JHK-02-108-2

Chemical Structure : JHK-02-108-2

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货号: PC-27200Not For Human Use, Lab Use Only.

JHK-02-108-2 is a potent, selective, type II, heterobifunctional CDK6 PROTAC degrader with DC50 of 11 nM in MOLT-4 cells, does not induce CDK5 degradation.

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生物&药学活性

JHK-02-108-2 is a potent, selective, type II, heterobifunctional CDK6 PROTAC degrader with DC50 of 11 nM in MOLT-4 cells, does not induce CDK5 degradation.
JHK-02-108-2 induces CDK6 degradation via the ubiquitin-proteasome system (UPS).
JHK-02-108-2 induces ternary complex formation between CDK6 and CRBN with EC50 of 0.22 uM in TR-FRET assays.
JHK-02-108-2 exhibits a growth inhibition with IC50 value of 0.64 μM and dose-dependent G1 arrest in MOLT-4 cells.
JHK-02-108-2 induces potent cell cycle arrest in GBM and AML cells.

物理化学性质&存储条件

分子量	989.04
分子式	C49H56F4N10O8
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	4-(4-(3-(4-((4-(8-(2-((1-(2,6-dioxopiperidin-3-yl)-3-methyl-2-oxo-2,3-dihydro-1H-benzo[d]imidazol-5-yl)oxy)acetamido)octyl)piperazin-1-yl)methyl)-3-(trifluoromethyl)phenyl)ureido)-3-fluorophenoxy)-N-methylpicolinamide

参考文献

1. Ji Hyeon Kim, et al. J Am Chem Soc. 2026 Jun 26. doi: 10.1021/jacs.6c10277.

JHK-02-108-2

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JHK-02-108-2

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