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首页-抗体药物偶连体和PROTACs-PROTAC-LL-K8-22
LL-K8-22

Chemical Structure : LL-K8-22

CAS No.: 3034487-84-5

LL-K8-22 (CDK8 degrader)

货号: PC-20323Not For Human Use, Lab Use Only.

LL-K8-22 is a potent, selective dual degrader of of CDK8 and cyclin C (MDA-MB-468 cell DC50, 2.52 and 2.64 uM), significantly degrades CDK8 without reducing CDK19 and does not degrade other cyclin proteins.

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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

LL-K8-22 is a potent, selective dual degrader of of CDK8 and cyclin C (MDA-MB-468 cell DC50, 2.52 and 2.64 uM), significantly degrades CDK8 without reducing CDK19 and does not degrade other cyclin proteins.
LL-K8-22 showed enhanced anti-proliferative effects over its parental molecule BI-1347.
LL-K8-22 exhibited more pronounced effects on CDK8–cyclin C downstream signaling than BI-1347, suppressing STAT1 phosphorylation more persistently.
LL-K8-22 inhibited E2F- and MYC-driven carcinogenic transcriptional programs.

物理化学性质&存储条件

分子量 573.79
分子式 C37H43N5O
外观性状 Solid
CAS No.
储存条件
固体粉末
-20°C 12 个月; 4°C 6 个月
配置液
-80°C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

1-(4-(3-((3r,5r,7r)-Adamantan-1-yl)propyl)piperazin-1-yl)-2-(4-(4-(isoquinolin-4-yl)phenyl)-1H-pyrazol-1-yl)ethan-1-one

参考文献

1. Mingyu Wang, et al. J Med Chem. 2023 Mar 17. doi: 10.1021/acs.jmedchem.2c02045.

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