibits proliferation of Jurkat cells (IC₅₀: 5.8 μM).

HDAC6 degrader-6 (compound 10c) is a ByeTAC protein degrader targeting HDAC6, with IC₅₀ values of 0.034 μM, 0.166 μM, 0.703 μM, and 0.293 μM for HDAC6, HDAC1, HDAC2, and HDAC3, respectively. HDAC6 degrader-6 induces cell apoptosis and can be used for the study of multiple myeloma(Blue: USP14 ligand HY-159808; Pink: HDAC ligand HY-176209; Black: linker HY-W016871)

HDAC3 degrader-2 is a selective HDAC3 degrader. HDAC3 degrader-2 inhibits the activation of the NLRP3 inflammasome by degrading HDAC3, thereby reducing the maturation of IL-1β and caspase-1. HDAC3 degrader-2 exhibits anti-inflammatory activity. HDAC3 degrader-2 can be used in research related to endotoxin shock, colitis and gouty arthritis.