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^[1][2].

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.

432.51

C₂₂H₂₅FN₂O₄S

904680-01-9

OC(C1=C2C(CCCC2)=CC=C1NS(=O)(C3=C(C=C(C=C3)F)/C=C\CN(C)C)=O)=O

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [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]