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 Ki of 78.1 nM, hCA XII Ki 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.
For research use only. We do not sell to patients.
- Formula: C22H20N8O4S
- Molecular Weight:492.51
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
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Biological Activity
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hCA IX 78.1 nM (Ki) |
hCA XII 64.4 nM (Ki) |
CAIX/XII/NAMPT-IN-1 (Compound 45) potently inhibits tumor-associated human carbonic anhydrase IX (Ki = 78.1 nM) and XII (Ki = 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.
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Cell Line:Human cancer cell lines (HCT116, SW620, A498, U87, 786-O, SF539, T47D, MDA-MB-231, SH-SY5Y, A549), normal renal epithelial HK-2 cells
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Concentration:0.00156-100 μM
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Incubation Time:48 h
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Result:Exerted submicromolar to nanomolar antiproliferative activity across multiple cancer cell lines: SW620 (IC50 = 0.6 μM normoxia, 0.3 μM hypoxia), A498 (IC50 = 0.7 μM normoxia, 0.6 μM hypoxia), U87 (IC50 = 0.4 μM normoxia, 0.3 μM hypoxia), 786-O (IC50 = 0.7 μM normoxia, 0.5 μM hypoxia), SF539 (IC50 = 0.16 μM normoxia, 0.14 μM hypoxia), HCT116 (IC50 = 3.0 μM normoxia, 1.3 μM hypoxia), A549 (IC50 = 1.5 μM normoxia, 1.1 μM hypoxia), T47D (IC50 = 1.3 μM normoxia, 1.0 μM hypoxia), MDA-MB-231 (IC50 = 7.0 μM normoxia, 1.3 μM hypoxia), SH-SY5Y (IC50 = 2.5 μM normoxia, 1.0 μM hypoxia).
Exhibited selective toxicity, with an IC50 of 4.7 μM against normal HK-2 renal epithelial cells.
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Cell Line:A498 renal carcinoma, U87 glioblastoma, HCT116 colorectal cancer, and T47D breast cancer cells
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Concentration:1 μM
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Incubation Time:24 h
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Result:Slightly reduced protein levels of NAMPT and CA IX across all cell lines.
Markedly reduced catalase protein levels across all cell lines.
Decreased phosphorylation of ERK1/2 and reduced total AKT levels, inhibiting proliferative and survival pathways.
Upregulated Bax and downregulated Bcl-2 protein expression, activating apoptotic signaling.
Chemical Information
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Molecular Weight 492.51
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Formula C22H20N8O4S
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SMILES
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
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
CAIX/XII/NAMPT-IN-1 Related Classifications
HY-181350 Related Classifications
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- CAIX/XII/NAMPT-IN-1
- Carbonic Anhydrase
- NAMPT
- Apoptosis
- Reactive Oxygen Species (ROS)
- ERK
- Akt
- DNA/RNA Synthesis
- Mitochondrial Metabolism
- glioblastoma
- human carbonic anhydrase XII
- 3D tumor spheroid models
- colorectal cancer
- human carbonic anhydrase IX
- human nicotinamide phosphoribosyltransferase
- ERK/mTOR signaling
- mitochondrial dysfunction
- apoptosis
- renal carcinoma
- Inhibitor
- inhibitor
- inhibit