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LB-100

Name: LB-100
Brand: Selleck Chemicals
SKU: S7537
Rating: 5 (51 reviews)

Catalog No.S7537 Purity:99.91%

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 Chemical Structure

CAS No. 1632032-53-1

Purity & Quality Control

Batch: Purity: 99.91%

99.91

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Cell Data

Cell Lines	Assay Type	Concentration	Incubation Time	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

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
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]
Kinase Assay	PP2A activity assays
Kinase Assay	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	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.
Experimental Result Images	Methods	Biomarkers	Images	PMID
	Western blot	Cyclin D1 / c-myc / mcl-1 / Hsp90		29199006
	Growth inhibition assay	Cell viability Cell division		29199006

In Vivo
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]
Animal Research	Animal Models	BALB/c nude mice bearing Panc-1 xenograft
	Dosages	2 mg/kg
	Administration	i.p.

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
Clinical Trial Information (data from https://clinicaltrials.gov, updated on 2024-05-22)
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

References

[1] Bai X, et al. Cancer Lett. 2014, 355(2), 281-287.

Chemical Information & Solubility

Molecular Weight	268.31	Formula	C₁₃H₂₀N₂O₄
CAS No.	1632032-53-1	SDF	Download LB-100 SDF
Smiles	CN1CCN(CC1)C(=O)C2C3CCC(C2C(=O)O)O3
Storage (From the date of receipt)	3 years-20°Cpowder	Storage of Stock Solutions Aliquot the stock solutions to avoid repeated freeze-thaw cycles	1 year-80°Cin solvent
Storage (From the date of receipt)	3 years-20°Cpowder		1 month-20°Cin solvent

In vitro
Batch:

Water : 54 mg/mL

DMSO : Insoluble ( Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : Insoluble

Molecular Weight Calculator

In vivo Batch: Add solvents to the product individually and in order.				In vivo Formulation Calculator
Clear solution	saline	54.000mg/ml (201.26mM)	Taking the 1 mL working solution as an example, add 54 mg of this product to 1 ml of physiological saline (0.9% NaCL solution), mix evenly to make it clear, The mixed solution should be used immediately for optimal results.
Clear solution	5% H2O 1 40% PEG 300 2 5% Tween 80 3 ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	5.000mg/ml (18.64mM)	Taking the 1 mL working solution as an example, add 50 μL of 100 mg/ml clarified H2O stock solution to 400 μL of PEG 300, mix evenly to clarify; add 50 μL of Tween 80 to the above system, mix evenly to clarify; Then continue to add 500 μL ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	saline	54.000mg/ml (201.26mM)	Taking the 1 mL working solution as an example, add 54 mg of this product to 1 ml of physiological saline (0.9% NaCL solution), mix evenly to make it clear, The mixed solution should be used immediately for optimal results.
Clear solution	saline	53.000mg/ml (197.53mM)	Taking the 1 mL working solution as an example, add 53 mg of this product to 1 ml of physiological saline (0.9% NaCL solution), mix evenly to make it clear, The mixed solution should be used immediately for optimal results.

Preparing Stock Solutions

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
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Dilution Calculator Molecular Weight Calculator

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg Average weight of animals: g Dosing volume per animal:μL Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

Calculation results:

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.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

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
If you have any other enquiries, please leave a message.

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