SMART1 | Smurf1 PROTAC degrader | Probechem Biochemicals

Chemical Structure : SMART1

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SMART1 (Smurf1-antagonizing repressor of tumor 1, Smurf1 degrader)

货号: PC-22749Not For Human Use, Lab Use Only.

SMART1 (Smurf1 PROTAC degrader) is a potent, highly selective degrader of E3 ligase SMAD ubiquitylation regulatory factor 1 (Smurf1) with DC50 of 1-5 nM in HT29 and PANC-1 cells, Dmax of 86%.

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生物&药学活性

SMART1 (Smurf1 PROTAC degrader) is a potent, highly selective degrader of E3 ligase SMAD ubiquitylation regulatory factor 1 (Smurf1) with DC50 of 1-5 nM in HT29 and PANC-1 cells, Dmax of 86%.
SMART1 binds to the HECT domain of Smurf1 but not Smurf2, with KD value of 500 nM.
SMART1 inhibits tumor growth in KRAS mutant CRC cells, including HCT116, LOVO, SW620, CFPAC-1 and Mia-PaCa-2, with IC50 of 10-50 nM, robustly inhibits PDK1 K163 neddylation, Akt T308 phosphorylation.
SMART1 could not induce Smurf1 degradation in CRBN-depleted cells, Smurf1 or PDK1 knockdown significantly reduces the sensitivity of CRC cells to SMART1.
SMART1 (50 and 100 mg/kg, daily dosing for 2 weeks) inhibits tumor growth and Akt phosphorylation in preclinical models of KRAS mutant CRC and synergizes with PDK1 inhibitor AR12 (OSU-03012).

物理化学性质&存储条件

分子量	753.78
分子式	C40H35N9O7
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-(4-(3-(1-(2-(2,6-dioxopiperidin-3-yl)-1,3-dioxoisoindolin-4-yl)piperidine-3-carboxamido)phenyl)-1H-1,2,3-triazol-1-yl)phenoxy)-N-methylpicolinamide

参考文献

1. Peng Z, et al. Nat Chem Biol. 2024 Jul 22. doi: 10.1038/s41589-024-01683-5.

SMART1 (Smurf1-antagonizing repressor of tumor 1, Smurf1 degrader)

生物&药学活性

物理化学性质&存储条件

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SMART1 (Smurf1-antagonizing repressor of tumor 1, Smurf1 degrader)

生物&药学活性

物理化学性质&存储条件

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