2785404-83-1

2785404-83-1 structure
2785404-83-1 structure
  • Name: HDAC6 degrader-3
  • Chemical Name: HDAC6 degrader-3
  • CAS Number: 2785404-83-1
  • Molecular Formula: C41H41F4N7O11
  • Molecular Weight: 883.80
  • Catalog: Signaling Pathways Cell Cycle/DNA Damage HDAC
  • Create Date: 2023-02-02 13:40:18
  • Modify Date: 2024-04-12 09:52:03
  • 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].

Name HDAC6 degrader-3
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
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.  

Molecular Formula C41H41F4N7O11
Molecular Weight 883.80