NSC45586 sodium
Based on 1 publication(s) in Google Scholar
NSC45586 sodium is an inhibitor of PHLPP. NSC45586 sodium targets the PP2C phosphatase domains of PHLPP1 and PHLPP2, blocks the phosphatase activity of PHLPP, increases the expression level of FOXO1 in the nucleus, and reduces the protein expression of PHLPP1. NSC45586 sodium activates the AKT survival signaling pathway, enhances IGF-1-induced AKT activation, and inhibits the phosphorylation of AKT/ERK under basal conditions. NSC45586 sodium reduces staurosporine-induced neuronal death, preserves notochord cell morphology and KRT19 expression, inhibits cell apoptosis (apoptosis), improves the viability and proliferation of nucleus pulposus cells, upregulates the expression of ACAN/SOX9, and downregulates the expression of MMP13. NSC45586 sodium binds tightly to bovine serum albumin (bovine serum albumin), and exerts a more significant effect on nucleus pulposus in male individuals. NSC45586 sodium can be used in studies related to global cerebral ischemia and intervertebral disc degeneration.
For research use only. We do not sell to patients.
- Purity : 98.0%
- CAS No.: 6300-44-3
- Formula: C20H17N6NaO3
- Molecular Weight:412.38
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Storage:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Publications Citing Use of MedChemExpress (MCE) NSC45586 sodium
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Biological Activity
Description
IC50 & Target
PHLPP1/2, Akt[1]
In Vitro
NSC45586 (0-100 μM; 35 min) sodium activates basal AKT in primary rat cortical neurons and enhances IGF-1-induced AKT activation[1].
NSC45586 (0-250 μM; 24 h) sodium significantly reduces STS (HY-15141)-induced death of primary rat cortical neurons[1].
NSC45586 (200 μM; 24 h) sodium increases the number of viable cells in rat primary neuron/astrocyte co-cultures following exposure to STS[1].
NSC45586 (50 μM; 35 min) sodium significantly inhibits basal AKT and ERK phosphorylation in primary rat astrocytes[1].
NSC45586 (100 μM; 24 h) sodium reduces the expression of PHLPP1 protein in degenerative human nucleus pulposus (NP) cells, with a more significant effect in male cells[2].
NSC45586 (0-100 μM; 24 h) sodium exhibits cytocompatibility and significantly promotes the proliferation of degenerated male human nucleus pulposus cells[2].
NSC45586 (25-100 μM; 24 h) sodium promotes the formation of healthy nucleus pulposus cell phenotypes by upregulating the expression of KRT19, ACAN and SOX9 and downregulating the expression of MMP13 in degenerative human nucleus pulposus cells, and this effect is more pronounced in male cells[2].
NSC45586 (25-100 μM; 30 min) sodium upregulates the phosphorylation level of AKT and the expression of FOXO1 protein in degenerative human nucleus pulposus cells from male donors in a dose-dependent manner[2].
NSC45586 (100 μM; 24 h) sodium promotes a healthy nucleus pulposus cell phenotype in degenerative human nucleus pulposus cells from male donors by activating the FOXO1 signaling pathway[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
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Cell Line:degenerated human nucleus pulposus (NP) cells (Pfirrman grade 4-5, sex-stratified: female and male, passage 2-3)
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Concentration:100 μM
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Incubation Time:24 h
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Result:Significantly reduced PHLPP1 protein expression (but not PHLPP2) in human NP cells, with a more pronounced reduction observed in male cells.
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Cell Line:degenerated human nucleus pulposus (NP) cells (Pfirrman grade 4-5, sex-stratified: female and male, passage 2-3)
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Concentration:25, 50, and 100 μM
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Incubation Time:24 h
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Result:Demonstrated good cytocompatibility at concentrations up to 100 μM.
Significantly increased cell proliferation in male human NP cells at all tested concentrations.
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Cell Line:degenerated human nucleus pulposus (NP) cells (Pfirrman grade 4-5, sex-stratified: female and male, passage 2-3)
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Concentration:25, 50, and 100 μM
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Incubation Time:24 h
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Result:Significantly increased KRT19 gene expression in both female and male cells.
Significantly increased SOX9 gene expression in both female and male cells.
Significantly increased ACAN gene expression in male cells.
Significantly reduced MMP13 gene expression in male cells, with effects more pronounced in males overall.
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Cell Line:degenerated human nucleus pulposus (NP) cells (Pfirrman grade 4-5, sex-stratified: female and male, passage 2-3)
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Concentration:25, 50, and 100 μM
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Incubation Time:30 min
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Result:Increased AKT phosphorylation in male human NP cells in a dose-dependent manner.
Increased FOXO1 protein expression in male human NP cells in a dose-dependent manner.
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Cell Line:degenerated human nucleus pulposus (NP) cells (Pfirrman grade 4-5, sex-stratified: female and male, passage 2-3)
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Concentration:100 μM
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Incubation Time:24 h (following 1 h pre-incubation with 200 nM AS1842856 or 100 nM Wortmannin)
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Result:Reversed the beneficial effects on KRT19 and ACAN gene expression in male human NP cells when pre-treated with the FOXO1 inhibitor AS1842856.
Showed no significant effect on gene expression changes induced by NSC45586 when pre-treated with the PI3K/AKT inhibitor Wortmannin.
Chemical Information
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CAS No. 6300-44-3
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Appearance Solid
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Molecular Weight 412.38
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Formula C20H17N6NaO3
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Color Brown to black
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SMILES
O=C(O[Na])C1=CC(/N=N/C2=CC=C(/N=N/C3=CC(C)=C(N)C=C3N)C=C2)=CC=C1O
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Publications (1)
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Journal Impact Factor
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Most Recent
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Int Dent J
Calpain-1 Potentiates Periodontal Regeneration via PHLPP1-ERK-Driven Osteogenesis in Periodontal Ligament Stem Cells. [Abstract]2025 Dec 6;76(1):109309. PMID: 41353895
Solvent & Solubility
In Vitro:
H2O : 5 mg/mL (12.12 mM; ultrasonic and warming and heat to 80°C)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Protocols
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Kinase activity and phosphorylation assays
Kinase activity assays measure the ability of kinases to transfer phosphate groups from ATP to specific substrates, while phosphorylation assays detect the presence and levels of phosphorylated proteins. Common methods include radiolabeled ATP incorporation (e. g. ,), ADP release detection via bioluminescence (e. g. ,[3]), enzyme-linked immunosorbent assays (ELISA) for phospho-specific epitopes (e. g. ,[6]), and microtiter-based formats for high-throughput screening (e. g. ,[8]). The ADP-Glo assay quantifies kinase activity by measuring ADP produced during phosphorylation using a luciferase-based system. Radiometric assays involve autoradiography or scintillation counting after incorporation of 32P-labeled ATP into substrate proteins. ELISA-based approaches rely on phospho-specific antibodies to detect activated kinases in cell lysates or purified samples.
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RNA extraction experimental
By lysing cells, releasing RNA, and removing impurities such as proteins and DNA, high-purity RNA products are finally obtained. The commonly used traditional method is the guanidine isothiocyanate/phenol/chloroform method (Trizol), which is suitable for a variety of animal materials including animal tissues, microorganisms, cultured cells, etc., and most plant materials.
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Western Blot
Western blotting (WB) is a commonly used experimental method in molecular biology, biochemistry, and immunogenetics for identifying and quantifying target proteins. It combines gel electrophoresis with immunoassay, enabling researchers to analyze protein expression, post-translational modifications, and molecular weight.
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Apoptosis
Apoptosis, also called programmed cell death, is generally characterized by distinct morphological characteristics.
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TUNEL staining for apoptotic DNA fragmentation
TUNEL staining detects DNA strand breaks by using terminal deoxynucleotidyl transferase to add labeled nucleotides to exposed 3′-OH DNA termini, generating either microscopic staining in fixed cells or tissue sections, or fluorescence/cytometric signal in cell suspensions. TUNEL positivity reflects DNA fragmentation but should not be interpreted alone as definitive apoptosis, because TUNEL can also label necrotic, autolytic, mechanically damaged, or DNA-repair-associated DNA breaks.
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Annexin V plus membrane-impermeant dye apoptosis staining
Annexin V-based apoptosis assays rely on the detection of phosphatidylserine (PS) externalization from the inner leaflet of the plasma membrane to the outer leaflet, an early biochemical hallmark of apoptosis. Fluorescently labeled Annexin V binds PS in a calcium-dependent manner, enabling identification of early apoptotic cells by flow cytometry or fluorescence microscopy. When combined with a membrane-impermeant DNA-binding dye (e. g. , propidium iodide), this approach allows discrimination between viable (Annexin V−/dye−), early apoptotic (Annexin V+/dye−), and late apoptotic or necrotic (Annexin V+/dye+) cell populations by assessing membrane integrity and PS exposure.
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Apoptosis Solutions
Apoptosis is a regulated, generally non-lytic cell-death pathway that removes unwanted, damaged, infected, or abnormal cells through coordinated morphological changes, caspase activation, DNA fragmentation, and membrane remodeling. The intrinsic apoptosis pathway is controlled mainly by mitochondrial outer membrane permeabilization, BCL-2 family proteins, cytochrome c release, apoptosome formation, caspase-9 activation, and downstream executioner caspase-3/7 activation. The extrinsic apoptosis pathway is initiated by death receptors such as Fas, TNFR, and TRAIL receptors, which recruit adaptor proteins and activate caspase-8 before engaging executioner caspases or mitochondrial amplification through BID cleavage. Apoptosis is linked to many phenotypes, including cancer cell killing, tissue homeostasis, immune regulation, neurodegeneration, infection response, and treatment-induced cytotoxicity; unresolved questions include how apoptosis interacts with necroptosis, pyroptosis, ferroptos
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Protocol for Kinase activity and phosphorylation assays
Kinase activity assays measure transfer of phosphate from ATP to a protein or peptide substrate, generating phosphorylated substrate, ADP, or incorporated radiolabeled phosphate as the readout; phosphorylation assays measure site-specific phosphorylation in cells or tissues as a proxy for kinase-pathway activation, inhibition, or substrate regulation. Phosphorylation can be detected by phospho-specific Western blot, immunoprecipitation kinase assay, phospho-immunofluorescence, phospho-flow cytometry, luminescent ADP detection, radiolabeled ATP incorporation, or reporter-based pathway assays, and these readouts can be applied to cancer cells, primary neurons, mouse tumors, organoids, inflammatory macrophages, ferroptosis studies, and mitophagy studies when the kinase target is biologically relevant.
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Protocol For Protein Expression And Purification
Recombinant protein expression in Escherichia coli followed by purification of a His-tagged soluble protein by immobilized metal affinity chromatography (IMAC), with optional MBP fusion and TEV tag removal when the construct includes these elements. The biological readout is production of the encoded target protein, detected as an inducible band at the expected molecular mass by SDS-PAGE and quantified by total protein assay or chromatographic absorbance; the purification readout is enrichment of the target protein in elution fractions after selective binding of polyhistidine residues to immobilized Ni2+/metal-chelate resin and elution by imidazole-containing buffer. Expression is driven by an inducible bacterial expression system, commonly T7/lac-based, in which IPTG or lactose/auto-induction activates transcription and translation of the cloned gene; lower induction temperature, lower inducer concentration, induction timing, and solubility-enhancing fusion tags can influence the frac
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Cell Viability Determination by MTT Colorimetric Assay
The following protocol uses the MTT colorimetric assay as a classic literature-established method for assessing cell viability/metabolic activity in cultured mammalian cells. MTT[3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide] is reduced by metabolically active cells to a colored formazan product; the amount of formazan is quantified spectrophotometrically and provides an indirect measure of metabolically active viable cells. Importantly, MTT reduction reflects cellular oxidoreductase/metabolic activity rather than an absolute direct count of living cells, so changes in cellular metabolism can alter the signal independently of cell number.
Purity & Documentation
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Data Sheet (277 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Handling Instructions (2659 KB)
References
[1]. Jackson TC, et al. Pharmacological inhibition of pleckstrin homology domain leucine-rich repeat protein phosphatase is neuroprotective: differential effects on astrocytes. J Pharmacol Exp Ther. 2013;347(2):516-528. [Content Brief]
[2]. Zhang C, et al. Differential efficacy of two small molecule PHLPP inhibitors to promote nucleus Pulposus cell health. JOR Spine. 2023;7(1):e1306. Published 2023 Dec 4. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| H2O | 1 mM | 2.4249 mL | 12.1247 mL | 24.2495 mL | 60.6237 mL |
| 5 mM | 0.4850 mL | 2.4249 mL | 4.8499 mL | 12.1247 mL | |
| 10 mM | 0.2425 mL | 1.2125 mL | 2.4249 mL | 6.0624 mL |
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.