1. Metabolic Enzyme/Protease
  2. Phosphatase
  3. LB-100

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.

For research use only. We do not sell to patients.

LB-100 Chemical Structure

LB-100 Chemical Structure

CAS No. : 1632032-53-1

Size Price Stock Quantity
Solid + Solvent
10 mM * 1 mL in Water
ready for reconstitution
USD 185 In-stock
Solution
10 mM * 1 mL in Water USD 185 In-stock
Solid
5 mg USD 168 In-stock
10 mg USD 264 In-stock
50 mg USD 450 In-stock
100 mg USD 750 In-stock
200 mg   Get quote  
500 mg   Get quote  

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Customer Review

Based on 8 publication(s) in Google Scholar

Other Forms of LB-100:

Top Publications Citing Use of Products

    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.
    • Biological Activity

    • Protocol

    • Purity & Documentation

    • References

    • Customer Review

    Description

    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[1][2][3].

    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

    LB-100 (2 mg/kg, i.p.) decreases in a time-dependent manner the activity of PP2A in xenografts and livers in nude mice. LB-100 does not alter the expression of the three PP2A subunits (PP2A_A, PP2A_B, and PP2A_C) in cell lines, xenografts, or livers, as confirmed by immunoblotting. The combination of doxorubicin (1.5 kg/mL, every other day) and LB-100 (2 mg/kg, every other day) significantly slows the growth of tumors with reduction of tumor volume in two animals with no effects on tumor growth in animals treated with single agents[2].

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

    Molecular Weight

    268.31

    Formula

    C13H20N2O4

    CAS No.
    Appearance

    Solid

    Color

    White to off-white

    SMILES

    O=C(C1[C@@H](O2)CC[C@@H]2C1C(N3CCN(C)CC3)=O)O

    Shipping

    Room temperature in continental US; may vary elsewhere.

    Storage
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 2 years
    -20°C 1 year
    Solvent & Solubility
    In Vitro: 

    H2O : ≥ 48 mg/mL (178.90 mM)

    DMSO : 1 mg/mL (3.73 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    *"≥" means soluble, but saturation unknown.

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 3.7270 mL 18.6352 mL 37.2703 mL
    5 mM 0.7454 mL 3.7270 mL 7.4541 mL
    View the 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.

    * 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.

    • Molarity Calculator

    • Dilution Calculator

    Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    This equation is commonly abbreviated as: C1V1 = C2V2

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    In Vivo Dissolution Calculator
    Please enter the basic information of animal experiments:

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    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Calculation results:
    Working solution concentration: mg/mL
    This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
    The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only.If necessary, please contact MedChemExpress (MCE).
    Purity & Documentation

    Purity: ≥98.0%

    References
    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.

    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.

    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.

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

    References

    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
    DMSO / H2O 1 mM 3.7270 mL 18.6352 mL 37.2703 mL 93.1758 mL
    H2O 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.

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    • 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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