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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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。
- 純度: 99.97%
- CAS 番号: 3091000-99-3
- 分子式: C24H32ClN5O2
- 分子量:458.00
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保管条件:
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)
生物活性
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.
化学情報
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CAS 番号 3091000-99-3
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性状 Solid
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分子量 458.00
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分子式 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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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
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)
純度とドキュメンテーション
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データシート (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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取扱説明書 (2659 KB)
参考文献
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)