OSMI-1

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Chemical Structure| 1681056-61-0 同义名 : -
CAS号 : 1681056-61-0
货号 : A1191949
分子式 : C28H25N3O6S2
纯度 : 99%+
分子量 : 563.645
MDL号 : MFCD30187585
存储条件：

Pure form Keep in dark place,Inert atmosphere,Room temperature

In solvent -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 105 mg/mL(186.29 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-GlcNAcylation is an important posttranslational modification governed by a single pair of enzymes-O-GlcNAc transferase (OGT) and O-GlcNAcase (OGA). These two enzymes mediate the dynamic cycling of O-GlcNAcylation on a wide variety of cytosolic, nuclear and mitochondrial proteins in a nutrient- and stress-responsive fashion[1]. OGT catalyses the transfer of N-acetylglucosamine from UDP-N-acetylglucosamine (UDP-GlcNAc) to serines and threonines of cytoplasmic, nuclear and mitochondrial proteins, including numerous transcription factors, tumour suppressors, kinases, phosphatases and histone-modifying proteins[2].Biofunctional investigation demonstrated that OGT significantly increased cell growth (p<0.001), clonogenicity (p<0.01), migration and invasion (p<0.05) ability in vitro, and promoted xenograft tumor growth as well as lung metastasis in nude mice[3].OSMI-1 is a cell-permeable OGT inhibitor with an IC50 value of 2.7 μM. OSMI-1 inhibits protein O-linked N-acetylglucosamine (O-GlcNAcylation) in several mammalian cell lines without qualitatively altering cell surface N- or O-linked glycans. OSMI-1 (50 μM; 24 hours; CHO cells) treatment decreases the viability by about 50% after 24 hours. OSMI-1 (10-100 μM; 24 hours; CHO cells) treatment reduces global O-linked N-acetylglucosamine (O-GlcNAcylation) a dose-dependent manner. OSMI-1 inhibits OGT activity in cells[4].Mammalian and zebrafish toxicity profiles are strikingly similar, and zebrafish can usually serve as an intermediate step between cell-based evaluation and conventional animal testing. The zebrafish model is used to investigate OSM1-1 acute toxicity in vivo. The LC50 of OSM1-1 is 0.031 mg/mL (56 μM, 12 h) and 0.025 mg/mL (45 μM, 24 h) in zebrafish model[5].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

1.77mL

0.35mL

0.18mL

8.87mL

1.77mL

0.89mL

17.74mL

3.55mL

1.77mL
参考文献

[1] Qunxiang Ong,et al. O-GlcNAc as an Integrator of Signaling Pathways. Front Endocrinol (Lausanne). 2018 Oct 16;9:599.

[2]Michael B Lazarus,et al. Structure of human O-GlcNAc transferase and its complex with a peptide substrate. Nature. 2011 Jan 27;469(7331):564-7.

[3]Weiqi Xu,et al. O-GlcNAc transferase promotes fatty liver-associated liver cancer through inducing palmitic acid and activating endoplasmic reticulum stress. J Hepatol. 2017 Aug;67(2):310-320.

[4]Ortiz-Meoz RF, et al. A small molecule that inhibits OGT activity in cells. ACS Chem Biol. 2015 Jun 19;10(6):1392-7.

[5]Liu Y, et al. Discovery of a Low Toxicity O-GlcNAc Transferase (OGT) Inhibitor by Structure-based Virtual Screening of Natural Products. Sci Rep. 2017 Sep 26;7(1):12334.