metap2

Fumagillin (Amebacilin) 由烟曲霉菌中提取的一种抗菌药，有抗阿米巴活性。它通过抑制 HIV-1 viral protein R 活性来抑制 HIV‐1感染。

TP-004 is a potent and reversible methionine aminopeptidase 2 (MetAP2) inhibitor (IC50: 6 nM).

MetAP2-IN-1为MetAP2抑制剂，用于血管生成介导疾病研究。

M8891 is an orally active, reversible and brain penetrant Methionine Aminopeptidase-2 (MetAP-2) inhibitor(IC50 :54nM;Ki:4.33 nM).M8891 inhibits growth of primary endothelial cells as well as tumor cells and demonstrates antiangiogenic and antitumoral acti

A-800141 是一种口服有效且选择性的MetAP2抑制剂，其IC50为12 nM。它对MetAP1的抑制作用较弱 (IC50为36 μM)。GAPDH 可作为A-800141抑制MetAP2的生物标志物。在多种异种移植肿瘤模型中，A-800141展现了抗血管生成和抗癌活性。

BAY-277 是一种 METAP2 的降解剂，对 hMETAP2 的 IC50 值为 5.8 nM，对 mMETAP2 的 IC50 值为 5.9 nM。

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 that demonstrates promising efficacy and safety profiles in preclinical trials. In a mouse model of obesity and insulin resistance, ZGN-1061 exhibits comparable weight loss efficacy to beloranib, while also improving 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.

Fumagillin (GMP)是 Fumagillin 的 GMP 级别试剂。Fumagillin 是一种由烟曲霉菌中提取的一种抗菌药，有抗阿米巴活性。它通过抑制 HIV-1 viral protein R 活性来抑制 HIV‐1感染。

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是一种 MetAP2 靶向自噬介导降解体 (AUTAC)，具有潜在的抗癌活性，可降解 MetAP2 和 FKBP12 蛋白，可用于合成 PROTAC。

Fumagilin-105 作为一种自噬靶向嵌合体 (AUTOTAC), 具备诱发p62自我寡聚化的能力，其在 HEK293 细胞中针对 MetAP2 的DC50值达到 0.7 μM。

Beloranib hemioxalate (ZGN-440; ZGN-433) 作为一种有效的MetAP2抑制剂,主要用于减少食物摄入、体重、脂肪量以及脂肪细胞尺寸.此化合物在抗肥胖活性和肥胖症研究中具有关键作用.