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Cat. No. Product Name CAS No. Information
PC-63317

A-832234

904679-91-0

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

PC-35112

TP-004

1454299-21-8 TP-004 is a potent, selective METAP2 (Methionine aminopeptidase-2) inhibitor.
PC-63409

JNJ-26993135

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.
PC-63347

A-800141

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.
PC-63319

PPI-2458

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

Discontinued

PC-63318

A-357300

369358-07-6 A-357300 is a potent, selective, reversible MetAP2 inhibitor with IC50 of 0.12 uM, does not inhibit MetAP1 or leucine aminopeptidases at 10 uM; suppresses tumor growth preclinically without the toxicities observed with TNP-470, induces cytostasis by cell cycle arrest at the G(1) phase selectively in endothelial cells and in a subset of tumor cells, but not in most primary cells of nonendothelial type; inhibits angiogenesis both in vitro and in vivo and shows potent antitumor efficacy in carcinoma, sarcoma, and neuroblastoma murine models.
PC-63316

LAF389

270902-51-7 LAF389 is a potent methionine aminopeptidase (MetAP) inhibitor with IC50 of 800 nM for MetAP-2, inhibits both MetAp1 and 2, potently inhibits HUVEC proliferation with IC50 of 20 nM; demonstrates both antiproliferative and antiangiogenetic properties, and preclinical investigations showed a broad antitumour activity.

Blood Cancer

Phase 1 Discontinued

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