2. Metabolic Enzyme/Protease
  3. Phosphatase
  4. 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.

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CAS 番号 : 1632032-53-1

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in Water
ready for reconstitution
 USD 184 在庫あり
Solution
10 mM * 1 mL in Water USD 184 在庫あり
Solid
5 mg $168 在庫あり
10 mg $264 在庫あり
50 mg $450 在庫あり
100 mg $699 在庫あり
250 mg $1400 在庫あり
500 mg $2100 在庫あり
1 g $2950 在庫あり
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カスタマーレビュー

Based on 13 publication(s) in Google Scholar

Other Forms of LB-100:

LB-100 関連抗体

Top Publications Citing Use of Products

    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).

    LB-100 purchased from MedChemExpress. Usage Cited in: Int J Biol Macromol. 2022 Sep 1:216:906-915.

    LB-100 (2 and 4 μM; 2 h) led to an increase in the phosphorylation level of T201 in PC12 cells.

    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.

    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.

    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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    製品説明

    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)
    体外実験

    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.

    LB-100 関連抗体
    体内実験

    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.
    臨床実験
    分子量

    268.31

    分子式

    C13H20N2O4
    CAS 番号
    Appearance

    Solid

    Color

    White to off-white

    SMILES

    O=C(N(CC1)CCN1C)C2[C@@](CC3)([H])O[C@@]3([H])C2C(O)=O
    輸送条件

    Room temperature in continental US; may vary elsewhere.
    保管条件
    Powder -20°C 3 years
      4°C 2 years
    In solvent -80°C 6 months
      -20°C 1 month
    溶剤 & 溶解度
    体外: 

    H2O : ≥ 48 mg/mL (178.90 mM)

    *"≥" 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
    10 mM 0.3727 mL 1.8635 mL 3.7270 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.

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    純度とドキュメンテーション

    純度: 99.77%

    COA (252 KB) HNMR (340 KB) RP-HPLC (196 KB) MS (70 KB)

    取扱説明書 (2659 KB)
    参考文献
    キナーゼ実験
    [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) はこれらの方法の精度を確認していません。 こちらは参照専用です。
    細胞実験
    [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) はこれらの方法の精度を確認していません。 こちらは参照専用です。
    動物実験
    [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) はこれらの方法の精度を確認していません。 こちらは参照専用です。
    参考文献

    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
    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.

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    LB-100 Related Classifications

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    Keywords:

    LB-1001632032-53-1LB100LB 100PhosphataseInhibitorinhibitorinhibit

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