HA-15

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. It binds to GRP79 in a cell-free assay and increases the expression of the genes encoding the unfolded protein response (UPR) proteins EIF2AK3, IRE1alpha, 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.Formal Name: N-[4-[3-[[[5-(dimethylamino)-1-naphthalenyl]sulfonyl]amino]phenyl]-2-thiazolyl]-acetamide. CAS Number: 1609402-14-3. Molecular Formula: C23H22N4O3S2. Formula Weight: 466.6. Purity: >98%. Formulation: (Request formulation change), A solid. Solubility: DMF: 15 mg/ml, DMSO: 30 mg/ml, Ethanol: 15 mg/ml, PBS (pH 7.2): insol. lambdamax: 219 nm. SMILES: O=C(C)NC1=NC(C2=CC(NS(=O)(C3=CC=CC4=C(N(C)C)C=CC=C43)=O)=CC=C2)=CS1. InChi Code: InChI=1S/C23H22N4O3S2/c1-15(28)24-23-25-20(14-31-23)16-7-4-8-17(13-16)26-32(29,30)22-12-6-9-18-19(22)10-5-11-21(18)27(2)3/h4-14,26H,1-3H3,(H,24,25,28). InChi Key: LBSMEKVVMYSTIH-UHFFFAOYSA-N.