A-849519
A-849519 is a reversible methionine aminopeptidase-2 (MetAP-2) inhibitor with an IC50 of 19 nM. A-849519 binds to the active site of the Mn2+ form of human MetAP-2, where the oxygen atom of one acidic functional group interacts with the manganese ion, and another heteroatom binds to the water molecule above the two manganese ions, thereby functionally inhibiting enzyme activity. A-849519 inhibits the methionine processing activity of MetAP-2 as well as the proliferation of fibrosarcoma cells. A-849519 can be used in studies related to fibrosarcoma.
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- CAS. Nr.: 904680-01-9
- Formel: C22H25FN2O4S
- Molecular Weight:432.51
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Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biologische Aktivität
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Chemical Information
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Help & FAQs
Biologische Aktivität
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MetAp2 19 nM (IC50) |
A-849519 (Compound 24n) potently inhibits recombinant human Mn2+-bound MetAP2 with an IC50 of 0.019 μM, and its potency is only moderately reduced in the presence of 40 mg/mL HSA (IC50 = 0.084 μM)[2].
A-849519 potently inhibits the proliferation of human fibrosarcoma HT-1080 cells with an EC50 of 0.036 μM, and its potency is only moderately reduced in the presence of 40 mg/mL HSA (EC50 = 0.18 μM)[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS. Nr. 904680-01-9
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Molecular Weight 432.51
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Formel C22H25FN2O4S
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SMILES
OC(C1=C2C(CCCC2)=CC=C1NS(=O)(C3=C(C=C(C=C3)F)/C=C\CN(C)C)=O)=O
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Reinheit & Dokumentation
Verweise
[1]. Heinrich T, et al. Discovery and Structure-Based Optimization of Next-Generation Reversible Methionine Aminopeptidase-2 (MetAP-2) Inhibitors. J Med Chem. 2019;62(10):5025-5039. [Content Brief]
[2]. Sheppard GS, et al. Discovery and optimization of anthranilic acid sulfonamides as inhibitors of methionine aminopeptidase-2: a structural basis for the reduction of albumin binding. J Med Chem. 2006;49(13):3832-3849. [Content Brief]
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
A-849519 Related Classifications
HY-182419 Related Classifications
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