NCGC00685960
Based on 1 Customer Validation
NCGC00685960 is a Nicotinamide N-methyltransferase (NNMT) inhibitor with an IC50 <10 nM. NCGC00685960 has potent antitumor activity. NCGC00685960 increases H3K27 trimethylation levels in ovarian cancer cells and inhibits α-SMA expression in NNMT-expressing ovarian fibroblasts. NCGC00685960 reduces 1-MNA levels, reverses SAM and H3K27 hypomethylation and significantly impairs collagen contractility in cancer-associated fibroblasts (CAFs). NCGC00685960 can be used for cancers research, such as ovarian cancer, breast cancer, colon cancer.
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- Pureté: 99.97%
- CAS No.: 3091000-99-3
- Formule: C24H32ClN5O2
- Masse moléculaire:458.00
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Stockage:
4°C, sealed storage, away from moisture and light
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
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Activité biologique
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Chemical Information
- Pureté et documentation
- Références
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Help & FAQs
Activité biologique
NCGC00685960 (NNMTi) (3-72 h) inhibits NNMT activity, reduces 1-methylnicotinamide (1-MNA) production, restores SAM levels, reverses H3K27me3 hypomethylation, downregulates complement factor (e.g., C3) secretion, decreases the expression of CAF markers (α-SMA, Ly6C, MHCII) and collagen contractility, reduces the recruitment of immunosuppressive Ly6C+PD-L1+ monocytes, and restores CD8+ T cell activation and proliferation[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:C57BL/6NCrl with ovarian cancer, breast cancer and colon cancer[1]
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Dosage:4, 25 mg/kg
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Administration:I.p. or i.t.; daily; 42 days
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Result:Reduced primary tumour weight.
Decreased C3 protein levels in tumour tissue compared to vehicle control.
Reduced number of immunosuppressive Ly6C+PD-L1+ monocytes per mg tumour compared to vehicle control.
Increased CD8+ granzyme B+ T cells per mg tumour compared to vehicle control.
Chemical Information
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CAS No. 3091000-99-3
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Appearance Solid
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Masse moléculaire 458.00
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Formule C24H32ClN5O2
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Color White to off-white
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SMILES
O=C1NC2=C(C=CC=C2N3N=C([C@@H]4CN(CCC5CCCCC5)CCC4)NC3=O)C=C1.Cl
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
4°C, sealed storage, away from moisture and light
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
Pureté et documentation
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Fiche technique (273 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Portuguese - PT (252 KB)
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Instruction de manipulation (2659 KB)
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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