CAIX/XII/NAMPT-IN-1 

CAIX/XII/NAMPT-IN-1 is a triple inhibitor of carbonic anhydrase IX/XII and nicotinamide phosphoribosyltransferase (NAMPT) with a hCA IX K_i of 78.1 nM, hCA XII K_i of 64.4 nM, and hNAMPT IC₅₀ of 168 nM. CAIX/XII/NAMPT-IN-1 induces apoptosis, ROS accumulation, suppresses ERK/AKT signaling, inhibits DNA synthesis, and causes mitochondrial dysfunction. CAIX/XII/NAMPT-IN-1 exerts antiproliferative effects against multiple cancer cells under normoxic and hypoxic conditions. CAIX/XII/NAMPT-IN-1 can be used for the research of cancer, such as renal carcinoma, glioblastoma and colorectal cancer^[1].

CAIX/XII/NAMPT-IN-1 (Compound 45) potently inhibits tumor-associated human carbonic anhydrase IX (K_i = 78.1 nM) and XII (K_i = 64.4 nM), with weaker activity against off-target cytosolic hCA I and hCA II^[1].
CAIX/XII/NAMPT-IN-1 potently inhibits recombinant human NAMPT with an IC₅₀ of 168 nM^[1].
CAIX/XII/NAMPT-IN-1 (0.00156-100 μM; 48 h) exerts potent, selective antiproliferative activity against a broad panel of human cancer cell lines under normoxic and hypoxic conditions, with IC₅₀ values ranging from 0.14 to 7 μM, and limited toxicity to normal HK-2 cells (IC₅₀ = 4.7 μM)^[1].
CAIX/XII/NAMPT-IN-1 (1 μM; 72 h) potently induces cytotoxicity and growth inhibition in 3D spheroids of U87 glioblastoma and 786-O renal carcinoma cells^[1].
CAIX/XII/NAMPT-IN-1 (100 nM-1 μM; 24-72 h) dose- and time-dependently inhibits DNA synthesis in U87 glioblastoma cells^[1].
CAIX/XII/NAMPT-IN-1 (1 μM; 24 h) induces oxidative stress in U87 glioblastoma cells, leading to nuclear ROS accumulation and cytoplasmic DNA fragmentation after 24 hours^[1].
CAIX/XII/NAMPT-IN-1 (1 μM; 24 h) disrupts lysosomal and mitochondrial homeostasis in U87 glioblastoma cells after 24 hours^[1].
CAIX/XII/NAMPT-IN-1 (1 μM; 24 h) modulates metabolic and survival pathways in multiple human cancer cell lines after 24 hours, reducing NAMPT/CA IX expression, suppressing ERK/AKT signaling, and inducing apoptotic Bax/Bcl-2 dysregulation^[1].

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

492.51

C₂₂H₂₀N₈O₄S

O=C(NC1=CC=CN=C1)C2=CC=C(C=C2)NC(NCC3=CN(N=N3)C4=CC=CC(S(=O)(N)=O)=C4)=O

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [1]. Paoletti N, et al. Targeting Metabolic and pH Regulatory Pathways in Cancer via Dual Inhibition of Nicotinamide Phosphoribosyltransferase and Carbonic Anhydrases IX and XII. J Med Chem. 2026;69(3):3289-3314.  [Content Brief]