PROTAC HDAC6 degrader (Compound A6) 是一种有效的、选择性的PROTAC HDAC6降解剂，DC50为 3.5 nM。PROTAC HDAC6 degrader 在髓系白血病细胞系中通过诱导凋亡 (apoptosis) 显示出抗增殖活性。
| 生物活性 | PROTACHDAC6 degrader(Compound A6) is a potent and selectivePROTACHDAC6degrader with aDC50of 3.5 nM. PROTACHDAC6 degradershows promising antiproliferative activity via inducingapoptosisin myeloid leukemia cell lines[1]. |
| IC50& Target[1] | HDAC6 3.5 nM (DC50) | HDAC6 4.86 nM (IC50) | HDAC1 0.1 μM (IC50) |
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体外研究
(In Vitro) | PROTAC HDAC6 degrader (Compound A6) (0.1-10 μM; 6 h) does not degrade HDAC1 but displays inhibitory activity toward HDAC1. PROTAC HDAC6 degrader demonstrates potent HDAC6 degradation as well as hyperacetylation of α-tubulin in U266 and HL-60 cells, confirming that the activity is not restricted to leukemia cell lines[1].
PROTAC HDAC6 degrader (0.5-50 μM) inhibits leukemia cells viability with log IC50values of 1.2-1.7 μM[1].
PROTAC HDAC6 degrader (8-24 μM; 48 h) induces MOLM13 cell apoptosis and arrests cell cycle at sub-G1 phase[1].
Western Blot Analysis[1] | Cell Line: | HL-60 cells | | Concentration: | 100 nM, 1 μM, 10 μM | | Incubation Time: | 6 h | | Result: | Degraded HDAC6 but not HDAC1. Induced hyperacetylation of α-tubulin and caused hyperacetylation of histone H3. |
Cell Viability Assay[1] | Cell Line: | Acute myeloid leukemia or AML (HL-60, Kasumi, THP-1, HL-60, SKNO1, and MOLM13) and B-cell acute lymphoblastic leukemia or B-ALL (REH and 697) | | Concentration: | 0.5-50 μM | | Incubation Time: | 72 h | | Result: | Inhibited cell viability with log IC50values of 1.2-1.7 μM. |
Apoptosis Analysis[1] | Cell Line: | MOLM13 | | Concentration: | 8, 16 and 24 μM | | Incubation Time: | 48 h | | Result: | Induced caspase 3/7-dependent apoptosis in dose-dependent fashion. |
Cell Cycle Analysis[1] | Cell Line: | MOLM13 | | Concentration: | 8, 16 and 24 μM | | Incubation Time: | 48 h | | Result: | Induced a dose-dependent increase in the sub-G1 fraction with a concomitant reduction of cell population in G2/M phase. |
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | Please store the product under the recommended conditions in the Certificate of Analysis. |
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