LB-100

Catalog No.S7537

LB-100 Chemical Structure

Molecular Weight(MW): 268.31

LB-100 is a water soluble protein phosphatase 2A (PP2A) inhibitor with IC50s of 0.85 μM and 3.87 μM in BxPc-3 and Panc-1 cells.

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1 Customer Review

  • LB-100 (a protein phosphatase-2A inhibitor) induces a significant increase for hypoxia-inducible factor (HIF)-1α and vascular endothelial growth factor (VEGF)-C expression by enhancing phosphatidylinositol 3-kinase (PI3K)p85/AKT/ mechanistic target of rapamycin (mTOR) signaling. Western blot analysis results for phosphorylated and total PI3Kp85/AKT/mTOR, HIF-1α, and VEGF-C with or without monocyte chemoattractant protein (MCP)-1 or LB-100 treatment. Bar graphs show quantitative results by densitometric analysis. n = 3 or more independent replications. ∗P < 0.05, ∗∗P < 0.01. Gapdh, glyceraldehyde-3-phosphate dehydrogenase; p, phosphorylated.

    Am J Pathol, 2017, 187(8):1736-1749. LB-100 purchased from Selleck.

Purity & Quality Control

Choose Selective phosphatase Inhibitors

Biological Activity

Description LB-100 is a water soluble protein phosphatase 2A (PP2A) inhibitor with IC50s of 0.85 μM and 3.87 μM in BxPc-3 and Panc-1 cells.
Targets
PP2A [1]
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]

In vivo In a mouse pancreatic cancer xenograft model, LB-100 (2 mg/kg, i.p.) enhances chemotherapy of doxorubicin. LB-100 causes higher density of microvessel in tumors and rapid blood flow at the surface of tumors. [1]

Protocol

Kinase Assay:

[1]

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PP2A activity assays:

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.
Cell Research:

[1]

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  • Cell lines: BxPc-3, and Panc-1 cell lines
  • Concentrations: ~ 10 μM
  • Incubation Time: 48 h
  • Method:

    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.


    (Only for Reference)
Animal Research:

[1]

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  • Animal Models: BALB/c nude mice bearing Panc-1 xenograft
  • Formulation: Phosphate buffered saline
  • Dosages: 2 mg/kg
  • Administration: i.p.
    (Only for Reference)

Solubility (25°C)

In vitro Water 53 mg/mL (197.53 mM)
DMSO Insoluble
Ethanol Insoluble

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 268.31
Formula

C13H20N2O4

CAS No. 1026680-07-8
Storage powder
in solvent
Synonyms N/A

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT03027388 Not yet recruiting Astrocytoma, Grade IV|Glioblastoma Multiforme|Giant Cell Glioblastoma National Cancer Institute (NCI)|National Institutes of Health Clinical Center (CC) January 5, 2017 Early Phase 1
NCT01837667 Completed Tumors|Neoplasms|Cancer Lixte Biotechnology Holdings, Inc. February 2013 Phase 1

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

Tel: +1-832-582-8158 Ext:3

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID