CA/PRAK-IN-1
CA/PRAK-IN-1 is a dual inhibitor of carbonic anhydrase (Carbonic Anhydrase) and PRAK, with a Ki of 20.1 nM against hCA IX and 16.4 nM against hCA XII. CA/PRAK-IN-1 exhibits inhibitory activity against YES1 kinase, BTK, and MAP4K3. CA/PRAK-IN-1 induces G0/G1 phase arrest of the cancer cell cycle, inhibits DNA synthesis, disrupts hypoxia-driven survival pathways, promotes cell death, and shows broad-spectrum cytotoxicity against tumor cells. CA/PRAK-IN-1 can be used in research on various cancers including leukemia, colon cancer, melanoma, and renal cancer.
For research use only. We do not sell to patients.
- Formula: C26H21N3O5S
- Molecular Weight:487.53
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
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hCA IX 20.1 nM (Ki) |
hCA XII 16.4 nM (Ki) |
GLK/MAP4K3 |
YES1 |
CA/PRAK-IN-1 (Compound 8d) potently and selectively inhibits tumor-associated human carbonic anhydrase isozymes IX (Ki = 20.1 nM) and XII (Ki = 16.4 nM), with significantly stronger inhibitory effects compared to the off-target isozymes I and II[1].
CA/PRAK-IN-1 (0.01-100 μM; 48 h) exhibits broad-spectrum antiproliferative activity against the NCI-60 panel of human tumor cell lines, with consistently low micromolar GI50 values ranging from 0.943 to 5.18 μM, and an overall panel MG-MID of 3.06 μM[1].
CA/PRAK-IN-1 maintains cytotoxic activity against MDA-MB-231 breast cancer cells under both normoxic (IC50 = 13.44 μM) and hypoxic (IC50 = 10.13 μM) conditions, while it shows low cytotoxicity against human normal fibroblast Wi-38 cells (IC50 = 16.25 μM)[1].
CA/PRAK-IN-1 (10 μM) inhibits key cancer-associated kinases, including PRAK (61% inhibition rate), YES1 (54% inhibition rate), BTK (52% inhibition rate), and MAP4K3 (52% inhibition rate)[1].
CA/PRAK-IN-1 (13.44 μM; 24 h) induces G0/G1 cell cycle arrest and inhibits DNA synthesis in MDA-MB-231 breast cancer cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:NCI-60 human tumor cell line panel
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Concentration:10 μM (single-dose screening); 0.01-100 μM (five-dose testing)
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Incubation Time:48 h
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Result:Showed a mean growth inhibition percentage of 131% across the NCI-60 panel in single-dose screening at 10 μM.
Exhibited GI50 values ranging from 0.943 μM (RPMI-8226 leukemia cells) to 5.18 μM (OVCAR-4 ovarian cancer cells) in five-dose testing.
Exhibited notable activity with GI50 = 1.32 μM (CCRF-CEM leukemia cells), 1.59 μM (HCT-15 colon cancer cells), 1.55 μM (LOX IMVI melanoma cells), 1.26 μM (RXF 393 renal cancer cells), and 1.32 μM (MCF-7 breast cancer cells).
Demonstrated a full-panel MG-MID for GI50 of 3.06 μM.
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Cell Line:MDA-MB-231 breast cancer cells
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Concentration:13.44 μM
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Incubation Time:24 h
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Result:Increased the percentage of cells in the G0/G1 phase from 83.73% (control) to 96.18%.
Reduced the S phase population from 15.06% (control) to 2.63%.
Chemical Information
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Molecular Weight 487.53
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Formula C26H21N3O5S
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SMILES
O=S(C1=CC=C(N2N=C(C(/C=C/C3=CC=C(OC)C=C3)=O)C(C(C4=CC=CC=C4)=O)=C2)C=C1)(N)=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)
CA/PRAK-IN-1 Related Classifications
HY-184792 Related Classifications
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