HDAC6 Degrader

Thalidomide-4-OH (Cereblon ligand 2) is the Thalidomide-based Cereblon ligand used in the recruitment of CRBN protein. Thalidomide-4-OH (Cereblon ligand 2) can be connected to the ligand for protein by a linker to form PROTACs.

TO-1187 TFA is a selective HDAC6 PROTAC degrader (DC₅₀: 5.81 nM). TO-1187 TFA promotes the ubiquitination and degradation of HDAC6 and can be used in the study of hematological malignancies and solid tumors.

PROTAC HDAC6 degrader 11 is a potent and selective HDAC6 degrader via ternary complex formation and the ubiquitin-proteasome pathway with a DC₅₀ value of 19.4 nM. PROTAC HDAC6 degrader 11 has IC₅₀s of 4.54 nM and 0.647 μM for HDAC6 and HDAC1, respectively. PROTAC HDAC6 degrader 11 causes strong hyperacetylation of α-tubulin.

TO-1187 is a selective HDAC6 PROTAC degrader (DC₅₀: 5.81 nM). TO-1187 promotes the ubiquitination and degradation of HDAC6 and can be used in the study of hematological malignancies and solid tumors.

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.

PROTAC HDAC6 degrader 6 (Compound 12) is a selective HDAC6-targeting photochemically targeting chimeras (PHOTACs) (subset of PROTAC) degrader with a ～50% D_max only upon activation to its cis-state with 390 nm light irradiation.

PROTAC HDAC6 degrader 9 is a selective HDAC6 PROTAC degrader. PROTAC HDAC6 degrader 9 can be used for the research cancers related to HDAC6 abnormalities, such as multiple myeloma.

PROTAC HDAC6 degrader 12 is a PROTAC and a selective HDAC6 degrader consists of a non-selective HDAC inhibitor and thalidomide-type E3 ligase ligand. HDAC6 degrader-4 can be used for cancer research.

HDAC-IN-97 is a PROTAC HDAC6 degrader-6that can be used for synthesis of PROTACs, such as HDAC6 degrader-6 (HY-177758). HDAC6 degrader-6 is a potent HDAC6 PROTAC degrader with anticancer activity.

PROTAC HDAC8 Degrader-2 is a HDAC6/8 PROTAC degrader, with IC₅₀ values of 0.042 μM and 0.147 μM against human HDAC8 and HDAC6, respectively, and exhibits selectivity over other class I HDAC isozymes. PROTAC HDAC8 Degrader-2 induces apoptosis (apoptosis) in leukemia cells, shows no obvious cytotoxicity to normal cells, and has favorable chemical stability. PROTAC HDAC8 Degrader-2 can be used in research related to acute myeloid leukemia.

PROTAC HDAC6 degrader (Compound A6) is a potent and selective PROTAC HDAC6 degrader with a DC₅₀ of 3.5 nM. PROTAC HDAC6 degrader shows promising antiproliferative activity via inducing apoptosis in myeloid leukemia cell lines.

HDAC6 degrader-6 (Compound 11b) is a potent and selective HDAC6 PROTAC degrader with a DC₅₀ of 1.9 nM. HDAC6 degrader-6 has no effect on the protein levels of other HDAC family members and does not degrade IKZF1, IKZF3, and GSPT1. HDAC6 degrader-6 can be used to study multiple myeloma.

PROTAC HDAC6 degrader 10 is a highly efficient, safe and selective HDAC6 PROTAC degrader with a pIC₅₀ of 8.75 and a pDC₅₀ of 9.2 in BEAS-2B cells. PROTAC HDAC6 degrader 10 recruits cereblon to form a ternary complex with HDAC6, thereby achieving the degradation of HDAC6. PROTAC HDAC6 degrader 10 significantly induces hyperacetylation of α-tubulin without affecting the acetylation of H3, and achieves sustained HDAC6 knockdown in mouse lung tissues. PROTAC HDAC6 degrader 10 exhibits high bioavailability after subcutaneous administration in mice. PROTAC HDAC6 degrader 10 enables the study of HDAC6 pharmacology via chemical knockdown of HDAC6 in vitro and in vivo, and can be used for research on pulmonary diseases.

PROTAC HDAC6 degrader 4 (Compound 17c) is the PROTAC degrader for HDAC6 with a DC₅₀ of 14 nM. PROTAC HDAC6 degrader 4 exhibits inhibitory activit against HDAC1, HDAC2, HDAC3 and HDAC6 with IC₅₀s of 2.2, 2.37, 0.61 and 0.295 μM, respectively. (Pink: ligand for target protein HDAC6 ligand-3 (HY-172360); Black: linker (HY-138387); Blue: ligand for cereblon E3 ligase (HY-W093272))

PRO-HD2 is a HDAC6 PROTAC degrader. PRO-HD2 exerts antiproliferative activity in leukemia cells. PRO-HD2 can be used for leukemia research.