LB-100
Based on 15 publication(s) in Google Scholar
LB-100 is a protein phosphatase 2A (PP2A) inhibitor, with IC50 of 0.85 μM and 3.87 μM in BxPc-3 and Panc-1 cells.
Nos produits utilisent uniquement pour la recherche. Nous ne vendons pas aux patients.
- Pureté: 99.77%
- CAS No.: 1632032-53-1
- Formule: C13H20N2O4
- Masse moléculaire:268.31
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Stockage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Activité biologique
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Chemical Information
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Solvant et solubilité
- Protocole
- Pureté et documentation
- Références
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Help & FAQs
Publications Citing Use of MedChemExpress (MCE) LB-100
More- Nat Commun. 2026 May 29. [Abstract]
- Nat Commun. 2017 May 31:8:15580. [Abstract]
- J Biomed Sci. 2026 May 15;33(1):51. [Abstract]
- Environ Sci Technol. 2026 Mar 3;60(8):5979-5990. [Abstract]
- Int J Biol Macromol. 2022 Sep 1:216:906-915. [Abstract]
- Mol Cancer Ther. 2019 Mar;18(3):556-566. [Abstract]
- JCI Insight. 2021 May 10;6(9):e141426. [Abstract]
- Cell Mol Life Sci. 2024 Jul 8;81(1):292. [Abstract]
- PLoS Pathog. 2025 Dec 3;21(12):e1013731. [Abstract]
- Cancer Sci. 2025 Sep 3. [Abstract]
- Development. 2025 Jul 1;152(13):dev204532. [Abstract]
- Viruses. 2022 Jan 14;14(1):145. [Abstract]
- Biol Reprod. 2018 May 1;98(5):644-653. [Abstract]
- Clin Rheumatol. 2026 Mar;45(3):1709-1720. [Abstract]
- Elife. 2022 Jun 10;11:e78301. [Abstract]
Customer Validation & Images
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WB
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Gel Electrophoresis
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2D/3D Cell Culture and Differentiation
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Bio/Physico-chemical Assay
Activité biologique
Description
IC50 & Target
IC50: 0.85 μM (PP2 in BxPc-3 cell), 3.87 μM (PP2 in Panc-1 cell)
In Vitro
LB-100 inhibits the cell growth with IC50 of 2.3 μM (in BxPc-3) or 1.7 μM (in Panc-1 cell). In BxPc-3, Panc-1, and SW1990 cells, LB-100 reduces the PP2A activity by 30-50%. LB-100 increases concentration of doxorubicin within cells (2.5 fold to control) and sensitizes tumor cells to the cytotoxicity of doxorubicin. LB-100 increaseds VEGF secretion, and thus enhances HIF-1α-VEGF mediated angiogenesis[1]. LB-100 alters VE-cadherin integrity between endothelial cells. Pretreatment of LB-100 results in a nearly 40% increase in dye passing through the HUVECs monolayer. LB-100 induces higher paracellular permeability of vascular endothelial cells potentially accounting for LB-100 increasing the concentration of doxorubicin in tumor cells[2]. LB-100 downregulates Bcl-2 expression and enhances sorafenib-induced apoptosis in HCC cells[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.
Essai clinique
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 1632032-53-1
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Appearance Solid
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Masse moléculaire 268.31
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Formule C13H20N2O4
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Color White to off-white
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SMILES
O=C(N(CC1)CCN1C)C2[C@@](CC3)([H])O[C@@]3([H])C2C(O)=O
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (15)
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Journal Impact Factor
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Most Recent
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Nat Commun
Native long-read RNA sequencing of human monocytes reveals activation-induced alternative splicing toward functional isoforms. [Abstract]2026 May 29. PMID: 42215459 -
Nat Commun
Systematic discovery of mutation-specific synthetic lethals by mining pan-cancer human primary tumor data. [Abstract]2017 May 31:8:15580. PMID: 28561042 -
J Biomed Sci
SARS-CoV-2 membrane protein recruits PP2A to dephosphorylate the nucleocapsid and promote virion production. [Abstract]2026 May 15;33(1):51. PMID: 42141450 -
Environ Sci Technol
Environmental Dose MEOHP Promotes Bladder Cancer Progress through Hybrid EMT Mechanism: Based on the Adverse Outcome Pathway. [Abstract]2026 Mar 3;60(8):5979-5990. PMID: 41650175 -
Int J Biol Macromol
Synaptotagmin 1-mediated cell membrane penetration and dopamine release enhancement by latroeggtoxin-VI. [Abstract]2022 Sep 1:216:906-915. PMID: 35914553
LB-100 purchased from MedChemExpress. Usage Cited in: Int J Biol Macromol. 2022 Sep 1:216:906-915. [Abstract]
LB-100 (2 and 4 μM; 2 h) led to an increase in the phosphorylation level of T201 in PC12 cells.
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Mol Cancer Ther
The Antitumor Drug LB-100 Is a Catalytic Inhibitor of Protein Phosphatase 2A (PPP2CA) and 5 (PPP5C) Coordinating with the Active-Site Catalytic Metals in PPP5C. [Abstract]2019 Mar;18(3):556-566. PMID: 30679389
LB-100 purchased from MedChemExpress. Usage Cited in: Mol Cancer Ther. 2019 Mar;18(3):556-566. [Abstract]
Inhibition of PP2AC (circles) and PPP5C (triangles) activity by LB-100 (10-4-103 μM; 10 min) assayed using a phosphopeptide (K-R-pT-I-R-R) as a substrate. LB-100 inhibits the catalytic activity of both PP2AC and PPP5C in a dose dependent manner.
LB-100 purchased from MedChemExpress. Usage Cited in: Mol Cancer Ther. 2019 Mar;18(3):556-566. [Abstract]
Representative western blot comparing S6 phosphorylation in cell extracts generated from wild-type (WT) HEK-293 cells treated with LB-100 (0.2-2 μM; 3 h), and untreated HEK-293 cells in which the expression of PPP5C was disrupted (PPP5KO) using CRISPR-cas9 based methods. LB-100 induced phosphorylation of ribosomal protein S6 (Ser235/236) in the wild-type HEK-293 cells in a dose-dependent manner.
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JCI Insight
2021 May 10;6(9):e141426. PMID: 33986191
LB-100 purchased from MedChemExpress. Usage Cited in: JCI Insight. 2021 May 10;6(9):e141426. [Abstract]
Western blot of a Phos-tag gel showing the decrease in NPR2 phosphorylation in chondrocytes treated with FGF18 (0.5 μg/mL; 10 min). LB-100 (10 μM; 1 h) pretreatment attenuated this dephosphorylation in chondrocytes.
LB-100 purchased from MedChemExpress. Usage Cited in: JCI Insight. 2021 May 10;6(9):e141426. [Abstract]
LB-100(10 μM; 6 d) and BMN-111 (0.1 μM) acted synergistically to stimulate growth in fetal femurs from Fgfr3Y367C/+ mice. LB-100 alone also increased the extent of elongation and bone area.
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Cell Mol Life Sci
Nuclear translocation of ISG15 regulated by PPP2R2B inhibits cisplatin resistance of bladder cancer. [Abstract]2024 Jul 8;81(1):292. PMID: 38976080
LB-100 purchased from MedChemExpress. Usage Cited in: Cell Mol Life Sci. 2024 Jul 8;81(1):292. [Abstract]
Western blot analysis of pDNA PKcs (S2056) levels in T24 treated with PP2A-specific inhibitor LB-100 (0.5-8 μM/L). LB-100 significantly enhanced the level of pDNA PKcs (S2056).
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PLoS Pathog
2025 Dec 3;21(12):e1013731. PMID: 41337097 -
Cancer Sci
Synergistic Efficacy of Chidamide and LB100 in Sézary Syndrome via TNC Downregulation and PI3K/AKT/mTOR Dephosphorylation. [Abstract]2025 Sep 3. PMID: 40903394 -
Development
Distinct FGF-FGFR sets regulate inhibitory presynaptic differentiation from parvalbumin- and somatostatin-positive interneurons. [Abstract]2025 Jul 1;152(13):dev204532. PMID: 40554746 -
Viruses
HERV-W Envelope Triggers Abnormal Dopaminergic Neuron Process through DRD2/PP2A/AKT1/GSK3 for Schizophrenia Risk. [Abstract]2022 Jan 14;14(1):145. PMID: 35062349 -
Biol Reprod
Palmitic acid induces ceramide accumulation, mitochondrial protein hyperacetylation, and mitochondrial dysfunction in porcine oocytes. [Abstract]2018 May 1;98(5):644-653. PMID: 29385411
LB-100 purchased from MedChemExpress. Usage Cited in: Biol Reprod. 2018 May 1;98(5):644-653. [Abstract]
Comparison of SIRT3 expression of PA-treated oocytes cultured with or without 10 μM LB100.
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Clin Rheumatol
PP2A dysfunction mediated by PPP2R1A deficiency drives cGAS-STING-dependent hyperinflammation in SLE CD14+ monocytes. [Abstract]2026 Mar;45(3):1709-1720. PMID: 41582267 -
Elife
2022 Jun 10;11:e78301. PMID: 35686730
Solvant et solubilité
In Vitro:
H2O : ≥ 48 mg/mL (178.90 mM)
* "≥" means soluble, but saturation unknown.
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
* 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
* 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)
Protocole
Kinase Assay[1]
Cultured pancreatic cancer cells are treated with IC50 of LB-100 for each cell line or equal volume of vehicle for 2 hours, and PP2A activity assays are then performed using Ser/Thr phosphatase assay kit. Cells are lysed with an ultrasonic cell disruptor, and the PP2A concentration is measured using a Ser/Thr phosphatase assay kit according to the instructions. Assays for each cell line are performed in triplicate.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Cell Assay[1]
Cytotoxicity is conducted by using a Cell Counting Kit-8. Cells are seeded in 96-well plates with a density of 3000 cells per well and are assessed after treatments following the CCK-8 protocol. Relative cytotoxicity is expressed as a percentage of specific controls.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration[2]
BALB/c nude mice are injected subcutaneously in the right flank with 1×106 Huh-7 cells suspended in 200 μL PBS per mouse. After a tumor volume of 100 to 200 mm3 is reached, tumor-bearing mice are randomLy allocated to four groups: control group, doxorubicin/cisplatin group, LB-100 group, and doxorubicin/cisplatin plus LB-100 group. For the doxorubicin plus LB-100 study (n=6 to 8), doxorubicin and LB-100 are injected i.p. at 1.5 and 2 mg/kg, respectively, on alternate days for a total of 16 days. For the cisplatin plus LB-100 study (n=8 to 10), cisplatin and LB-100 are injected at 3 and 2.5 mg/kg, i.p., respectively; cisplatin is injected every 4 days and LB-100 is used every other day for 16 days. Control mice are injected with DMSO (in the doxorubicin plus LB-100 group) or PBS (in the cisplatin plus LB-100 group) on the same schedule as the drug-treated animals. Tumor size is monitored every 3 or 4 days, and is calculated by the formula: tumor volume=length × width × height/2. All mice are sacrificed at day 16, and xenografts are obtained, weighed, and fixed with 10% formaldehyde.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Pureté et documentation
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Fiche technique (282 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Instruction de manipulation (2659 KB)
Références
[1]. Bai X, et al. Inhibition of protein phosphatase 2A sensitizes pancreatic cancer to chemotherapy by increasing drug perfusion via HIF-1α-VEGF mediated angiogenesis. Cancer Lett. 2014 Oct 7. pii: S0304-3835(14)00589-8. [Content Brief]
[2]. Bai XL, et al. Inhibition of protein phosphatase 2A enhances cytotoxicity and accessibility of chemotherapeutic drugs to hepatocellular carcinomas. Mol Cancer Ther. 2014 Aug;13(8):2062-72. [Content Brief]
[3]. Fu QH, et al. LB-100 sensitizes hepatocellular carcinoma cells to the effects of sorafenib during hypoxia by activation of Smad3 phosphorylation. Tumour Biol. 2016 Jun;37(6):7277-8 [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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
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| H2O | 1 mM | 3.7270 mL | 18.6352 mL | 37.2703 mL | 93.1758 mL |
| 5 mM | 0.7454 mL | 3.7270 mL | 7.4541 mL | 18.6352 mL | |
| 10 mM | 0.3727 mL | 1.8635 mL | 3.7270 mL | 9.3176 mL | |
| 15 mM | 0.2485 mL | 1.2423 mL | 2.4847 mL | 6.2117 mL | |
| 20 mM | 0.1864 mL | 0.9318 mL | 1.8635 mL | 4.6588 mL | |
| 25 mM | 0.1491 mL | 0.7454 mL | 1.4908 mL | 3.7270 mL | |
| 30 mM | 0.1242 mL | 0.6212 mL | 1.2423 mL | 3.1059 mL | |
| 40 mM | 0.0932 mL | 0.4659 mL | 0.9318 mL | 2.3294 mL | |
| 50 mM | 0.0745 mL | 0.3727 mL | 0.7454 mL | 1.8635 mL | |
| 60 mM | 0.0621 mL | 0.3106 mL | 0.6212 mL | 1.5529 mL | |
| 80 mM | 0.0466 mL | 0.2329 mL | 0.4659 mL | 1.1647 mL | |
| 100 mM | 0.0373 mL | 0.1864 mL | 0.3727 mL | 0.9318 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.
LB-100 Related Classifications
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