2. Cell Cycle/DNA Damage Metabolic Enzyme/Protease Autophagy Apoptosis
  3. HSP Autophagy Apoptosis
  4. Luminespib

Luminespib  (Synonyms: VER-52296; AUY922; NVP-AUY922)

Cat. No.: HY-10215 Purity: 99.74%
COA Handling Instructions

Luminespib (VER-52296) est un inhibiteur puissant de HSP90 avec des IC50s de 7,8 et 21 nM pour HSP90α et HSP90β, respectivement.

Luminespib (VER-52296) 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.

Luminespib Chemical Structure

Luminespib Chemical Structure

CAS No. : 747412-49-3

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10 mM * 1 mL in DMSO
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10 mg USD 92 In-stock
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Customer Review

Based on 18 publication(s) in Google Scholar

Luminespib Related Antibodies

Top Publications Citing Use of Products

    Luminespib 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.

    Luminespib 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).

    Luminespib 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).

    View All HSP Isoform Specific Products:

    View All Isoforms
    HSP40 HSP70 HSP90 HSP105 HSF1 HSP HSPA5

    • Biological Activity

    • Protocol

    • Purity & Documentation

    • References

    • Customer Review

    Description

    Luminespib (VER-52296) is a potent HSP90 inhibitor with IC50s of 7.8 and 21 nM for HSP90α and HSP90β, respectively[1].

    IC50 & Target

    HSP90α

    7.8 nM (IC50)

    HSP90β

    21 nM (IC50)

    GRP94

    535 nM (IC50)

    TRAP-1

    85 nM (IC50)

    In Vitro

    Luminespib 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. Luminespib 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. Luminespib 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) significantly reduces CD40L fibroblast-induced changes in immunophenotype and STAT3 signaling but with no effect on the viability of chronic lymphocytic leukemia (CLL) cells. Luminespib (500 nM) in combination with NSC 118218 more effectively induces apoptosis in cells in co-culture than either drug alone, and overcomes fibroblast-derived resistance to Hsp90 inhibitor[2]. Luminespib shows great inhibition of pancreatic cancer cells with IC50 of at 10 nM. Luminespib (10 nM) 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. Luminespib (10 nM) 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.

    Luminespib Related Antibodies
    In Vivo

    Luminespib (50, 75 mg/kg, i.p.) significantly inhibits tumor growth rate, reducing the mean weights of tumors on day 11 in human tumor xenografts[2]. Luminespib (50 mg/kg/week, 3×25 mg/kg/week) significantly reduces tumor growth rates and lowers tumor weights in the L3.6pl pancreatic cancer cell-bearing mice model[3].

    MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
    Clinical Trial
    Molecular Weight

    465.54

    Appearance

    Solid

    Formula

    C26H31N3O5
    CAS No.
    SMILES

    O=C(C1=NOC(C2=CC(C(C)C)=C(O)C=C2O)=C1C3=CC=C(CN4CCOCC4)C=C3)NCC
    Shipping

    Room temperature in continental US; may vary elsewhere.
    Storage
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 1 year
    -20°C 6 months
    Solvent & Solubility
    In Vitro: 

    DMSO : ≥ 62 mg/mL (133.18 mM)

    *"≥" means soluble, but saturation unknown.

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 2.1480 mL 10.7402 mL 21.4804 mL
    5 mM 0.4296 mL 2.1480 mL 4.2961 mL
    10 mM 0.2148 mL 1.0740 mL 2.1480 mL
    *Please refer to the solubility information to select the appropriate solvent.
    In Vivo:
    • 1.

      Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

      Solubility: ≥ 2.5 mg/mL (5.37 mM); Clear solution

    • 2.

      Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

      Solubility: ≥ 2.5 mg/mL (5.37 mM); Clear solution

    • 3.

      Add each solvent one by one:  10% DMSO    90% Corn Oil

      Solubility: ≥ 2.5 mg/mL (5.37 mM); Clear solution

    • 4.

      Add each solvent one by one:  5% DMSO    40% PEG300    5% Tween-80    50% Saline

      Solubility: ≥ 2.5 mg/mL (5.37 mM); Clear solution

    • 5.

      Add each solvent one by one:  5% DMSO    95% (20% SBE-β-CD in Saline)

      Solubility: ≥ 2.5 mg/mL (5.37 mM); Clear solution

    *All of the co-solvents are available by MedChemExpress (MCE).
    Purity & Documentation

    Purity: 99.81%

    COA (258 KB) HNMR (199 KB) LCMS (120 KB) Elemental Analysis Report (116 KB)

    Handling Instructions (2659 KB)
    References
    Cell Assay
    [1]

    Cell lines are grown in DMEM/10% FCS, 2 mM glutamine, and nonessential amino acids in a humidified atmosphere of 5% CO2 in air. All lines are free of Mycoplasma. Cell proliferation is determined using the SRB assay for tumor cells and prostate epithelial cells, the WST-1 assay for MCF10A and HB119, or an alkaline phosphatase assay for HUVEC and HDMEC. GI50 is the compound concentration inhibiting cell proliferation by 50% compared with vehicle controls. Active caspase-3/7 is measured using a homogenous caspase assay kit[1].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    Animal Administration
    [1]

    Mice[1]
    For efficacy studies, human tumor xenografts are established s.c. in athymic mice. WM266.4 cells are also injected i.v. to generate experimental lung metastases and PC3LN3 prostate carcinoma cells are implanted into the prostates of male mice. Dosing by i.p. with Luminespib commences when tumors are well established. Tumor growth is monitored and at study end samples are harvested for analysis[1].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    References
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    Luminespib Related Classifications

    Help & FAQs
    • Do most proteins show cross-species activity?

      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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    Keywords:

    Luminespib747412-49-3VER-52296 AUY922 NVP-AUY922VER52296VER 52296AUY922AUY 922AUY-922HSPAutophagyApoptosisHeat shock proteinsInhibitorinhibitorinhibit

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