NCGC00685960 

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^[1].

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.

NCGC00685960 (25 mg/kg, i.p. or 4 mg/kg, i.t., 3 times/weekfor 42 days) inhibits tumors growth and omental metastases, decreases C3 protein levels and Ly6C⁺PD-L1⁺ monocyte infiltration in tumor tissues, and enhances cytokine (IFN-γ, TNF-α) secretion by CD8⁺ T cells in ovarian cancer, breast cancer and colon cancer mice models^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

458.00

C₂₄H₃₂ClN₅O₂

3091000-99-3

Solid

White to off-white

O=C1NC2=C(C=CC=C2N3N=C([C@@H]4CN(CCC5CCCCC5)CCC4)NC3=O)C=C1.Cl

Room temperature in continental US; may vary elsewhere.

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)

• [1]. Heide J, et al. NNMT inhibition in cancer-associated fibroblasts restores antitumour immunity. Nature. 2025;645(8082):1051-1059.  [Content Brief]