HDAC8 Degrader

SZUH280 is a selective HDAC8 PROTAC degrader with a DC₅₀ of 0.58 μM. SZUH280 recruits the CRBN E3 ubiquitin ligase to mediate polyubiquitination and proteasomal degradation of HDAC8, and exhibits higher selectivity for HDAC8 over other HDAC family members. SZUH280 induces apoptosis and G2/M cell cycle arrest in cancer cells. SZUH280 impairs DNA damage repair and promotes radiosensitization in cancer cells. SZUH280 inhibits the proliferation of cancer cells. SZUH280 is used in research related to lung cancer and breast cancer.

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.

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.

PROTAC HDAC8 Degrader-5 is a selective HDAC8 PROTAC degrader that mediates ubiquitination and proteasomal degradation through the formation of a ternary complex. PROTAC HDAC8 Degrader-5 degrades HDAC8 with a DC₅₀ of 1.8 nM in MDA-MB-231 cells and a DC₅₀ of 4.7 nM in Jurkat cells. PROTAC HDAC8 Degrader-5 inhibits cancer cell migration and proliferation, induces apoptosis through caspase 3/7 activation, and increases acetylated SMC3 and α-tubulin. PROTAC HDAC8 Degrader-5 is useful for cancer-related research, such as leukemia, triple-negative breast cancer, etc..

PROTAC HDAC6 degrader 5 is a selective HDAC6 PROTAC degrader with an IC₅₀ of 43 nM. PROTAC HDAC6 degrader 5 induces proteasome-dependent degradation of HDAC6 by bridging HDAC6 and CRBN to form a ternary complex. PROTAC HDAC6 degrader 5 is applicable to research related to pulmonary fibrosis.