HDAC6 degrader-3

Names

[ CAS No. ]:
2785404-83-1

[ Name ]:
HDAC6 degrader-3

Biological Activity

[Description]:

HDAC6 degrader-3 is a potent and selective HDAC6 degrader via ternary complex formation and the ubiquitin-proteasome pathway with a DC50 value of 19.4 nM. HDAC6 degrader-3 has IC50s of 4.54 nM and 0.647 μM for HDAC6 and HDAC1, respectively. HDAC6 degrader-3 causes strong hyperacetylation of α-tubulin[1].

[Related Catalog]:

Research Areas >> Cancer
Signaling Pathways >> Cell Cycle/DNA Damage >> HDAC
Signaling Pathways >> PROTAC >> PROTAC
Signaling Pathways >> Epigenetics >> HDAC

[Target]

HDAC6:19.4 nM (ID50)

HDAC6:4.54 nM (IC50)

HDAC1:0.647 μM (IC50)

Cereblon


[In Vitro]

HDAC6 degrader-3 (化合物 B4; 100-1000 nM; 24 小时) 表现出有效的 HDAC6 降解以及 α-微管蛋白的高度乙酰化[1]。 HDAC6 degrader-3 (0.5-50 μM; 72 小时) 对白血病细胞系 (697、HL-60、KASUMI-1、MV4-11、REH、THP-1、SKNO- 1, MOLM-13)[1]。 Western Blot Analysis[1] Cell Line: U266 multiple myeloma cell line Concentration: 100 nM and 1000 nM Incubation Time: 24 h Result: Demonstrated potent HDAC6 degradation as well as hyperacetylation of α-tubulin.

[References]

[1]. Laura Sinatra, et al. Solid-Phase Synthesis of Cereblon-Recruiting Selective Histone Deacetylase 6 Degraders (HDAC6 PROTACs) with Antileukemic Activity. J Med Chem. 2022 Dec 22;65(24):16860-16878.  

Chemical & Physical Properties

[ Molecular Formula ]:
C41H41F4N7O11

[ Molecular Weight ]:
883.80

Related Compounds