OSMI-4

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Chemical Structure| 2260791-14-6 同义名 : -
CAS号 : 2260791-14-6
货号 : A1177005
分子式 : C27H26ClN3O7S2
纯度 : 98%
分子量 : 604.094
MDL号 : MFCD31813742
存储条件:

粉末 Keep in dark place,Inert atmosphere,Store in freezer, under -20°C

液体 -20°C:3-6个月-80°C:12个月

溶解度 :

DMSO: 60 mg/mL(99.32 mM),配合低频超声助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO

动物实验配方:
生物活性
描述 O-linked N-acetylglucosamine (OGlcNAc) transferase (OGT) is an essential enzyme responsible for nucleocytoplasmic glycosylation. OSMI-4 is a potent OGT inhibitor with an EC50 value of ~3μM. Treatment of HEK293T cell lysates with OSMI-4 for 24 hours almost completely reduced the level of OGlcNAc at a concentration of 5μM. Cells treated with 20μM of OSMI-4 for 48 hours also showed decreased levels of HCF-1 cleavage products and the appearance of uncleaved HCF-1 compared to the control group. Also in HEK293T cells, 2-hour treatment with 10μM of OSMI-4 resulted in an increase in OGT’s detained intron splicing[2].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

1.66mL

0.33mL

0.17mL

8.28mL

1.66mL

0.83mL

16.55mL

3.31mL

1.66mL

参考文献

[1]Martin SES, et al. Structure-Based Evolution of Low Nanomolar O-GlcNAc Transferase Inhibitors. J Am Chem Soc. 2018 Oct 24;140(42):13542-13545.

[2]Martin SES, Tan ZW, Itkonen HM, Duveau DY, Paulo JA, Janetzko J, Boutz PL, Törk L, Moss FA, Thomas CJ, Gygi SP, Lazarus MB, Walker S. Structure-Based Evolution of Low Nanomolar O-GlcNAc Transferase Inhibitors. J Am Chem Soc. 2018 Oct 24;140(42):13542-13545. doi: 10.1021/jacs.8b07328