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LL-K8-22

Chemical Structure : LL-K8-22

CAS No.:

LL-K8-22

Catalog No.: 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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Purity & Documentation Purity: >98% (HPLC)

Biological Activity

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.

Physicochemical Properties

M.Wt 573.79
Formula C37H43N5O
Appearance Solid
CAS No.
Storage
Solide Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 6 Months
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

References

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

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