grp78-in-3

GRP78-IN-3, a potent small-molecule-competitive inhibitor of Hsp70 substrate binding and is a selective Grp78 (HSPA5) inhibitor with an IC50 of 0.59 μM. GRP78-IN-3 is 7-fold selective for HspA5 compared to HspA9 (IC50 of 4.3 μM) and >20-fold selective for HspA5 compared to HspA2 (IC50 of 13.9 μM).

COX-2-IN-55 (compound 1) is an orally active Celecoxib analogue with broad-spectrum anticancer properties and relatively weak COX-2 inhibition. It specifically inhibits SERCA2, leading to increased caspase-3 cleavage and DR5 levels, which activates GRP78 and suppresses the progression of triple-negative breast cancer (TNBC). Additionally, COX-2-IN-55 downregulates the angiogenesis markers VEGF-α and IL-8, thereby inhibiting microvessel formation.

1,2-Dipalmitoyl-3-Octanoyl-rac-glycerol, a triacylglycerol, has palmitic acid at its sn-1 and sn-2 positions, and octanoic acid at the sn-3 position. Palmitic acid, a long-chain saturated fatty acid found in both animals and plants, can induce glucose-regulated protein 78 (GRP78) and CCAAT/enhancer binding protein homologous protein (CHOP) expression in mouse granulosa cells. Octanoic acid, an oily liquid with a slightly unpleasant rancid taste, is utilized in ester production for perfumery, dye manufacturing, and also serves as a tremor-suppressing agent [1] [2] [3] [4].

12-Dipalmitoyl-3-Linoelaidoyl-rac-glycerol is a triacylglycerol containing palmitic acid in the sn-1 and sn-2 positions and linolelaidic acid in the sn-3 position. Palmitic acid is a long-chain saturated fatty acid commonly found in animals and plants, capable of inducing the expression of glucose-regulated protein 78 (GRP78) and CCAAT/enhancer-binding protein homologous protein (CHOP) in mouse granulosa cells. Linolelaidic acid, an omega-6 trans fatty acid (TFA), serves as an energy source and is an essential nutrient that can be incorporated into enteral, parenteral, and infant formulas. Additionally, linolelaidic acid is utilized in heart disease research.