STAT3/NF-κB-IN-1 

STAT3/NF-κB-IN-1 is a potentSTAT3 and NF-κB inhibitor with IC₅₀s of 5.86 (STAT3) and 4.22 μM (NF-κB) in 4 T1 cells. STAT3/NF-κB-IN-1 is able to induce apoptosis via its upregulation on key apoptotic regulators; caspases-3,9, Bax and downregulation of Bcl-2. STAT3/NF-κB-IN-1 exerts considerable anticancer activity against breast cancer cell lines and reduces tumor volume in vivo. STAT3/NF-κB-IN-1 can be used for the study of breast cancer^[1].

STAT3/NF-κB-IN-1 (Compound 12a) (72 h) exhibits cytotoxicity against 4T1, MDA-MB-231, MDA-MB-468 and MCF-7 cells with IC_{50s of 7.68, 1.53, 7.00 and 6.14 μM, respectively^[1].
STAT3/NF-κB-IN-1 (10 μM, 24 h) significantly inhibits cell migration and invasion in 4T1 and MDA-MB-231 cells^[1].
STAT3/NF-κB-IN-1 (1-10 μM, 24-72 h) significantly induces early MDA-MB-231 cell apoptosis with increasement activity of caspase 3/9 and increasement of Bax/Bcl-2^[1].
STAT3/NF-κB-IN-1 (1-5 μM, 48-96 h) significantly inhibits the expressions of p-STAT3 and NF-κB^[1].}

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

STAT3/NF-κB-IN-1 (Compound 12a) (40 mg/kg, s.c., once daily for 12 days) has significant antitumor activity in ehrlich solid carcinoma mice model^[1].

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

542.61

C₂₇H₂₆N₈O₃S

CCN1C(SCC(N/N=C\C2=CN(N=C2C3=CC=CC=C3)C4=CC=CC=C4)=O)=NC5=C1C(N(C(N5C)=O)C)=O

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• [1]. Afifi OS, et al. Revisiting multi-pathway modulation with theophylline derivatives: Targeting STAT3, NF-κB, and apoptotic signaling in breast cancer. Bioorg Chem. 2025 Jun 30;163:108708.  [Content Brief]