grp94

Grp94 Inhibitor-1 is a potent, selective Grp94 inhibitor (IC50 : 2 nM).

Grp94-IN-2 is a inhibitor of Grp94.

EPZ032597 is a novel selective inhibitor of SMYD2 with an IC50 of 16 nM. EPZ032597 has anticancer activity and can be used to prevent and treat pancreatic cancer.

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

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].

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.

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.

Retaspimycin Hydrochloride is a potent and water-soluble Hsp90 inhibitor(Hsp90 and Grp9 with EC50s of 119 nM).

Alvespimycin (17-DMAG) is a potent Hsp90 inhibitor with potential anticancer activity, which acts by binding to Hsp90.

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

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.

Radamide is an inhibitor of Grp94.

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

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

Retaspimycin is a potent and water-soluble Hsp90 inhibitor(EC50s of 119 nM for both Hsp90 and Grp9).

KUNG38 is a purine-based inhibitor of Grp94.