1. Metabolic Enzyme/Protease
  2. MetAP
  3. A-849519

A-849519 是一种可逆性甲硫氨酸氨基肽酶-2 (MetAP-2) 抑制剂,其 IC50 为 19 nM。A-849519 结合于人源 MetAP-2 的 Mn2+ 形式的活性位点,其中一个酸性官能团的氧原子与锰离子接触,另一个杂原子结合两个锰离子上方的水分子,从而在功能上抑制酶活性。A-849519 可抑制 MetAP-2 的甲硫氨酸加工活性以及纤维肉瘤细胞的增殖。A-849519 可用于纤维肉瘤的相关研究。

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A-849519

A-849519 Chemical Structure

CAS No. : 904680-01-9

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查看 MetAP 亚型特异性产品:

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

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].

IC50 & Target[2]

MetAp2

19 nM (IC50)

体外研究
(In Vitro)

A-849519 (Compound 24n) 可强效抑制结合 Mn2+ 的重组人源 MetAP2,其 IC50 为 0.019 μM;在 40 mg/mL HSA 存在的情况下,其效力仅中度下降 (IC50 = 0.084 μM)[2]
A-849519 可强效抑制人纤维肉瘤 HT-1080 细胞的增殖,其 EC50 为 0.036 μM;在 40 mg/mL HSA 存在的情况下,其效力仅中度降低 (EC50 = 0.18 μM)[2]

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

分子量

432.51

Formula

C22H25FN2O4S

CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

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

纯度 & 产品资料
参考文献
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    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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产品名称:
A-849519
目录号:
HY-182419
需求量: