Home PI3K/Akt/mTOR PP2A inhibitor LB-100

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LB-100 PP2A inhibitor

Cat.No.S7537

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.
LB-100 PP2A inhibitor Chemical Structure

Chemical Structure

Molecular Weight: 268.31

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Quality Control

Batch: Purity: 99.91%
99.91

Cell Culture, Treatment & Working Concentration

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
U251 cells Function assay 2 μM 3 hours and 6 hours treatment with 2 μM LB100 reduced PP2A activity to 61% of control cells after both three and six hours of LB100 exposure. 25939762
D283 cells Cell viability assay IC50=0.9 μM, using XTT assays 26799670
DAOY cells Cell viability assay IC50=2.9 μM, using XTT assays 26799670
D341 cells Cell viability assay IC50=1.9 μM, using XTT assays 26799670
CH-157 cells Function assay 2.5 μM 3 hours LB-100 significantly enhanced the proportion of cells in G2/M. 29199006
SKOV-3 Cytotoxicity assay 72 h IC50 = 10.1 ± 1.8 μM 25376608
OVCAR-8 Cytotoxicity assay 72 h IC50 = 5.5 ± 0.5 μM 25376608
PEO-4 Cytotoxicity assay 72 h IC50 = 5 ± 0.6 μM 25376608
PEO-6 Cytotoxicity assay 72 h IC50 = 5.1 ± 0.2 μM 25376608
PEO1-Brca2 Missense Cytotoxicity assay 72 h IC50 = 6.2 ± 1.5 μM 25376608
PEO1-Brca2 STOP Cytotoxicity assay 72 h IC50 = 6.2 ± 1.0 μM 25376608
Huh-7 PP2A activity assays 5 μmol/L 2 h reduced the activity of PP2A to about 70% 24867249
HepG2 PP2A activity assays 5 μmol/L 2 h reduced the activity of PP2A to about 70% 24867249
HL-7702 PP2A activity assays 5 μmol/L 2 h reduced the activity of PP2A to about 70% 24867249
Click to View More Cell Line Experimental Data

Solubility

In vitro
Batch:

Water : 54 mg/mL

DMSO : Insoluble
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : Insoluble

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Dilution Calculator Molecular Weight Calculator

In vivo
Batch:

In vivo Formulation Calculator (Clear solution)

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Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
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Chemical Information, Storage & Stability

Molecular Weight 268.31 Formula

C13H20N2O4

 Storage (From the date of receipt)
CAS No. 1632032-53-1 Download SDF Storage of Stock Solutions

Synonyms N/A Smiles CN1CCN(CC1)C(=O)C2C3CCC(C2C(=O)O)O3

Mechanism of Action

Targets/IC50/Ki
PP2A
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, this compound reduces the PP2A activity by 30-50%. It increases concentration of doxorubicin within cells (2.5 fold to control) and sensitizes tumor cells to the cytotoxicity of doxorubicin. This chemical increaseds VEGF secretion, and thus enhances HIF-1α-VEGF mediated angiogenesis.
Kinase Assay
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.
In vivo
In a mouse pancreatic cancer xenograft model, LB-100 (2 mg/kg, i.p.) enhances chemotherapy of doxorubicin. This compound causes higher density of microvessel in tumors and rapid blood flow at the surface of tumors.
References

Applications

Methods Biomarkers Images PMID
Western blot Cyclin D1 / c-myc / mcl-1 / Hsp90
S7537-WB2
29199006
Growth inhibition assay Cell viability Cell division
S7537-viability2
29199006

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT06012734 Not yet recruiting
Metastatic Microsatellite-stable Colorectal Cancer
The Netherlands Cancer Institute
 December 2023 Phase 1
NCT03886662 Unknown status
Myelodysplastic Syndromes
Lixte Biotechnology Holdings Inc.
 April 2019 Phase 1|Phase 2
NCT03027388 Completed
Astrocytoma Grades II III and IV|Glioblastoma Multiforme|Giant Cell Glioblastoma|Glioma|Oligodendrogliomas
National Cancer Institute (NCI)|National Institutes of Health Clinical Center (CC)
 January 9 2019 Phase 2
NCT01837667 Completed
Tumors|Neoplasms|Cancer
Lixte Biotechnology Holdings Inc.
 February 2013 Phase 1

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