LB-100

Catalog No.S7537 Batch:S753702

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Technical Data

Formula

C13H20N2O4
Molecular Weight 268.31 CAS No. 1632032-53-1
Solubility (25°C)* In vitro Water 54 mg/mL (201.25 mM)
DMSO Insoluble
Ethanol Insoluble
* <1 mg/ml means slightly soluble or 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.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

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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 (from reference)

Kinase Assay:

[1]
  • 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 Assay:

[1]
  • 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.
Animal Study:

[1]
  • Animal Models

    BALB/c nude mice bearing Panc-1 xenograft

  • Dosages

    2 mg/kg

  • Administration

    i.p.

Customer Product Validation

Data from [Data independently produced by , , Exp Mol Med, 2018, 50(7):83]

Data from [Data independently produced by , , Am J Pathol, 2017, 187(8):1736-1749]

Selleck's LB-100 has been cited by 43 publications

CUL4B mutations impair human cortical neurogenesis through PP2A-dependent inhibition of AKT and ERK [ Cell Death Dis, 2024, 15(2):121] PubMed: 38331954
Targeting PP2A-dependent autophagy enhances sensitivity to ruxolitinib in JAK2V617F myeloproliferative neoplasms [ Blood Cancer J, 2023, 13(1):106] PubMed: 37423955
VPA mediates bidirectional regulation of cell cycle progression through the PPP2R2A-Chk1 signaling axis in response to HU [ Cell Death Dis, 2023, 14(2):114] PubMed: 36781846
N-acetyltransferase 10 promotes cutaneous wound repair via the NF-κB-IL-6 axis [ Cell Death Discov, 2023, 9(1):324] PubMed: 37644005
The CIP2A-TOPBP1 complex safeguards chromosomal stability during mitosis [ Nat Commun, 2022, 13(1):4143] PubMed: 35842428
LCK-Mediated RIPK3 Activation Controls Double-Positive Thymocyte Proliferation and Restrains Thymic Lymphoma by Regulating the PP2A-ERK Axis [ Adv Sci (Weinh), 2022, e2204522] PubMed: 36161785
Targeting Ribonucleotide Reductase Induces Synthetic Lethality in PP2A-Deficient Uterine Serous Carcinoma [ Cancer Res, 2022, 82(4):721-733] PubMed: 34921012
A cannabidiol aminoquinone derivative activates the PP2A/B55α/HIF pathway and shows protective effects in a murine model of traumatic brain injury [ J Neuroinflammation, 2022, 19(1):177] PubMed: 35810304
PTEN/AKT signaling pathway related to hTERT downregulation and telomere shortening induced in Toxoplasma GRA16-expressing colorectal cancer cells [ Biomed Pharmacother, 2022, 153:113366] PubMed: 35810694
Cytoplasmic zinc promotes IL-1β production by monocytes and macrophages through mTORC1-induced glycolysis in rheumatoid arthritis [ Sci Signal, 2022, 15(716):eabi7400] PubMed: 35015571

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

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