MetAP Inhibitor

YOK24 is an orally active MetAP2 inhibitor and anti-amoebic agent. YOK24 binds covalently to MetAP2 and inhibits its peptidase activity, where MetAP2 is a protein essential for the proliferation of *Entamoeba histolytica*. YOK24 can be used in the research of amoebiasis.

Anticancer agent 313 is a MetAP2 inhibitor with an IC₅₀ of 4.11 μM. Anticancer agent 313 activates the transcription factor ATF4 via a non-canonical mTORC1-dependent pathway. Anticancer agent 313 inhibits cancer cell proliferation. Anticancer agent 313 is applicable to the research of breast cancer and pancreatic cancer.

NS-181 is an orally active MetAP2 inhibitor and antiamebic agent with oral effectiveness.NS-181 functionally inhibits methionine aminopeptidase 2, a protein critical for Entamoeba histolytica proliferation. NS-181 exerts antiamebic activity against Entamoeba histolytica, leading to resolution of amebic liver abscess. NS-181 can be used for the research of amebiasis.

Beloranib (ZGN-440; CKD-732 free base) hemioxalate is a selective, irreversible inhibitor of methionine aminopeptidase MetAP2 that suppresses appetite and increases energy expenditure. Beloranib hemioxalate blocks the enzymatic cleavage of N-terminal methionine from nascent proteins by forming a covalent bond with MetAP2, thereby regulating fatty acid metabolism, adrenergic signaling, and hypothalamic NF-κB expression. Beloranib hemioxalate significantly reduces food intake, body weight, and fat accumulation, while improving glucose tolerance, insulin sensitivity, and lipid metabolism. Beloranib hemioxalate also elevates energy expenditure and fat oxidation levels, without affecting body temperature, spontaneous activity, or the inflammatory cytokine IL-1β. Beloranib hemioxalate can be used in research on obesity and hypothalamic obesity.

5-(2-Nitrophenyl)-2-furoic acid (O-Nitrophenylfuroic acid) is a Mn²⁺-form Escherichia coli methionine aminopeptidase (EcMetAP) inhibitor with an IC₅₀ of 1.08 μM against Escherichia coli. 5-(2-Nitrophenyl)-2-furoic acid selectively inhibits the Mn²⁺-form over the Co²⁺-, Ni²⁺-, and Fe²⁺-forms of EcMetAP, with its carboxyl group preferentially coordinating with Mn²⁺ ions as the major determinant for this metalloform selectivity. 5-(2-Nitrophenyl)-2-furoic acid can be used for the research of bacterial infection.

ecMetAP-IN-1 is an inhibitor of E. coli methionine aminopeptidase (ecMetAP) with an IC₅₀ of 2.086 μM. ecMetAP-IN-1 is applicable to research related to bacterial infections caused by E. coli.