metap2

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

Fumagillin (Amebacilin) is a selective and potent irreversible inhibitor of Methionine aminopeptidase 2 (MetAP2), used as an antibiotic to treat microsporidiosis.

MetAP2-IN-1 is a selective inhibitor of MetAP2, a target involved in angiogenesis-related conditions, suitable for research applications [1].

M8891 is an orally active, reversible, and brain-penetrant Methionine Aminopeptidase-2 (MetAP-2) inhibitor (IC50: 54 nM; Ki: 4.33 nM). It inhibits the growth of primary endothelial cells and tumor cells, demonstrating both antiangiogenic and antitumoral activity.

A-800141 is an orally active and selective MetAP2 inhibitor with an IC50 of 12 nM, while showing weaker inhibitory activity against MetAP1 (IC50: 36 μM). GAPDH can serve as a biomarker for monitoring the inhibition of MetAP2 by A-800141. This compound exhibits anti-angiogenic and anticancer properties in various xenograft tumor models.

BAY-277 is a degrader of METAP2, with IC50 values of 5.8 nM for human METAP2 (hMETAP2) and 5.9 nM for mouse METAP2 (mMETAP2).

SDX-7539 is a selective MetAP2 inhibitor that inhibits the proliferation of HUVEC, with an IC50 of 120 μM. It has demonstrated antitumor activity in xenografted NSCLC in athymic nude mice.

Relzomostat is a MetAP2 inhibitor, specifically targeting methionine aminopeptidase 2. It holds potential in research concerning obesity, type 2 diabetes, and other conditions associated with obesity.

Aclimostat (ZGN-1061) is a highly potent inhibitor of the MetAP2 enzyme, demonstrating promising efficacy and safety profiles in preclinical trials. In a mouse model of obesity and insulin resistance, ZGN-1061 shows comparable weight loss efficacy to beloranib and improves metabolic parameters. Additionally, ZGN-1061 induces consistent changes in gene transcription in HepG2 cells, further supporting its positive pharmacological effects.

A-849519 is a reversible inhibitor of MetAP2 that has demonstrated anti-angiogenesis and anticancer activity in a number of in vitro and in vivo models. In this study, we evaluated the anticancer activity of A-849519 in a modified Dunning model of androgen-independent prostate cancer and compared its efficacy with TNP-470, an established MetAP2 inhibitor.

PPI-2458 is a synthetic derivative of fumagillin with antineoplastic and cytotoxic properties. PPI-2458 irreversibly inhibits the enzyme methionine aminopeptidase type 2 (MetAP2), thereby preventing abnormal cell growth and angiogenesis. PPI-2458 is reported to have a better toxicity profile compared to other agents of its class.

A-357300 is a potent, selective, reversible MetAP2 inhibitor with IC50 of 0.12 uM. Methionine aminopeptidase 2 inhibition is an effective treatment strategy for neuroblastoma in preclinical models.

AUTAC1 is a MetAP2-targeted autophagy-mediated degrader (AUTAC) with potential anticancer activity that degrades MetAP2 and FKBP12 proteins and can be used to synthesize PROTAC.

Fumagilin-105, an autophagy-targeting chimera (AUTOTAC), induces self-oligomerization of p62 and exhibits a DC50 of 0.7 μM against MetAP2 in HEK293 cells.

Beloranib hemioxalate (ZGN-440; ZGN-433) is an inhibitor of MetAP2. It significantly reduces food intake, body weight, fat mass, and the size of adipocytes. This compound plays a vital role in research related to anti-obesity activities and obesity management.

Cis-Fumagillin methyl ester inhibits both MetAP2 and MetAP1.