grp78

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).

GRP78-IN-2 is a glucose regulatory protein 78 (GRP78) inhibitor that preferentially targets GRP78 on the cell surface and has significant anti-angiogenic and anti-cancer effects without affecting other normal cells.

GRP78-IN-1 displays interactions with specific residues on the GRP78 protein with a binding energy of -8.07 kcal/mol. This compound possesses potent cytotoxic and anti-proliferative effects on cancer cells, particularly demonstrating promising apoptosis in breast cancer cells and wound healing properties [1].

Questiomycin A derivatives 18 TFA is A Questiomycin A derivative with antibacterial and anticancer activity and inhibition of the expression of the cell-protective ER chaperone protein GRP78.

HA15 targets specifically BiP/GRP78/HSPA5. HA15 exhibits anti-cancerous activity on all melanoma cells tested, including cells isolated from patients and cells that developed resistance to BRAF inhibitors.

VER-155008 is a potent Hsp70 family inhibitor with IC50 of 0.5 μM, 2.6 μM, and 2.6 μM in cell-free assays for HSP70, HSC70, and GRP78, respectively, >100-fold selectivity over HSP90.

BOLD-100 free base (NKP-1339; IT-139), a ruthenium-based anticancer agent, inhibits stress-induced GRP78 upregulation, thus disrupting endoplasmic reticulum (ER) homeostasis. This action induces ER stress and unfolded protein response (UPR), interfering with the intricate relationship between ER-stress response, lysosome dynamics, and autophagy execution.

HM03 trihydrochloride is a potent and selective inhibitor of HSPA5, also known as Bip or Grp78. It exhibits anticancer activity.

BiP inducer X (BIX) is a selective inducer of immunoglobulin heavy chain binding protein (BiP)/GRP78 and an ER chaperone inducer. BiP inducer X prevents cell death in neurons and retinal cell lines.

Calcium palmitate, a long-chain saturated fatty acid prevalent in animals and plants, induces the expression of glucose-regulated protein 78 (GRP78) and CCAAT/enhancer binding protein homologous protein (CHOP) in mouse granulosa cells. It is employed to establish a cell steatosis model [1] [2].

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].

Sodium palmitate-13C is the 13C-labeled variant of palmitic acid, a long-chain saturated fatty acid prevalent in animals and plants. This compound has been shown to induce the expression of glucose-regulated protein 78 (GRP78) and CCAAT/enhancer-binding protein homologous protein (CHOP) in mouse granulosa cells.

Neoisoliquiritigenin, isolated from Spatholobus suberectus, inhibits cell proliferation and induces cell apoptosis in breast cancer by directly binding to GRP78 to regulate the β-catenin pathway

Palmitic acid-13C2 is the 13C-labeled Palmitic acid. Palmitic acid is a long-chain saturated fatty acid commonly found in both animals and plants. Palmitic acid can induce the expression of glucose-regulated protein 78 (GRP78) and CCAAT/enhancer binding protein homologous protein (CHOP) in in mouse granulosa cells.

YUM70 is a potent and selective glucose-regulated protein 78 (GRP78) inhibitor(with an IC50 of 1.5 μM for inhibiting GRP78 ATPase activity of the full-length protein). It induces endoplasmic reticulum (ER) stress-mediated apoptosis in pancreatic cancer.

Questiomycin A is an antibiotic produced in crème fraiche with antibacterial and anticancer activities. Questiomycin A suppresses expression of GRP78, a cell-protective ER chaperone protein.

Palmitic acid-13C16 sodium, a 13C-labeled form of the naturally occurring saturated fatty acid Palmitic acid sodium, is prevalent in animals and plants. This compound can trigger the expression of glucose-regulated protein 78 (GRP78) and CCAAT/enhancer binding protein homologous protein (CHOP) in mouse granulosa cells.