2082752-83-6
Chemical Structure
Aclimostat
Synonym(s): ZGN-1061
- CAS No.: 2082752-83-6
- Formula:C26H42N2O6
- Molecular Weight:478.62
IUPAC Name: (3R,4S,5S,6R)-5-methoxy-4-((2R,3R)-2-methyl-3-(3-methylbut-2-en-1-yl)oxiran-2-yl)-1-oxaspiro[2.5]octan-6-yl 3-(2-morpholinoethyl)azetidine-1-carboxylate
InChIKey: QJWJPMLDQYEPPW-AUKZVGPFSA-N
SMILES: C[C@]1([C@H](O1)C/C=C(C)\C)[C@]2([H])[C@]3(CC[C@H]([C@H]2OC)OC(N4CC(C4)CCN5CCOCC5)=O)CO3
Biological Activity: Aclimostat (ZGN-1061) is a methionine aminopeptidase 2 (MetAP2) inhibitor. Aclimostat exhibits anti-obesity, anti-diabetic and ovarian cancer-related activities, and does not readily distribute to the central nervous system. Aclimostat acts on the active site of MetAP2 via irreversible covalent binding, and blocks enzyme activity through interactions with His231 and His339. Aclimostat regulates gene expression, reduces fat mass, plasma glucose, insulin levels, LDL-C, hs-CRP and leptin levels, while increasing adiponectin levels. Aclimostat can be used in research related to type 2 diabetes, overweight, obesity and ovarian cancer[1][2][3][4][5].
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Aclimostat | 98.0% | Aclimostat (ZGN-1061) is a methionine aminopeptidase 2 (MetAP2) inhibitor. Aclimostat exhibits anti-obesity, anti-diabetic and ovarian cancer-related activities, and does not readily distribute to the central nervous system. Aclimostat acts on the active site of MetAP2 via irreversible covalent binding, and blocks enzyme activity through interactions with His231 and His339. Aclimostat regulates gene expression, reduces fat mass, plasma glucose, insulin levels, LDL-C, hs-CRP and leptin levels, while increasing adiponectin levels. Aclimostat can be used in research related to type 2 diabetes, overweight, obesity and ovarian cancer. | ||||||||||||||||||||
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- [1]. Wentworth JM, et al. The methionine aminopeptidase 2 inhibitor ZGN-1061 improves glucose control and weight in overweight and obese individuals with type 2 diabetes: A randomized, placebo-controlled trial. Diabetes, obesity & metabolism. 2020 Jul;22(7):1215-1219. [Content Brief]
- [2]. Burkey BF, et al. Preclinical Efficacy and Safety of the Novel Antidiabetic, Antiobesity MetAP2 Inhibitor ZGN-1061. J Pharmacol Exp Ther. 2018 May;365(2):301-313. [Content Brief]
- [3]. Wu L, et al. METAP2 inhibits K48-linked ubiquitination of YTHDF2 to promote ovarian cancer progression. Oncogene. 2025 Dec;44(46):4505-4519. [Content Brief]
- [4]. Malloy J, et al. Single and multiple dose evaluation of a novel MetAP2 inhibitor: Results of a randomized, double-blind, placebo-controlled clinical trial. Diabetes, obesity & metabolism. 2018 Aug;20(8):1878-1884. [Content Brief]
- [5]. Moon DO, et al. MetAP2 as a Therapeutic Target for Obesity and Type 2 Diabetes: Structural Insights, Mechanistic Roles, and Inhibitor Development. Biomolecules. 2024 Dec 10;14(12):1572. [Content Brief]
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