您好,欢迎来到化工原料网! [登录] [免费注册]
化工原料网
位置:首页 > 产品库 > PROTAC HDAC6 degrader 1
立即咨询
咨询类型:
     
*姓名:
*电话:
*单位:
Email:
*留言内容:
请详细说明您的需求。
*验证码:
 
PROTAC HDAC6 degrader 1
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
PROTAC HDAC6 degrader 1图片
CAS NO:2785404-76-2
包装与价格:
包装价格(元)
100mg电议
250mg电议
500mg电议

产品介绍
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)

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.
分子量

734.80

Formula

C37H46N6O10

CAS 号

2785404-76-2

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.