TRIB2 PROTAC 5k | TRIB2 PROTAC | Probechem Biochemicals

Chemical Structure : TRIB2 PROTAC 5k

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TRIB2 PROTAC 5k (Compound 5k)

货号: PC-23445Not For Human Use, Lab Use Only.

TRIB2 PROTAC 5k (Compound 5k) is a potent, selective pseudokinase TRIB2 PROTAC degrader with DC50 of 16.8 nM and Dmax of 92% in PC3 cells.

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生物&药学活性

TRIB2 PROTAC 5k (Compound 5k) is a potent, selective pseudokinase TRIB2 PROTAC degrader with DC50 of 16.8 nM and Dmax of 92% in PC3 cells.
Compound 5k also demonstrates potent degradation activity against TRIB2 protein levels in other prostate cancer cell lines including H660 and LTL-331R-CL neuroendocrine prostate cancer cells.
Compound 5k facilitates TRIB2 degradation via Cereblon-dependent ubiquitination and proteasomal pathways.
Compound 5k dose-dependently inhibits the ATP binding affinity of TRIB2 with IC50 of 65.2 nM.
Compound 5k exhibits selectivity towards TRIB2 over other pseudokinases.
Compound 5k shows potent anti-proliferative and apoptotic effects in AR- prostate cancer cell lines (neuroendocrine-like LTL-331R-CL cells, IC50=3.9 nM, PC3 cell IC50=30.38 nM).
Compound 5k triggers apoptosis in a panel of prostate cancer cell lines (LTL-331R-CL and PC3 cells).

物理化学性质&存储条件

分子量	812.90
分子式	C45H45FN8O6
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	N-(2-(10-((2-(2,6-dioxopiperidin-3-yl)-1,3-dioxoisoindolin-5-yl)amino)-decanoyl)-1,2,3,4-tetrahydroisoquinolin-7-yl)-5-(2-fluoropyridin-3-yl)-1H-indazole-3-carboxamide

参考文献

1. Wen C, et al. Eur J Med Chem. 2024 Nov 1;281:117016.

TRIB2 PROTAC 5k (Compound 5k)

生物&药学活性

物理化学性质&存储条件

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TRIB2 PROTAC 5k (Compound 5k)

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物理化学性质&存储条件

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