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Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!2025-02-06
40 Results for "
MetAP2
" in MedChemExpress (MCE) Product Catalog:
Products (40)
40 Results for "MetAP2" in MCE Product Catalog:
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1 Cited Publications
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TP-004 is a potent and reversible inhibitor of methionine aminopeptidase 2 (MetAP2), with an IC50 of 6 nM against MetAP2. TP-004 is a chemical probe. TP-004 suppresses MetAP2 enzymatic activity, blocks N-terminal methionine cleavage, impairs protein maturation and stability, and thereby inhibits cell proliferation and angiogenesis. TP-004 can be used for the study of tumors and diseases associated with excessive angiogenesis .
Cat. No.: HY-P4344
CAS No.: 1926163-52-1
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M8891 is an orally active, reversible and brain penetrant Methionine Aminopeptidase-2 (MetAP-2) inhibitor with an IC50 of 54 nM and a Ki 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 [2].
Synonyms: ZGN-1061
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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 .
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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 [2].
Cat. No.: HY-14811
CAS No.: 251111-30-5
Synonyms: ZGN-440; CKD-732 free base
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Beloranib (ZGN-440; CKD-732 free base) is a selective, irreversible inhibitor of methionine aminopeptidase MetAP2 that suppresses appetite and increases energy expenditure. Beloranib 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 significantly reduces food intake, body weight, and fat accumulation, while improving glucose tolerance, insulin sensitivity, and lipid metabolism. Beloranib also elevates energy expenditure and fat oxidation levels, without affecting body temperature, spontaneous activity, or the inflammatory cytokine IL-1β. Beloranib can be used in research on obesity and hypothalamic obesity [2] .
Cat. No.: HY-161743
CAS No.: 2410081-56-8
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PBA-1105 is an autophagy-targeting chimera (AUTOTAC) that induces p62 self-oligomerization. PBA-1105 selectively binds to exposed hydrophobic regions of misfolded proteins, facilitating their degradation via the autophagic pathway. PBA-1105 increases the autophagic flux of Ub-conjugated aggregates .
Cat. No.: HY-RS08350
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METAP2 Human Pre-designed siRNA Set A contains three designed siRNAs for METAP2 gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.
Cat. No.: HY-156959
CAS No.: 19683-98-8
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Ovalicin is a multi-target inhibitor that targets MetAP2, HRH2, JAK2 and TRPV1, with anti-inflammatory and anti-atopic dermatitis activities. Ovalicin covalently binds to MetAP2 to inhibit its function, thereby blocking the replication of Enterocytozoon bieneusi and Vittaforma corneae. Ovalicin alleviates intestinal injury and prolongs survival in infected mouse models, without showing obvious hepatorenal toxicity. Ovalicin attenuates LPS-induced calcium influx, reduces the infiltration of macrophages and mast cells in the skin, and regulates the expression of inflammation-related genes such as IL-31, effectively relieving allergic symptoms in mouse models. Ovalicin can be used for the research of microsporidiosis and atopic dermatitis [2].
Cat. No.: HY-161742
CAS No.: 2410081-58-0
Fumagilin-105 is an autophagy-targeting chimera (AUTOTAC) that degrades MetAP2 via p62-mediated macroautophagy in a ubiquitination-independent manner. Fumagilin-105 can inhibit the migration of tumor cells and induce programmed cell death. Fumagilin-105 has anti-tumor activity. (p62-ZZ ligand (HY-W489121); target-binding ligand (HY-B0751); linker (HY-W245803)) .
Cat. No.: HY-119062
CAS No.: 681245-85-2
A-800141 is an orally active, selective, sulfonamide-based MetAP2 inhibitor (IC50=12 nM) that binds reversibly to MetAP2 and interacts with its manganese ions. A-800141 induces the production of N-terminal methionine-unprocessed GAPDH variants, which in turn triggers G1-phase cell cycle arrest, elevates p21 levels, and reduces the levels of phosphorylated Rb and total cyclin A. A-800141 exhibits anti-angiogenic and tumor growth inhibitory effects, and produces synergistic effects when combined with cytotoxic inhibitors or BCL-2 inhibitors. A-800141 has been widely used in scientific research related to B-cell lymphoma, neuroblastoma, prostate cancer, colon cancer, melanoma and other fields [2] .
Cat. No.: HY-118953
CAS No.: 270902-51-7
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LAF389, a prodrug of LAF153 (HY-183876), is a methionine aminopeptidase (MetAps) inhibitor with an IC50 of 800 nM against MetAp2, and exhibits a maximum inhibition rate of 20% against MetAp1 at 300 nM. LAF389 possesses antiproliferative, antiangiogenic and cytotoxic activities. LAF389 can be used in research related to cancers such as advanced solid tumors [2].
Cat. No.: HY-109188
CAS No.: 2081078-92-2
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Relzomostat (Example 18) is a methionyl aminopeptidase 2 (MetAP2) inhibitor. Relzomostat is used for research on obesity and type 2 diabetes .
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AUTAC1 is a MetAP2-targeting autophagy-mediated degrader (AUTAC). AUTACs contain a degradation tag and a warhead to provide target specificity. AUTAC1 contains an FBnG (p-Fluorobenzyl Guanine) and a Fumagillol moiety. Fumagillol binds covalently to MetAP2 .
(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 .
Cat. No.: HY-14811A
CAS No.: 529511-79-3
Synonyms: ZGN-440 hemioxalate; ZGN-433 hemioxalate; CDK732 hemioxalate
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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 [2] .
Cat. No.: HY-158006
CAS No.: 1631953-52-0
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 .
Cat. No.: HY-103653
CAS No.: 251111-15-6
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CKD-731 is a Fumagillin (HY-B0751) analogue. CKD-731 inhibits the proliferation of calf pulmonary artery endothelial cells (CPAE), lymphoma EL-4 cells and murine leukemia P388D1 cells. CKD-731 exerts the effect of inhibiting MetAP-2 activity and blocking angiogenesis. CKD-731 can be used for the research of anti-angiogenesis-related cancer .
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Protocols
Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!A suitable model is crucial in drug screening experiments. Organs can mimic the three-dimensional functional structure of internal organs, have similar spatial organization to corresponding organs, maintain some key characteristics, and reproduce some physiological functions. They are widely used for modeling and personalized drug screening physiological functions.2025-02-06
