DU-14 | PTP1B/TC-PTP PROTAC | Probechem Biochemicals

Chemical Structure : DU-14

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DU-14 (PTP1B/TC-PTP PROTAC DU-14)

货号: PC-20349Not For Human Use, Lab Use Only.

DU-14 is a highly potent and selective small molecule degrader for both PTP1B and TC-PTP with DC50 values of 4.3 and 4.8 nM, respectively, in HEK293 cells after 16 hours treatment.

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生物&药学活性

DU-14 is a highly potent and selective small molecule degrader for both PTP1B and TC-PTP with DC50 values of 4.3 and 4.8 nM, respectively, in HEK293 cells after 16 hours treatment.
DU-14 inhibits the phosphatase activity of PTP1B and TC-PTP with IC50 values of 24.2 nM and 30.1 nM, respectively.
DU-14 exhibits >88-fold selectivity for PTP1B and TC-PTP over a representative list of 12 PTPs, consisting of receptor-like, nonreceptor-like, and dual specific phosphatases.
DU-14 amplified IFN-γ induced pSTAT1/Y701 with EC50 of 76.2 nM, promoted CD8+ T cell activation.
DU-14 efficiently amplified IFN-γ signaling through inhibition of PTP1B and TC-PTP catalyzed yyrosine dephosphorylation of JAK2/Y1007/Y1008, JAK1/Y1034/Y1035 and/or STAT1/Y701, leading to increased cell surface MHC-I expression, which is required for efficient T-cell mediated killing of tumor cells.
DU-14 (25-50 mg/kg, i,p,) repressed MC38 tumor in mice, with nearly complete PTP1B and TC-PTP degradation in whole tumor homogenates.

物理化学性质&存储条件

分子量	1505.48
分子式	C74H85BrF2N9O14PS
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-((S)-3-(((S)-6-(3-bromo-4-methylbenzamido)-1-((3-(2-(((S)-1-((2S,4R)-4-hydroxy-2-(((S)-1-(4-(4-methylthiazol-5-yl)phenyl)ethyl)carbamoyl)pyrrolidin-1-yl)-3,3-dimethyl-1-oxobutan-2-yl)amino)-2-oxoethyl)benzyl)amino)-1-oxohexan-2-yl)amino)-2-((S)-2-(2-(4-hydroxy-3-methoxyphenyl)acetamido)-3-phenylpropanamido)-3-oxopropyl)phenyl)difluoromethyl)phosphonic acid

参考文献

1. Jiajun Dong, et al. Angew Chem Int Ed Engl. 2023 Mar 27;e202303818.

DU-14 (PTP1B/TC-PTP PROTAC DU-14)

生物&药学活性

物理化学性质&存储条件

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DU-14 (PTP1B/TC-PTP PROTAC DU-14)

生物&药学活性

物理化学性质&存储条件

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