MetAP

Methionine Aminopeptidase

Methionine aminopeptidase (MetAP) is an enzyme that plays a crucial role in protein biosynthesis. MetAP is responsible for the removal of the N-terminal methionine residue from nascent polypeptide chains, which is essential for the proper folding, maturation and function of many proteins. MetAP1 and MetAP2 have different subcellular localizations and substrate specificities. MetAP1 is mainly involved in the processing of cytosolic proteins. MetAP2 is of particular interest in cancer research as it is involved in angiogenesis and has been targeted for anti-cancer drug development. Inhibition of MetAP2 can disrupt the growth and proliferation of cancer cells by interfering with the processing of certain proteins involved in angiogenesis^[1]^[2].

References:

[1]. Lowther WT, Matthews BW. Structure and function of the methionine aminopeptidases. Biochim Biophys Acta. 2000 Mar 7;1477(1-2):157-67. [Content Brief]

[2]. Heinrich T, et al. Methionine aminopeptidases[M]//Metalloenzymes. Academic Press, 2024: 343-373.

MetAP Inhibitors (16)

MetAP Related Products (16):

Cat. No.	Product Name	Effect	Purity	Chemical Structure

HY-133016

M8891	Inhibitor	98.97%
M8891 is an orally active, reversible and brain penetrant Methionine Aminopeptidase-2 (MetAP-2) inhibitor with an IC₅₀ of 54 nM and a K_i of 4.33 nM. M8891 does not inhibit MetAP-1 (IC₅₀>10 µM). M8891 inhibits growth of primary endothelial cells as well as tumor cells and demonstrates antiangiogenic and antitumoral activity.

HY-120868

TP-004	Inhibitor	98.89%
TP-004 is a potent and reversible inhibitor of methionine aminopeptidase 2 (MetAP2), with an IC₅₀ of 6 nM.

HY-128147

MetAP-2-IN-6	Inhibitor	99.55%
MetAP-2-IN-6 is a MetAP2 inhibitor. MetAP-2-IN-6 can be used for research in conditions mediated by angiogenesis.

HY-P4344

Met-Gly-Pro-AMC	Inhibitor	99.69%
Met-Gly-Pro-AMC is a fluorescent peptide substrate of MetAP2.

HY-114196

Aclimostat	Inhibitor	≥98.0%
Aclimostat (ZGN-1061) is a potent inhibitor of the MetAP2 enzyme and displays favorable efficacy and safety in preclinical studies. ZGN-1061 produced similar efficacy as beloranib for weight loss, improvements in metabolic parameters in a mouse model of obesity and insulin resistance, and concordant changes in gene transcription in HepG2 cells.

HY-168967

BAY-277	Inhibitor
BAY-277 is a METAP2 degrader, with IC₅₀ values of 5.8 nM and 5.9 nM for hMETAP2 and mMETAP2, respectively.

HY-119062

A-800141	Inhibitor
A-800141 is an orally active and selective MetAP2 inhibitor with an IC₅₀ of 12 nM. A-800141 has weak inhibitory activity for MetAP1 (IC₅₀ : 36 μM). GAPDH can be used as a biomarker to monitor the MetAP2 inhibition of A-800141. A-800141 has antiangiogenic and anticancer activity in a variety of xenograft tumor models.

HY-14811

Beloranib	Inhibitor
Beloranib is a fumagillin-class methionine aminopetidase-2 (MetAP2) inhibitor. Beloranib decreases food intake, body weight, fat mass, and the size of adipocytes.

HY-133016A

(R)-M8891	Inhibitor	98.67%
(R)-M8891 (compound R-9) is a less active isomer of M8891. M8891 is an orally active, reversible and brain penetrant Methionine Aminopeptidase-2 (MetAP-2) inhibitor.

HY-109188

Relzomostat	Inhibitor
Relzomostat is a methionine aminopeptidase 2 (MetAP2) inhibitor.Relzomostat may be useful for the research of obesity, type 2 diabetes, and other obesity-associated conditions.

HY-148442

ecMetAP-IN-1	Inhibitor
ecMetAP-IN-1 (compound 17) is a potent ecMetAP inhibitor with an IC₅₀ value of 2.086 µM.

HY-13731

PPI-2458	Inhibitor	99.67%
PPI-2458 is a potent, orally active, selective and irreversible inhibitor of methionine aminopeptidase-2 (MetAP-2). PPI-2458 can be used for arthritis and lymphoma research.

HY-146396

Anticancer agent 51	Inhibitor
Anticancer agent 51 (compound 3d) is a potent anticancer agent with an K_i of 731.62 nM. Anticancer agent 51 shows anticancer activity. Anticancer agent 51 has the potential for the research of prostate cancer.

HY-158006

SDX-7539	Inhibitor
SDX-7539 is a selective inhibitor for Methionine aminopeptidase type 2 (MetAP2). SDX-7539 inhibits proliferarion of HUVECs with an IC₅₀ of 120 μM. SDX-7539 exhibits antitumor activity in NSCLC xenograft athymic nude mice.

HY-126564

Ebelactone A	Inhibitor
Ebelactone A is a mycolic acid β-lactone, which exhibits inhibitory activity for esterase, lipase, fMet aminopeptidase (fMet AP) and PNBase, with IC₅₀s of 56, 3, 8 and 7.5 μM, respectively. Ebelactone A inhibits cutinase, exhibits plants protective potency against Erysiphe graminis.

HY-14811A

Beloranib hemioxalate	Inhibitor
Beloranib (ZGN-440; ZGN-433) hemioxalate is a fumagillin-class methionine aminopetidase-2 (MetAP2) inhibitor. Beloranib hemioxalate decreases food intake, body weight, fat mass, and the size of adipocytes. Beloranib hemioxalate plays an important role in anti-obesity activity or obesity research.

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