grp94

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

Grp94 Inhibitor-3 (Compound C6) is a selective inhibitor of glucose-regulated protein 94 (Grp94), with an affinity of 5.52 μM. It shows potential for research in primary open-angle glaucoma and metastatic cancer.

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

Grp94-IN-2 is a inhibitor of Grp94.

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.

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.

Luminespib (VER-52296) is an HSP90 inhibitor that inhibits HSP90α and HSP90β (IC50=7.8 21 nM). Luminespib has antitumor activity and is used in studies of head and neck tumors, among others.

Alvespimycin hydrochloride (BMS 826476) is a potent HSP90 inhibitor with IC50 of 62 nM. Phase 2.

SNX2112 (PF 04928473) is an orally active Hsp90 inhibitor, with a Kd of 16 nM.

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

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.

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

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

KUNG65 acts as a selective Grp94 inhibitor, demonstrating a target dissociation constant (K_d) of 540 nM. It exhibits a minimum selectivity of 73-fold compared to other Hsp90 isoforms.

Alvespimycin (17-DMAG) is a potent Hsp90 inhibitor that binds to Hsp90, exhibiting potential anticancer activity.

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

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.

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.

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.

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].

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].