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25mg |
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Purity: ≥98%
LB-100 (LB100) is a water soluble small-molecular protein phosphatase 2A (PP2A) inhibitor with anticancer activity. It inhibits PP2A with IC50 of 0.85 μM and 3.87 μM in BxPc-3 and Panc-1 cells. By using CCK-8 assays, LB-100 showed dose-dependent inhibition of cell growth in both cell lines. The IC50 of LB-100 was 0.85 μM and 3.87 μM in BxPc-3 and Panc-1, respectively. While the IC50 of doxorubicin was 2.3 μM and 1.7 μM in BxPc-3 and Panc-1, respectively, LB-100 did not synergize with doxorubicin in both cell lines. LB-100 treatment reduced PP2A activity by 30–50% in different pancreatic cell lines. LB-100 treatment increased the relative concentration of doxorubicin by up to 2.5 fold compared to cells not exposed to LB-100. LB-100 significantly enhanced inhibition of HCC by doxorubicin and cisplatin in vitro and in vivo in a PP2A-dependent way, while having little inhibitory activity when used alone.
ln Vitro |
With IC50 values of 2.3 μM (BxPc-3) and 1.7 μM (Panc-1), LB-100 suppresses cell proliferation. In BxPc-3, Panc-1, and SW1990 cells, LB-100 exhibited a 30-50% reduction in PP2A activity. LB-100 sensitizes tumor cells to the cytotoxicity of doxorubicin and raises its intracellular concentration (to 2.5 times the control). LB-100 promotes HIF-1α-VEGF-mediated angiogenesis by increasing VEGF production [1]. The integrity of ve-cadherin in endothelial cells is changed by LB-100. The amount of dye that passed through the HUVECs monolayer increased by nearly 40% after pretreatment with LB-100. The quantity of doxorubicin in tumor cells may be increased by LB-100 because it causes an increase in the paracellular permeability of vascular endothelial cells [2]. Sorafenib-induced HCC cell death is enhanced by LB-100, which also downregulates Bcl-2 expression [3].
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ln Vivo |
In nude mouse xenografts and livers, LB-100 (2 mg/kg, i.p.) decreases PP2A activity in a time-dependent way. The expression of the three PP2A subunits (PP2A_A, PP2A_B, and PP2A_C) in cell lines, xenografts, and liver is not changed by LB-100, as demonstrated by immunoblotting. While a single drug treatment had little effect on the animals, the combined use of doxorubicin (1.5 kg/mL, every other day) and LB-100 (2 mg/kg, every other day) can dramatically slow down the tumor growth and lower the tumor volume in both animals. Growth of tumors has little impact [2].
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Animal Protocol |
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References |
[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.
[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. [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 |
Molecular Formula |
C13H20N2O4
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Molecular Weight |
268.31
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CAS # |
1632032-53-1
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SMILES |
O1[C@]2([H])C([H])([H])C([H])([H])[C@@]1([H])[C@@]([H])(C(N1C([H])([H])C([H])([H])N(C([H])([H])[H])C([H])([H])C1([H])[H])=O)[C@]2([H])C(=O)O[H]
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InChi Key |
JUQMLSGOTNKJKI-UHFFFAOYSA-N
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InChi Code |
InChI=1S/C13H20N2O4/c1-14-4-6-15(7-5-14)12(16)10-8-2-3-9(19-8)11(10)13(17)18/h8-11H,2-7H2,1H3,(H,17,18)
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Chemical Name |
3-[(4-Methylpiperazin-1-yl)carbonyl]-7-oxabicyclo[2.2.1]heptane-2-carboxylic acid
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Synonyms |
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Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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Solubility (In Vitro) |
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Preparing Stock Solutions | 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 |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration: mg/mL;
Method for preparing DMSO stock solution: mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation::Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.