Formulation: A solid
Formal Name: N-[4-[3-[[[5-(dimethylamino)-1-naphthalenyl]sulfonyl]amino]phenyl]-2-thiazolyl]-acetamide
Purity: ≥98%
Formula Markup: C23H22N4O3S2
Formula Weight: 466,6
Shelf life (days): 1460
CAS Number: 1609402-14-3
Notes: HA-15 is an inhibitor of glucose-regulated protein 78 kDa (GRP78), also known as heat shock 70 kDa protein 5 (HspA5) and immunoglobulin heavy chain-binding protein (BiP), a cellular chaperone.{64581} It binds to GRP79 in a cell-free assay and increases the expression of the genes encoding the unfolded protein response (UPR) proteins EIF2AK3, IRE1α, ATF6, DDIT3, and XBP1, as well as the apoptosis-associated genes JUN and BCL2 and the autophagy marker gene LC3. HA-15 decreases the viability of A375 melanoma cells (IC50 = 2.5 µM). In vivo, HA-15 (0.7 mg/animal per day) reduces tumor volume and induces intratumor apoptosis and autophagy in an A375 mouse xenograft model. HA-15 also increases osteogenesis and reduces bone loss in a mouse model of ovariectomy-induced osteoporosis.{64582}
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