Luminespib mesylate
Based on 27 publication(s) in Google Scholar
Luminespib mesylate (VER-52296 mesylate) is a potent HSP90 inhibitor with IC50s of 7.8 and 21 nM for HSP90α and HSP90β, respectively.
For research use only. We do not sell to patients.
- CAS No.: 1051919-21-1
- Formula: C27H35N3O8S
- Molecular Weight:561.65
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
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Publications Citing Use of MedChemExpress (MCE) Luminespib mesylate
More- Blood. 2018 Jul 19;132(3):307-320. [Abstract]
- Nat Commun. 2026 Feb 12;17(1):1214. [Abstract]
- Nat Commun. 2017 Sep 4;8(1):422. [Abstract]
- J Biomed Sci. 2021 Jul 23;28(1):55. [Abstract]
- Pharmacol Res. 2020 Jan:151:104512. [Abstract]
- Cancer Lett. 2025 Feb 1:610:217354. [Abstract]
- Clin Cancer Res. 2018 Feb 15;24(4):794-806. [Abstract]
- NPJ Precis Oncol. 2025 Apr 25;9(1):122. [Abstract]
- Leukemia. 2019 Jun;33(6):1373-1386. [Abstract]
- Cell Rep. 2026 Jul 5;45(7).
- Cell Rep. 2025 Jun 30;44(7):115936. [Abstract]
- Cancer Cell Int. 2021 Jun 5;21(1):291. [Abstract]
- Eur J Med Chem. 2024 Nov 15:278:116801. [Abstract]
- Biochem Pharmacol. 2026 May:247:117785. [Abstract]
- J Chem Theory Comput. 2018 Jul 10;14(7):3859-3869. [Abstract]
- Int J Mol Sci. 2021 Jun 11;22(12):6309. [Abstract]
- Cancers (Basel). 2021 Feb 23;13(4):927. [Abstract]
- Bioengineering (Basel). 2025 Oct 19;12(10):1121. [Abstract]
- Nanomedicine. 2026 Jun:74:102957. [Abstract]
- J Biol Chem. 2024 Feb;300(2):105633. [Abstract]
- Viruses. 2021 Apr 2;13(4):610. [Abstract]
- SLAS Discov. 2020 Feb;25(2):195-206. [Abstract]
- Am J Cancer Res. 2024 May 15;14(5):2072-2087. [Abstract]
- Stem Cell Res. 2014 Sep;13(2):284-99. [Abstract]
- SSRN. 2025 Feb 7.
- bioRxiv. 2024 Jul 25.
- Cold Spring Harb Mol Case Stud. 2020 Jun 12;6(3):a004853. [Abstract]
Customer Validation & Images
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Cell Proliferation/Viability Assay
Biological Activity
Description
IC50 & Target
[1]|
HSP90α 7.8 nM (IC50) |
HSP90β 21 nM (IC50) |
GRP94 535 nM (IC50) |
TRAP-1 85 nM (IC50) |
In Vitro
Luminespib mesylate (VER-52296 mesylate) is a potent and selective HSP90 inhibitor, with IC50s and Kis of 21 ± 16, 8.2 ± 0.7 nM against HSP90β and of 7.8 ± 1.8, 9.0 ± 5.0 nM for HSP90α[1]. Luminespib mesylate shows weak activity against GRP94 and TRAP-1 wich IC50s of 535 ± 51 nM (Ki, 108 nM) and 85 ± 8 nM (Ki, 53 nM), respectively[1].Luminespib mesylate exhibits inhibitory effect on proliferation of various human tumor cell lines (2.3-49.6 nM), induces cell cycle arrest and apoptosis and depletes client proteins in human cancer cells (80 nM)[1]. Luminespib (100 nM) mesylate significantly reduces CD40L fibroblast-induced changes in immunophenotype and STAT3 signaling but with no effect on the viability of chronic lymphocytic leukemia (CLL) cells[2].Luminespib (500 nM) mesylate in combination with NSC 118218 (Fludarabine) (HY-B0069) more effectively induces apoptosis in cells in co-culture than either drug alone, and overcomes fibroblast-derived resistance to Hsp90 inhibitor[2].Luminespib mesylate shows great inhibition of pancreatic cancer cells with IC50 of at 10 nM[3].Luminespib (10 nM) mesylate reduces the expression and the epidermal growth factor (EGF)-mediated activation of EGFR and substantially disrupts EGF signaling in terms of diminishing downstream phosphorylation of ERKThr202/Tyr204[3].Luminespib (10 nM) mesylate significantly blocks pancreatic cancer cell migration and invasion both in the absence and presence of EGF[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 1051919-21-1
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Molecular Weight 561.65
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Formula C27H35N3O8S
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SMILES
O=C(C1=NOC(C2=C(O)C=C(O)C(C(C)C)=C2)=C1C3=CC=C(CN4CCOCC4)C=C3)NCC.O=S(O)(C)=O
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Synonyms
VER-52296 mesylate; AUY922 mesylate; NVP-AUY922 mesylate
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Publications (27)
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Journal Impact Factor
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Most Recent
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Blood
Targeting HSP90 dimerization via the C terminus is effective in imatinib-resistant CML and lacks the heat shock response. [Abstract]2018 Jul 19;132(3):307-320. PMID: 29724897
Luminespib mesylate purchased from MedChemExpress. Usage Cited in: Blood. 2018 Jul 19;132(3):307-320. [Abstract]
K562, KCL22 and HL60 are treated with the indicated (cytotoxic) concentration of Amidopyrine (AX) and AUY922 for 48h and later protein lysates are subjected to immunoblot analysis.
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Nat Commun
Human iPSC-based Modeling of Pulmonary Fibrosis Reveals p300/CBP Inhibition Suppresses Alveolar Transitional Cell State. [Abstract]2026 Feb 12;17(1):1214. PMID: 41680175 -
Nat Commun
2017 Sep 4;8(1):422. PMID: 28871086 -
J Biomed Sci
2021 Jul 23;28(1):55. PMID: 34301262 -
Pharmacol Res
Destabilization of ROR1 enhances activity of Ibrutinib against chronic lymphocytic leukemia in vivo. [Abstract]2020 Jan:151:104512. PMID: 31726100 -
Cancer Lett
HSP90 inhibitor AUY922 suppresses tumor growth and modulates immune response through YAP1-TEAD pathway inhibition in gastric cancer. [Abstract]2025 Feb 1:610:217354. PMID: 39603381 -
Clin Cancer Res
Colorectal Cancer Consensus Molecular Subtypes Translated to Preclinical Models Uncover Potentially Targetable Cancer Cell Dependencies. [Abstract]2018 Feb 15;24(4):794-806. PMID: 29242316
Luminespib mesylate purchased from MedChemExpress. Usage Cited in: Clin Cancer Res. 2018 Feb 15;24(4):794-806. [Abstract]
HSP90 inhibition with Luminespib or Ganetespib treatment at 50 and 100 nM for 24 hours in three CMS4 cell lines with response to HSP90 inhibition (CACO2, LIM2099 and SW480) confirmed up-regulation of HSP70 and HSP40 at the protein level in treated versus untreated control cells (western blotting).
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NPJ Precis Oncol
Functional screening identifies kinesin spindle protein inhibitor filanesib as a potential treatment option for hepatoblastoma. [Abstract]2025 Apr 25;9(1):122. PMID: 40281281 -
Leukemia
Targeting nuclear β-catenin as therapy for post-myeloproliferative neoplasm secondary AML. [Abstract]2019 Jun;33(6):1373-1386. PMID: 30575820 -
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Cell Rep
Gut microbiota-bile acid crosstalk contributes to calcium oxalate nephropathy through Hsp90α-mediated ferroptosis. [Abstract]2025 Jun 30;44(7):115936. PMID: 40591459 -
Cancer Cell Int
Construction of a prognostic model with histone modification-related genes and identification of potential drugs in pancreatic cancer. [Abstract]2021 Jun 5;21(1):291. PMID: 34090418 -
Eur J Med Chem
HSP90/LSD1 dual inhibitors against prostate cancer as well as patient-derived colorectal organoids. [Abstract]2024 Nov 15:278:116801. PMID: 39241481 -
Biochem Pharmacol
2026 May:247:117785. PMID: 41679664 -
J Chem Theory Comput
Estimation of Drug-Target Residence Times by τ-Random Acceleration Molecular Dynamics Simulations. [Abstract]2018 Jul 10;14(7):3859-3869. PMID: 29768913 -
Int J Mol Sci
Effects of a Unique Combination of the Whole-Body Low Dose Radiotherapy with Inactivation of Two Immune Checkpoints and/or a Heat Shock Protein on the Transplantable Lung Cancer in Mice. [Abstract]2021 Jun 11;22(12):6309. PMID: 34208396 -
Cancers (Basel)
2021 Feb 23;13(4):927. PMID: 33672199 -
Bioengineering (Basel)
Precision Oncology for High-Grade Gliomas: A Tumor Organoid Model for Adjuvant Treatment Selection. [Abstract]2025 Oct 19;12(10):1121. PMID: 41155119 -
Nanomedicine
Nanotechnology-based reformulation of AUY922 mitigates retinal toxicity and retains potent anti-tumor activity. [Abstract]2026 Jun:74:102957. PMID: 42134612 -
J Biol Chem
Functional Maturation of Cytochromes P4503A4 and 2D6 Relies on GAPDH- and Hsp90-Dependent Heme Allocation. [Abstract]2024 Feb;300(2):105633. PMID: 38199567 -
Viruses
Deep Transfer Learning Approach for Automatic Recognition of Drug Toxicity and Inhibition of SARS-CoV-2. [Abstract]2021 Apr 2;13(4):610. PMID: 33918368 -
SLAS Discov
Medium-Throughput Detection of Hsp90/Cdc37 Protein-Protein Interaction Inhibitors Using a Split Renilla Luciferase-Based Assay. [Abstract]2020 Feb;25(2):195-206. PMID: 31662027 -
Am J Cancer Res
The small-molecule drug homoharringtonine targets HSF1 to suppress pancreatic cancer progression. [Abstract]2024 May 15;14(5):2072-2087. PMID: 38859866 -
Stem Cell Res
2014 Sep;13(2):284-99. PMID: 25171775
Luminespib mesylate purchased from MedChemExpress. Usage Cited in: Stem Cell Res. 2014 Sep;13(2):284-99. [Abstract]
HSP90 inhibition affects ciliation. 24 h treatment with 100 nM AUY922 significantly affects ciliation, under 20% (left) O2 tension but not 5% O2 tension (right).
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Cold Spring Harb Mol Case Stud
2020 Jun 12;6(3):a004853. PMID: 32532875
Purity & Documentation
References
[1]. Eccles, Suzanne A., et al. NVP-AUY922: A Novel Heat Shock Protein 90 Inhibitor Active against Xenograft Tumor Growth, Angiogenesis, and Metastasis. Cancer Research (2008), 68(8), 2850-2860. [Content Brief]
[2]. Best OG, et al. Heat shock protein-90 inhibitor, NVP-AUY922, is effective in combination with NSC 118218 against chronic lymphocytic leukemia cells cultured on CD40L-stromal layer and inhibits their activated/proliferative phenotype. Leuk Lymphoma. 2012 Jul 9. [Content Brief]
[3]. Moser C, et al. Stoeltzing O.Targeting HSP90 by the novel inhibitor NVP-AUY922 reduces growth and angiogenesis of pancreatic cancer. Anticancer Res. 2012 Jul;32(7):2551-61. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Luminespib mesylate Related Classifications
HY-10215A Related Classifications
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