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Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!2025-02-06
22 Results for "
Grp94 Inhibitor
" in MedChemExpress (MCE) Product Catalog:
Products (22)
22 Results for "Grp94 Inhibitor" in MCE Product Catalog:
9
9 Publications Verification
Synonyms: TAS-116
Pimitespib (TAS-116) is an oral bioavailable, ATP-competitive, highly specific HSP90α/HSP90β inhibitor (Kis of 34.7 nM and 21.3 nM, respectively) without inhibiting other HSP90 family proteins such as GRP94 . Pimitespib demonstrates less ocular toxicity .
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7 Cited Publications
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BiP inducer X, a selective inducer of immunoglobulin heavy chain binding protein (BiP)/GRP78, is an effective ER (endoplasmic reticulum) stress inhibitor. BiP inducer X preferentially induces BiP with slight inductions of GRP94, calreticulin, and C/EBP homologous protein. BiP inducer X protects neurons from ER stress .
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5 Cited Publications
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Grp94 Inhibitor-1 is a potent, selective Grp94 inhibitor with an IC50 value of 2 nM, and over 1000-fold selectivity to Grp94 against Hsp90α .
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VER-82576 (NVP-BEP800) is a potent, orally available and selective Hsp90 inhibitor, with an IC50 of 58 nM for Hsp90β; VER-82576 also slightly blocks Grp94 and Trap-1, with IC50s of 4.1 and 5.5 μM, respectively.
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NVP-HSP990 is a potent, selective and orally active Hsp90 inhibitor, with IC50 values of 0.6, 0.8, and 8.5 nM for Hsp90α, Hsp90β, and Grp94, respectively.
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SNX-2112 (PF 04928473) is an orally active Hsp90 inhibitor, with a Kd of 16 nM for Hsp90 and IC50s of 30 nM, 30 nM for Hsp90 α and Hsp90 β, also induces Her-2 degradation, and inhibits Grp94 and Trap-1, with IC50s of 10 nM, 4.275 μM and 0.862 μM, respectively . SNX-2112 (PF 04928473) binds Hsp90 isoforms Hsp90α, Hsp90β and Hsp90b1/Grp94 with Kds of 4 nM, 6 nM and 484 nM, respectively .
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PU-H54, a Grp94-selective inhibitor, can be used for the research of breast cancer. Hsp90 chaperone family, comprised in humans of four paralogs, Hsp90α, Hsp90β, Grp94 and Trap-1, has important roles in malignancy . PU-H54 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
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TRAP1-IN-1 (compound 35) is a potent and selective inhibitor of TRAP1，a mitochondrial isoform of Hsp90. TRAP1-IN-1 has >250-fold TRAP1 selectivity over Grp94，and disrupts TRAP1 tetramer stability，induces TRAP1 client protein degradation. TRAP1-IN-1 also inhibits mitochondrial complex I of oxidative phosphorylation OXPHOS，disrupts the mitochondrial membrane potential，and enhances glycolysis metabolism .
Cat. No.: HY-162767
CAS No.: 2144469-30-5
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KUNG65 is a selective inhibitor of Grp94, with a target Kd of 540 nM and at least 73 fold selectivity vs. the other Hsp90 isoforms .
Cat. No.: HY-120800
CAS No.: 1887032-92-9
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KUNG29 is a potent and selective Grp94 inhibitor with a Kd of 0.2 μM. KUNG29 induces the degradation of integrin α2 in MDA-MB-231 cells .
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4-Br-Bnlm is a selective inhibitor of glucose-regulated protein 94 (Grp94) with an EC50 value of 0.96 µM. 4-Br-Bnlm reduces the levels of mutant myocilin proteins as well as wild-type myocilin misfold in cells. 4-Br-Bnlm promotes the clearance of toxic formsof myocilin and reduces myocilin toxicity .
Cat. No.: HY-180195
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Grp94-IN-3 (Compound 47) is a selective ATP competitive inhibitor of Grp94, with a Kd value of 76 nM. Grp94-IN-3 has a much lower affinity for Hsp90α, with a Kd value of 9.17 μM. Grp94-IN-3 induces the degradation of integrin α2 (Integrin α2) in MDA-MB-231 cells and reduces the intracellular accumulation of mutant cardiac proteins in human trabecular meshwork cells. Grp94-IN-3 can be used for the study of metastatic cancer and open-angle glaucoma .
Cat. No.: HY-124221
CAS No.: 1166398-85-1
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Radamide is an inhibitor of Grp94 with anti-migratory activity. Radamide is used to inhibit Grp94-related diseases such as glaucoma, cancer metastasis, and multiple myeloma. Radamide exhibits selective inhibitory activity by acting on the specific structure of Grp94. Radamide derivatives show better potency and selectivity in improved structure-activity relationship studies .
Cat. No.: HY-119732
CAS No.: 2134571-29-0
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KUNG94 is a selective Grp94/HSP90B inhibitor (IC50=8 nM). By inhibiting the chaperone function of Grp94, KUNG94 reduces the maturation and cell surface trafficking of its specific client proteins. KUNG94 can be used for studies on Grp94-related biological mechanisms, as well as diseases including cancer and primary open-angle glaucoma .
Cat. No.: HY-103063
CAS No.: 852030-37-6
Iso-PU-H54 is a purine-scaffold Grp94 inhibitor with an IC50 of 1.63 μM .
Cat. No.: HY-10214R
CAS No.: 908112-43-6
Synonyms: PF-04928473 (Standard)
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SNX-2112 (Standard) is the analytical standard of SNX-2112 (HY-10214). This product is intended for research and analytical applications. SNX-2112 (PF 04928473) is an orally active Hsp90 inhibitor, with a Kd of 16 nM for Hsp90 and IC50s of 30 nM, 30 nM for Hsp90 α and Hsp90 β, also induces Her-2 degradation, and inhibits Grp94 and Trap-1, with IC50s of 10 nM, 4.275 μM and 0.862 μM, respectively . SNX-2112 (PF 04928473) binds Hsp90 isoforms Hsp90α, Hsp90β and Hsp90b1/Grp94 with Kds of 4 nM, 6 nM and 484 nM, respectively .
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Protocols
Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!A suitable model is crucial in drug screening experiments. Organs can mimic the three-dimensional functional structure of internal organs, have similar spatial organization to corresponding organs, maintain some key characteristics, and reproduce some physiological functions. They are widely used for modeling and personalized drug screening physiological functions.2025-02-06
