grp94 inhibitor

Grp94 Inhibitor-1 is a potent and selective inhibitor of Grp94 with an IC50 of 2 nM.

Grp94 Inhibitor-2 (compound 23) is a cyclopropane analog that exhibits high affinity for Glucose Regulated Protein 94 (Grp94), with dissociation constants (Kd) of 0.48 µM for Grp94 and 0.65 µM for Hsp90α.

PU-WS13 hydrobromide is a GRP94 inhibitor with anti-inflammatory activity and inhibits the proliferation of M2-like macrophages in mouse TNBC tumors.

PU-H54 is a purine-based inhibitor of Grp94. It is a Grp94-selective resorcinol-based inhibitor isolated through probing of the exclusive binding region of S2 subpocket in Grp94.

NVP-HSP990 (HSP990) is an effective and specific HSP90α β inhibitor (IC50: 0.6 0.8 nM).

VER-82576 (NVP-BEP800), a synthetic HSP90β inhibitor (IC50: 58 nM), exhibits >70-fold selectivity against Hsp90 family members Trap-1 and Grp94.

TRAP1-IN-1 (compound 35) is a potent, selective TRAP1 inhibitor affecting the mitochondrial variant of Hsp90. It exhibits over 250-fold greater selectivity for TRAP1 compared to Grp94, destabilizes TRAP1 tetramers, and promotes the degradation of TRAP1 client proteins. Additionally, TRAP1-IN-1 impedes mitochondrial complex I activity involved in oxidative phosphorylation (OXPHOS), compromises the mitochondrial membrane potential, and augments glycolytic metabolism [1].

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.

Grp94-IN-2 is a inhibitor of Grp94.

KUNG94 is a potent and selective inhibitor of Glucose regulated protein 94 (Grp94) (IC50 = 8 nM), the endoplasmic reticulum resident of the 90 kDa heat shock protein (Hsp90) family.

PU-H54-iso is a novel Hsp90- and Grp94-selective inhibitor.

Radamide is an inhibitor of Grp94.

KUNG38 is a purine-based inhibitor of Grp94.

4-Br-Bnlm, with an EC 50 of 0.96 µM, acts as a selective inhibitor of glucose-regulated protein 94 (Grp94). It effectively reduces both mutant and wild-type misfolded myocilin proteins in cells, thereby enhancing the clearance of toxic forms of myocilin and diminishing myocilin toxicity [1] [2].