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OSMI-1

CAS号

1681056-61-0

分子式

C28H25N3O6S2

主要靶点

Others|Acyltransferase

仅限科研使用

Cat No : CM05352

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Synonyms

zebrafish|toxicity|transferase|mono- acylglycerol acyltransferase|mammalian|Inhibitor|OSMI 1|OSMI1|OSMI-1|O-GlcNAc transferase (OGT)|O-GlcNAc|O-GlcNAc transferase|OGT|O-GlcNAcylation|Diglyceride acyltransferase|Diacylglycerol acyltransferase|inhibit|acyl-CoA:cholesterol acyltransferase|Acyltransferase|cell-permeable

验证数据展示

  • CAS No.: 1681056-61-0

    OSMI-1
    CAS#: 1681056-61-0

产品信息

CAS号 1681056-61-0
分子式 C28H25N3O6S2
主要靶点 Others|Acyltransferase
主要通路 代谢
分子量 563.64
纯度 99.83%， 此纯度可做参考，具体纯度与批次有关系，可咨询客服
储存条件 Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
别名 zebrafish|toxicity|transferase|mono- acylglycerol acyltransferase|mammalian|Inhibitor|OSMI 1|OSMI1|OSMI-1|O-GlcNAc transferase (OGT)|O-GlcNAc|O-GlcNAc transferase|OGT|O-GlcNAcylation|Diglyceride acyltransferase|Diacylglycerol acyltransferase|inhibit|acyl-CoA:cholesterol acyltransferase|Acyltransferase|cell-permeable

靶点活性

OGT:2.7 μM

体内活性

方法：为检测体内抗肿瘤活性，将 OSMI-1 (1 mg/kg，静脉注射) 和 TRAIL (500 μg/kg，腹腔注射) 给药给携带人结直肠癌肿瘤 HCT116 的 BALB/c-Foxn1nu/ArcGem nude 小鼠，每天一次，持续三周。 结果：单独用 OSMI-1 或 TRAIL 治疗的小鼠的肿瘤大小略有减小，但在 OSMI-1 和 TRAIL 组合组中显著减小。联合治疗协同提高 HCT116 裸鼠移植瘤的抗肿瘤活性。[3] 方法：为研究对 Stx 介导的致病反应的保护作用，将 OSMI-1 (300-1000 μg/mouse in water containing 4.5% DMSO and 5% Tween 80) 腹腔注射给 Stx2a 攻击的 C57BL/6 小鼠，每天一次，持续七天。 结果：O-GlcNAc 抑制可以改善小鼠的死亡率和 Stx2a 暴露引起的各种疾病症状，进一步加强了 O-GlcNAc 的抑制作用。[4]

体外活性

方法：COS7 和 Hela 细胞用 OSMI-1 (2-100 μM) 处理 24 h，使用 CCK8 Assay 检测细胞活力。 结果：50?μM OSMI-1 使细胞活力降低 50% 以上。[1] 方法：CHO 细胞用 OSMI-1 (10-100 ?μM) 处理 24 h，使用 Western Blot 检测靶点蛋白表达水平。 结果：OSMI-1 以剂量依赖的方式减少了全局 OGlcNAcylation，在 50?μM 时达到最大效果。[2]

溶解度

DMSO:100 mg/mL (177.42 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:1.83 mg/mL (3.25 mM)

参考文献

1.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.
2.Ortiz-Meoz RF, et al. A small molecule that inhibits OGT activity in cells. ACS Chem Biol. 2015 Jun 19;10(6):1392-7.
3.Lee SJ, et al. OSMI-1 Enhances TRAIL-Induced Apoptosis through ER Stress and NF-κB Signaling in Colon Cancer Cells. Int J Mol Sci. 2021 Oct 14;22(20):11073.
4.Lee KS, et al. Inhibition of O-GlcNAcylation protects from Shiga toxin-mediated cell injury and lethality in host. EMBO Mol Med. 2022 Jan 11;14(1):e14678.

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