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.
For research use only. We do not sell to patients.
- CAS No.: 904680-01-9
- Formula: C22H25FN2O4S
- Molecular Weight:432.51
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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
- Protocols
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
Description
IC50 & Target
[2]|
MetAp2 19 nM (IC50) |
In Vitro
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. Further protocols information, click here.
Chemical Information
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CAS No. 904680-01-9
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Molecular Weight 432.51
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Formula 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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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.
Protocols
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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
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Cell Viability Determination by MTT Colorimetric Assay
The following protocol uses the MTT colorimetric assay as a classic literature-established method for assessing cell viability/metabolic activity in cultured mammalian cells. MTT[3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide] is reduced by metabolically active cells to a colored formazan product; the amount of formazan is quantified spectrophotometrically and provides an indirect measure of metabolically active viable cells. Importantly, MTT reduction reflects cellular oxidoreductase/metabolic activity rather than an absolute direct count of living cells, so changes in cellular metabolism can alter the signal independently of cell number.
Purity & Documentation
References
[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
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
A-849519 Related Classifications
HY-182419 Related Classifications
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