II399
II399 is a potent, selective NNMT bisubstrate inhibitor containing an unconventional SAM mimic, with a Ki of 5.9 nM. II399 exhibits an explicit pattern of competitive inhibition for NAM. II399 occupies both the substrate and cofactor binding pockets. II399 has the potential for the research of cancers, metabolic, cardiovascular, and neurodegenerative diseases.
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研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- CAS 番号: 2928480-72-0
- 分子式: C24H24ClN5O4
- 分子量:481.93
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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生物活性
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化学情報
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
生物活性
NNMT[1]
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| 769-P | GI50 |
>200 μM
Compound: 5a; II399
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Cytotoxicity against human 769-P cells assessed as suppression of cell viability measured after 8 days by Alamar blue dye based assay
Cytotoxicity against human 769-P cells assessed as suppression of cell viability measured after 8 days by Alamar blue dye based assay
|
[PMID: 37523719] |
| 786-0 | GI50 |
71 μM
Compound: 5a; II399
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Cytotoxicity against human 786-0 cells assessed as suppression of cell viability measured after 8 days by Alamar blue dye based assay
Cytotoxicity against human 786-0 cells assessed as suppression of cell viability measured after 8 days by Alamar blue dye based assay
|
[PMID: 37523719] |
| CAKI-1 | GI50 |
57 μM
Compound: 5a; II399
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Cytotoxicity against human CAKI-1 cells assessed as suppression of cell viability measured after 8 days by Alamar blue dye based assay
Cytotoxicity against human CAKI-1 cells assessed as suppression of cell viability measured after 8 days by Alamar blue dye based assay
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[PMID: 37523719] |
| UO-31 | GI50 |
135 μM
Compound: 5a; II399
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Cytotoxicity against human UO-31 cells assessed as suppression of cell viability measured after 8 days by Alamar blue dye based assay
Cytotoxicity against human UO-31 cells assessed as suppression of cell viability measured after 8 days by Alamar blue dye based assay
|
[PMID: 37523719] |
化学情報
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CAS 番号 2928480-72-0
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分子量 481.93
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分子式 C24H24ClN5O4
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SMILES
O[C@H]1[C@@H](C[C@@H]([C@H]1O)CN(C(C)=O)CC#CC2=CC(C(N)=O)=CC=C2)N3C4=NC=NC(Cl)=C4C=C3
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
純度とドキュメンテーション
参考文献
[1]. Meng Y, et al. Comparative Analysis of Two NNMT Bisubstrate Inhibitors through Chemoproteomic Studies: Uncovering the Role of Unconventional SAM Analogue Moiety for Improved Selectivity. ACS Chem Biol. 2024 Jan 19;19(1):89-100. [Content Brief]
[2]. ID, et, al. Exploring Unconventional SAM Analogues To Build Cell-Potent Bisubstrate Inhibitors for Nicotinamide N-MethyltransferaseIyamu. Angew Chem Int Ed Engl. 2022 Apr 11;61(16):e202114813. [Content Brief]
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
II399 関連分類
HY-163174 関連分類
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