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5 mg

Ref. AG-CR1-3673-M005
AdipoGen Life Sciences
847499-27-8

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Neuf 110.00 H.T.

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Détails Produit

Product description: Potent, selective, reversible orally bioavailable proteasome inhibitor. Synthetic P2 threonine boronic acid. Targets the chymotrypsin-like beta5 subunit of the constitutive 20S proteasome (IC50=3.8nM). Cross-reacts and inhibits the caspase-like/peptidyl-glutamyl peptide-hydrolyzing (PGPH) beta1 subunit (IC50=~70nM). Displays similar potency for the chymotrypsin-like activity of the proteasome compared to bortezomib. Exhibits a favorable cytotoxicity profile toward normal human epithelial cells, bone marrow progenitors and bone marrow-derived stromal cells relative to bortezomib (Prod. No. AG-CR1-3602). Anticancer compound effective against multiple myeloma in vivo. In vitro, blocks the growth of representative human solid and hematological tumor cell lines (IC50s=5.6-34nM). Shown to down-modulate NF-kappaB, induce apoptosis, inhibit angiogenesis and M-CSF-RANKL-induced osteoclastogenesis.

Alternate Names/Synonyms: NPH 007098; CT 47098; CIP 18770; [(1R)-1-[[(2S,3R)-3-Hydroxy-2-[(6-phenylpyridine-2-carbonyl)amino]butanoyl]amino]-3-methylbutyl]boronic acid

CAS: 847499-27-8

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