904680-01-9
Chemical Structure
A-849519
- CAS No.: 904680-01-9
- Formula:C22H25FN2O4S
- Molecular Weight:432.51
InChIKey: CTZLIARLNXSXGL-ALCCZGGFSA-N
SMILES: OC(C1=C2C(CCCC2)=CC=C1NS(=O)(C3=C(C=C(C=C3)F)/C=C\CN(C)C)=O)=O
Biological Activity: 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[1][2].
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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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- [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]
Keywords
