HDAC8 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.

YX968 is a selective HDAC3/HDAC8 PROTAC dual degrader, with a DC₅₀ value of 1.7 nM against HDAC3 and 6.1 nM against HDAC8. YX968 inhibits cancer cell growth, induces apoptosis, prevents global histone hyperacetylation, and exerts effects via antiproliferative activity. YX968 can be used in research related to triple-negative breast cancer, non-small cell lung cancer, and multiple myeloma.

SZUH280 is a potent and selective PROTAC HDAC8 degrader with a DC₅₀ of 0.58 μM in A549 cells. SZUH280 induces cancer cell apoptosis. SZUH280 hampers DNA damage repair in cancer cells, promoting cellular radiosensitization.

Degrader-1 (compound Z16) is a potent and selective HDAC8 PROTAC degrader with an DC₅₀ of 0.27 nM in A549 cells.

PROTAC HDAC8 Degrader-3 (Compound BP6) is an efficient, selective and low-toxicity HDAC8 PROTAC degrader with a DC₅₀ of 80 nM. PROTAC HDAC8 Degrader-3 exhibits IC₅₀ of PROTAC for HDAC8 and CRBN of 0.26 and 30 μM respectively. PROTAC HDAC8 Degrader-3 increases the level of Ac-SMC3, stabilizes p53 and sensitizes targeted reagents (such as Idasanutlin (HY-15676)), demonstrating its great potential in combination therapy.

PROTAC HDAC8 Degrader-3 (Compound BP1) is an efficient and selective HDAC8 PROTAC degrader with a DC₅₀ of 20 nM. PROTAC HDAC8 Degrader-3 exhibits IC₅₀ for HDAC8 and CRBN of 0.46 and 7.5 μM, respectively. PROTAC HDAC8 Degrader-3 exhibits potent anti-proliferative activity against MM.1S and HL-60 cells. PROTAC HDAC8 Degrader-3 can be used for research on multiple myeloma and acute myeloid leukemia.

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.