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).

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.

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.

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.

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.

YUM70 is a potent and selective inhibitor of glucose-regulated protein 78 (GRP78), 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.

Dehydroeffusol (Dehydro Effusol) possesses anti-cancer, anxiolytic and sedative properties. Dehydroeffusol inhibits gastric cancer cell growth and tumorigenicity by selectively inducing tumor-suppressive endoplasmic reticulum stress and a moderate apoptosis.

Anti-Human/Mouse GRP78 Antibody (C38) is a mouse IgG2b kappa isotype antibody designed for in vivo use, specifically targeting GRP78. The recommended isotype control for this antibody is Mouse IgG2b kappa, Isotype Control.

Anti-Human/Mouse GRP78 Antibody (N88) is an IgG1, κ antibody inhibitor derived from mice, designed to target human or mouse GRP78.

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].

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.

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.

HSP70-IN-7 is a non-selective HSP70 inhibitor with dissociation constants (Kd) of 4.71, 2.16, and 2.93 μM for HSP70, GRP75, and GRP78, respectively. It exhibits selective toxicity toward breast cancer cells, induces apoptosis, and effectively inhibits the characteristics of breast cancer stem cells (BCSC). HSP70-IN-7 is useful for breast cancer research.

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

Palmitic acid-13C sodium is the 13C-labeled variant of palmitic acid sodium (T77788), 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.

Palmitic acid-13C16 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.

Palmitic acid-13C2 is the 13C-labeled Palmitic acid. Palmitic acid (T2908) is a long-chain saturated fatty acid commonly found in both animals and plants. Palmitic acid (T2908) can induce the expression of glucose-regulated protein 78 (GRP78) and CCAAT/enhancer binding protein homologous protein (CHOP) in in mouse granulosa cells.

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.

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].

Palmitic acid-D2 is the deuterated form of Palmitic acid. Palmitic acid (T2908) is a long-chain saturated fatty acid commonly found in animals and plants. It is known to induce the expression of glucose-regulated protein 78 (GRP78) and CCAAT/enhancer-binding protein homologous protein (CHOP) in mouse granulosa cells.

Palmitic acid-D9 is the deuterated form of Palmitic acid. A long-chain saturated fatty acid, Palmitic acid (T2908) is commonly found in animals and plants. It has the ability to induce the expression of glucose-regulated protein 78 (GRP78) and CCAAT/enhancer-binding protein homologous protein (CHOP) in murine granulosa cells.

Palmitic acid-D4-1 is the deuterated form of Palmitic acid. This compound is a long-chain saturated fatty acid commonly found in animals and plants. Palmitic acid (T2908) has the ability to induce the expression of glucose-regulated protein 78 (GRP78) and CCAAT/enhancer-binding protein homologous protein (CHOP) in murine granulosa cells.

Palmitic acid-D31 is the deuterated form of palmitic acid. Palmitic acid (T2908) is a long-chain saturated fatty acid commonly found in animals and plants. It can induce the expression of glucose-regulated protein 78 (GRP78) and CCAAT/enhancer-binding protein homologous protein (CHOP) in murine granulosa cells.