生物活性 | |||
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描述 | Smad ubiquitination regulatory factor-1 (Smurf1) is an E3 ubiquitin-protein ligase that is specific for receptor-regulated SMAD proteins in the bone morphogenetic protein (BMP) pathway. Smurf1-IN-A01 is an ubiquitin Smurf1 inhibitor with a kd of 3.664 nM, which strongly block the WW1 domain of Smurf1 from interacting with Smad1/5[1]. Smurf1-IN-A01 stabilizes endogenous Smad1/5 protein level by preventing their ubiquitin-proteasome mediated degradation. Administration of Smurf1-IN-A01 by a concentration ladder drew a gradually increased ALP activity in C2C12 cells. After a 5 days administration, Smurf1-IN-A01 potentiated the intracellular Ca2+ accumulation significantly comparing with the control group; which also slightly increase cell proliferation upon administration. Smurf1-IN-A01 is able to enhance BMP signaling responsiveness in C2C12 cells, and potentiates BMP-2 induced osteoblastic activity[1]. . |
实验方案 | |||
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1mg | 5mg | 10mg | |
1 mM 5 mM 10 mM |
1.95mL 0.39mL 0.19mL |
9.75mL 1.95mL 0.97mL |
19.50mL 3.90mL 1.95mL |
参考文献 |
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