Chemical Structure : Nsun2‐i4
CAS No.:
684237-96-5
Nsun2‐i4
(NSUN2 inhibitor)
Catalog No.: PC-24232Not For Human Use, Lab Use Only.
Nsun2‐i4 is a specific small molecule inhibitor of m5C methyltransferase NSUN2 with KD of 2.65 uM in MST assays.
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Purity & Documentation Purity:
>98% (HPLC)
Biological Activity
Nsun2‐i4 is a specific small molecule inhibitor of m5C methyltransferase NSUN2 with KD of 2.65 uM in MST assays.
Nsun2‐i4 exhibits inhibitory effects in CRC cell lines with the lowest IC50 values measured at 56.04 µM in SW480 cell and 45.79 µM in HT29 cell, respectively.
Nsun2‐i4 (50 uM, 12h) decreased the expression levels of ENO1 and GRB2 proteins in treating CRC cells.
Nsun2‐i4 (50 mg/kg intraperitoneally) effectively inhibited tumor growth rates and reduced the total tumor burden in AOM/DSS‐induced CRC
Nsun2‐i4 does not result in any significant changes in body weight, or the histopathological analyses of major organs, including the kidney, liver, spleen, and colon.
Nsun2‐i4 treatment caused significant cGAMP‐induced activation of p‐STING and p‐TBK1 in CRC cells.
Nsun2‐i4 demonstrated a significantly enhanced inhibitory effect on tumor growth when combined with PD‐1.
Physicochemical Properties
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M.Wt
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453.51
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Formula
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C23H23N3O5S
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Appearance
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Solid
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CAS No.
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Storage
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- Solide Powder
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-20°C 12 Months; 4°C 6 Months
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- In Solvent
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-80°C 6 Months; -20°C 6 Months
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Shipping
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Solubility
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10 mM in DMSO
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Chemical Name/SMILES
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2-((3-cyano-4-(3-ethoxy-4-hydroxyphenyl)-6-oxo-1,4,5,6-tetrahydropyridin-2-yl)thio)-N-(4-methoxyphenyl)acetamide
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References
1. Chen B, et al. Adv Sci (Weinh). 2024 Jul;11(28):e2309840.
2. Hou X, et al. Theranostics. 2025 Jan 27;15(7):2757-2777.
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