Ispinesib mesylate
Based on 7 publication(s) in Google Scholar
Ispinesib (SB-715992) mesylate is a specific inhibitor of kinesin spindle protein (KSP), with a Ki app of 1.7 nM.
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- CAS No.: 514820-03-2
- Formule: C31H37ClN4O5S
- Masse moléculaire:613.17
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
- Protocole
- Pureté et documentation
- Références
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Publications Citing Use of MedChemExpress (MCE) Ispinesib mesylate
More- Redox Biol. 2019 Feb:21:101112. [Abstract]
- Cancer Lett. 2021 May 28:506:1-10. [Abstract]
- Cancers (Basel). 2024 Nov 5;16(22):3732. [Abstract]
- Gene. 2025 Apr 3:955:149458. [Abstract]
- Urol Oncol. 2023 May;41(5):253.e11-253.e20. [Abstract]
- Preprints. 2023 Sep 30.
- bioRxiv. 2023 Sep 12:2023.09.09.557001. [Abstract]
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Cell Proliferation/Viability Assay
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Flow Cytometry
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Flow Cytometry
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Flow Cytometry
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In Vivo Efficacy Study
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Activité biologique
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KSP 1.7 nM (Ki app) |
Ispinesib (150 nM) mesylate inhibits BT-474 and MDA-MB-468 cell lines, with GI50s of 45 and 19 nM, respectively[2].
Ispinesib (SB715992, 15 and 30 nM) mesylate suppresses the proliferation of PC-3 prostate cancer cell by 48.65% and 52.16%, and induces apoptosis of prostate cancer cell by 1094.88% and 1516.70%, respectively. Ispinesib mesylate up regulates genes responsible for apoptosis and cell cycle arrest, and down regulates genes responsible for cell proliferation and survival. The anti-proliferation and pro-apoptotic activities of Ispinesib mesylate can be enhanced by genistein[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 514820-03-2
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Masse moléculaire 613.17
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Formule C31H37ClN4O5S
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SMILES
O=C1N(CC2=CC=CC=C2)C([C@@H](C(C)C)N(CCCN)C(C3=CC=C(C)C=C3)=O)=NC4=CC(Cl)=CC=C14.OS(=O)(C)=O
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Synonyms
SB-715992 mesylate; CK-0238273 mesylate
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Publications (7)
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Journal Impact Factor
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Most Recent
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Redox Biol
Intracellular ion and protein nanoparticle-induced osmotic pressure modify astrocyte swelling and brain edema in response to glutamate stimuli. [Abstract]2019 Feb:21:101112. PMID: 30685709 -
Cancer Lett
2021 May 28:506:1-10. PMID: 33652084
Ispinesib mesylate purchased from MedChemExpress. Usage Cited in: Cancer Lett. 2021 May 28:506:1-10. [Abstract]
Ispinesib impaired cell cycle progression.Cell cycle distribution of MGM cells treated with 10 nM Filanesib (10 nM) or Ispinesib (10 nM) after 24, 48, and 72 h.
Ispinesib mesylate purchased from MedChemExpress. Usage Cited in: Cancer Lett. 2021 May 28:506:1-10. [Abstract]
Ispinesib (10 nM; 72 h) induced cell apoptosis. Filanesib or ispinesib treatment induced cell death by the accumulation of cells in early and late-stage apoptosis in all MGM cell lines measured by Annexin V (FITC)/PI staining (left). Numbers indicate the percentage of Annexin V-positive cells (right).
Ispinesib mesylate purchased from MedChemExpress. Usage Cited in: Cancer Lett. 2021 May 28:506:1-10. [Abstract]
NCH93 tumor-bearing mice were randomized into three groups after reaching a tumor size of 200 mm³. Treatment with vehicle (DMSO), filanesib (10 mg/kg body weight), or Ispinesib (5 mg/kg; i.p.) was initiated on day 0. Mice were treated once every three days on five occasions. KIF11i significantly inhibited NCH93 tumor growth in SCID mice.
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Cancers (Basel)
Targeting the EGFR and Spindle Assembly Checkpoint Pathways in Oral Cancer: A Plausible Alliance to Enhance Cell Death. [Abstract]2024 Nov 5;16(22):3732. PMID: 39594688
Ispinesib mesylate purchased from MedChemExpress. Usage Cited in: Cancers (Basel). 2024 Nov 5;16(22):3732. [Abstract]
Ispinesib (1.875-30 nM) + Cetuximab (15-240 nM) combinations potentiate cytotoxicity in SCC-25 cell lines. Cell viability (%) after 48 h of exposure to single or combination therapies was determined by MTT assay based on three independent experiments.
Ispinesib mesylate purchased from MedChemExpress. Usage Cited in: Cancers (Basel). 2024 Nov 5;16(22):3732. [Abstract]
Ispinesib (1.875 nM; 24 h) + Cetuximab (240 nM; 24 h) promoted increased cell death in SCC-25 oral cancer cells.
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Gene
2025 Apr 3:955:149458. PMID: 40187619 -
Urol Oncol
Identification of the KIF and MCM protein families as novel targets for combination therapy with CDK4/6 inhibitors in bladder cancer. [Abstract]2023 May;41(5):253.e11-253.e20. PMID: 36813612 -
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bioRxiv
Multiplexed single-cell lineage tracing of mitotic kinesin inhibitor resistance in glioblastoma. [Abstract]2023 Sep 12:2023.09.09.557001. PMID: 37745469
Protocole
Kinesin specificity analysis is carried out using a pyruvate kinase−lactate dehydrogenase detection system that couples the production of ADP to oxidation of NADH. Absorbance changes are monitored at 340 nm. Steady-state studies using nanomolar concentrations of KSP are performed using a sensitive fluorescence-based assay utilizing a pyruvate kinase, pyruvate oxidase, and horseradish peroxidase coupled detection system that couples the generation of ADP to oxidation of Amplex Red to fluorescent resorufin. Generation of resorufin is monitored by fluorescence (λexcitation = 520 nm and λemission= 580 nm). Steady-state biochemical experiments are performed in PEM25 buffer [25 mM Pipes-K+ (pH 6.8), 2 mM MgCl2, 1 mM EGTA] supplemented with 10 µM paclitaxel for experiments involving microtubules. The IC50 for steady-state inhibition is determined at 500 µM ATP, 5 µM MTs, and 1 nM KSP in PEM25 buffer. Ki app (apparent inhibitor dissociation constant) estimates of Ispinesib are extracted from the concentration-response curves, with explicit correction for enzyme concentration[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
PC-3 prostate cancer cells are seeded in 96 well plates at a density of 4 × 103 cells/well. PC-3 cells are incubated for 24 hours to allow attachment to the surface of each well of the tissue culture plate. Then, the cells are treated with varying concentration of reagents and incubated for 1 to 3 days. First, PC-3 cells are treated with 15 and 30 nM of Ispinesib, respectively. Second, PC-3 cells are subjected to combinational treatments with 7.5 or 10 nM of Ispinesib plus 30 μM of genistein. Finally, PC-3 cells are pre-treated with 30 μM of genistein for 24 hours followed by treatment with 15 nM of Ispinesib. Control cells are treated with 0.3 mM Na2CO3 (vehicle control). After treatment, PC3 cells are incubated at 37°C with MTT (0.5 mg/mL) for 2 hours and isopropyl alcohol at room temperature for 1 hour. The spectrophotometric absorbance of each sample is then determined by using ULTRA Multifunctional Micro Plate Reader at 595 nm[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Mice with a tumor volume of ∼250 mm3 receive a single dose of Ispinesib (10 mg/kg). Tumors are dissected, fixed in 10% buffered formalin, and embedded in paraffin, and 5-μm tissue sections are prepared. Antigen retrieval is done by boiling in 50 mM citrate buffer (pH 5.5), and sections are then incubated in 3% hydrogen peroxide, washed in PBS-0.1% Tween, and blocked in 10% goat serum. Phospho-histone H3 (PH3) antibody is detected using Alexa Fluor 488 secondary antibody. Images are taken with a microscope at ×10 magnification and captured using MetaMorph software to quantify PH3 expression by computing the area ratio of PH3-positive cells per total cells. Ki67/cleaved caspase-3 staining is done. Nonfluorescent images are taken on an Olympus BX41 microscope at ×20 magnification[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Pureté et documentation
Références
[1]. Lad L, et al. Mechanism of inhibition of human KSP by ispinesib. Biochemistry. 2008 Mar 18;47(11):3576-85. [Content Brief]
[2]. Purcell JW, et al. Activity of the kinesin spindle protein inhibitor ispinesib (SB-715992) in models of breast cancer. Clin Cancer Res. 2010 Jan 15;16(2):566-76. [Content Brief]
[3]. Davis DA, et al. Increased therapeutic potential of an experimental anti-mitotic inhibitor SB715992 by genistein in PC-3 human prostate cancer cell line. BMC Cancer. 2006 Jan 24;6:22. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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