STAT3/CAIX-IN-1 

STAT3/CAIX-IN-1 is a dual-target inhibitor of STAT3 (K_d: 60.03 μM) and CAIX (IC₅₀: 80.45 nM). STAT3/CAIX-IN-1 induces ferroptosis by increases the levels of reactive oxygen species (ROS) and lipid peroxides. STAT3/CAIX-IN-1 inhibits cell migration, induces apoptosis, and causes cell cycle arrest in MDA-MB-231 cells. STAT3/CAIX-IN-1 can be used for the study of triple-negative breast cancer (TNBC)^[1].

STAT3/CAIX-IN-1 (compound 7m) (2-8 μM, 24 h) inhibits STAT3 phosphorylation in MDA-MB-231 cells^[1].

STAT3/CAIX-IN-1 (4 μM) binds to STAT3 to enhance its stability^[1]. STAT3/CAIX-IN-1 enhances proliferation inhibition of tumor cell lines with IC₅₀s of 2.18 μM (hypoxia) and 4.21μM (normoxia) in the MDA-MB-231 cell line^[1]_.

STAT3/CAIX-IN-1 (4 μM, 8 μM, 24 h) induces ferroptosis via the GPX4 pathway, increases reactive oxygen species (ROS) levels, upregulates intracellular lipid peroxidation in MDA-MB-231 cells^[1].

STAT3/CAIX-IN-1 (2 μM, 4 μM, 24-48 h) inhibits the migration of MDA-MB-231 cells^[1]. STAT3/CAIX-IN-1 (4 μM, 8 μM, 24 h) induces apoptosis in MDA-MB-231 cells, induces cell cycle arrest in MDA-MB-231 cells at the G1/S phase^[1].

STAT3/CAIX-IN-1 has anti-tumor activity with IC₅₀s of 4.21 μM (MDA-MB-231), 5.67 μM (MCF-7), 6.60 μM (MDA-MB-231/ADR), 14.19 μM (MCF-10A)^[1].

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

STAT3/CAIX-IN-1 (compound 7m) (5 mg/kg, 10 mg/kg, 48 h) shows anti-tumor activity with 75% TIR, not changes weight or behavior^[1].

STAT3/CAIX-IN-1 (10 mg/kg, i.p.,21 days, every 2 days) reduces phosphorylated STAT3 expression in Balb/c nude mouse xenograft experiments^[1].

STAT3/CAIX-IN-1 (5 mg/kg, 10 mg/kg, i.p., 21 days, every 2 days) inhibits tumor growth on Balb/c nude mice with MDA-MB-231 xenograft tumors^[1].

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

687.63

C₂₈H₂₃F₆N₅O₅S₂

3053583-60-8

O=C(NC1=NN=C(S(=O)(N)=O)S1)CCCC(N2C/C(C(/C(C2)=C/C3=CC=C(C(F)(F)F)C=C3)=O)=C\C4=CC=C(C(F)(F)F)C=C4)=O

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• [1]. Chen L, et al. Discovery of Diaryl Piperidone-Sulfonamide as a Novel Dual-Target Inhibitor of STAT3/CAIX Inducing Ferroptosis in Triple-Negative Breast Cancer Cells. J Med Chem. 2025 Jun 26;68(12):12493-12512.  [Content Brief]