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Cat. No. Product Name CAS No. Information



A-832234 is a potent, selective, reversible MetAP2 inhibitor with IC50 of 19 nM.




ZGN-1061 (Aclimostat) is a novel potent, selective Methionine aminopeptidase 2 (MetAP2) inhibitor being investigated for treatment of diabetes and obesity; reduces body weight in diet-induced obese (DIO) insulin-resistant mice, also produced improvements in metabolic parameters, including plasma glucose and insulin, and, in HepG2 cells, initiated gene changes similar to beloranib; does not increase coagulation markers in dogs and ZGN-1061 had a greatly improved safety profile in rats relative to beloranib.


Phase 2 Clinical




Tosedostat (CHR-2797, CHR2797) is a potent, orally bioavailable aminopeptidases inhibitor with IC50 of 150, 220 and 100 nM for PuSA, aminopeptidase N and leucine aminopeptidase, respectively; exerts antiproliferative effects against a range of tumor cell lines in vitro and in vivo and shows selectivity for transformed over nontransformed cells; inhibits phosphorylation of mTOR substrates and reduces protein synthesis in HL-60 cells.

Blood Cancer

Phase 2 Clinical



1454299-21-8 TP-004 is a potent, selective METAP2 (Methionine aminopeptidase-2) inhibitor.


841202-16-2 JNJ-26993135 is a potent, selective leukotriene A4 hydrolase (LTA4H) inhibitor, inhibits both the epoxide hydrolase and aminopeptidase activities of recombinant human LTA4H with IC50 of 10 nM; has no significant effects on LTC4, lipoxin A4, or PGE2 production; dose-dependently inhibits ex vivo LTB(4) production in blood (IC50=339 nM), in parallel with dose-dependent inhibition of neutrophil influx (ED50, 1-3 mg/kg) and ear edema in murine model of arachidonic acid-induced ear inflammation; selectively inhibited LTB(4) production, without affecting cysteinyl leukotriene production.


681245-85-2 A-800141 is a potent, highly specific, orally bioavailable MetAP2 inhibitor with IC50 of 12 nM, shows no inhibition for MetAP1 (IC50>30 uM); also shows a greater selectivity against other aminopeptidases, as well as a CEREP panel of >80 receptors; causes the formation of GAPDH variants with an unprocessed N-terminal methionine in cell cultures in vitro, exhibits an antiangiogenesis effect and a broad anticancer activity in a variety of tumor xenografts including B cell lymphoma, neuroblastoma, and prostate and colon carcinomas, either as a single agent or in combination with cytotoxic agents; blocks tumor growth and MetAP2 activity in mouse models, which are causally connected to MetAP2 inhibition in vivo.


431077-35-9 PPI-2458 is potent, specific, irreversible methionine aminopeptidase-2 (MetAP-2) inhibitor with IC50 of 0.2 nM, inhibits growth inhibition of HFLS-RA and HUVEC with IC50 of 0.04 nM; significantly attenuates paw swelling when therapeutically administered after the onset of chronic disease in rat model of peptidoglycan-polysaccharide-induced arthritis; exhibits potent antiproliferative activity on NHL lines in vitro (GI50=0.2-1.9 nM) and oral antitumor activity in vivo.

Blood Cancer


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