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Merck
CN

654271

MetAP2 Inhibitor, A832234 - Calbiochem

Synonym(s):

Methionine aminopeptidase-2 Inhibitor, 2-[({2-[(1Z)-3-(Diethylamino)-1-propenyl]-4-fluorophenyl}-sulfonyl)amino]-5,6,7,8-tetrahydro-1-naphthalenecarboxylic Acid, Methionyl aminopeptidase 2 Inhibitor

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assay

≥97% (HPLC)

form

solid

potency

11 nM IC50

color

light beige

solubility

DMSO: 5 mg/mL, pale yellow

General description

A cell-permeable anthranilic acid sulfonamide compound that acts as a potent and reversible inhibitor of methionine aminopetidase-2 (MetAP2, IC50 = 11 nM). Acts by directly targeting the active site of MetAP2 without any significant binding to human serum albumin. Also shown to inhibit cellular MetAP2 activity (EC50 = 5.3 nM) and block the proliferation of HT1080 fibrosarcoma cells (EC50 = 6 nM).
The MetAP2 Inhibitor, A832234 controls the biological activity of MetAP2.

Biochem/physiol Actions

MetAP2

Preparation Note

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

Storage Class

10-13 - German Storage Class 10 to 13

Regulatory Information

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George S Sheppard et al.
Journal of medicinal chemistry, 49(13), 3832-3849 (2006-06-23)
Methionine aminopeptidase-2 (MetAP2) is a novel target for cancer therapy. As part of an effort to discover orally active reversible inhibitors of MetAP2, a series of anthranilic acid sulfonamides with micromolar affinities for human MetAP2 were identified using affinity selection

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