Bioactivity | 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]. |
Invitro | 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: |
Name | HDAC6 degrader-3 |
CAS | 2785404-83-1 |
Formula | C41H41F4N7O11 |
Molar Mass | 883.80 |
Transport | Room temperature in continental US; may vary elsewhere. |
Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
Reference | [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. |