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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- CAS. Nr.: 2928480-72-0
- Formel: C24H24ClN5O4
- Molecular Weight:481.93
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Speicherung:
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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Biologische Aktivität
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Chemical Information
- Reinheit & Dokumentation
- Verweise
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Help & FAQs
Biologische Aktivität
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
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[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
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[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
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[PMID: 37523719] |
Chemical Information
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CAS. Nr. 2928480-72-0
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Molecular Weight 481.93
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Formel 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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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Reinheit & Dokumentation
Verweise
[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
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
II399 Related Classifications
HY-163174 Related Classifications
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