LB-100

Name: LB-100
Brand: Selleck Chemicals
SKU: S7537
Rating: 5 (15 reviews)

For research use only.

Catalog No.S7537

15 publications

CAS No. 1026680-07-8

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.

Selleck's LB-100 has been cited by 15 publications

J Cell Biol, 2020, 219(4)

PubMed: 32050025 ( click the link to review the publication )

Cancer Res, 2020, 10;canres.57.2020

PubMed: 32522823 ( click the link to review the publication )

PLoS One, 2020, 29;15(5):e0233863

PubMed: 32470053 ( click the link to review the publication )

Neurosci Lett, 2020, 721:134817

PubMed: 32032748 ( click the link to review the publication )

Biochem Biophys Res Commun, 2020, 526(1):1-7

PubMed: 32192773 ( click the link to review the publication )

Sci Rep, 2020, 10(1):10992

PubMed: 32620893 ( click the link to review the publication )

World J Gastroenterol, 2019, 25(45):6607-6618

PubMed: 31832001 ( click the link to review the publication )

Eur J Pharmacol, 2019, 852:99-106

PubMed: 30851273 ( click the link to review the publication )

Mol Cell, 2018, 71(1):11-24

PubMed: 29937341 ( click the link to review the publication )

Mol Cancer, 2018, 17(1):44

PubMed: 29455644 ( click the link to review the publication )

Exp Mol Med, 2018, 50(7):83

PubMed: 30050113 ( click the link to review the publication )

Anticancer Res, 2018, 38(10):5791-5798

PubMed: 30275201 ( click the link to review the publication )

Am J Pathol, 2017, 187(8):1736-1749

PubMed: 28627412 ( click the link to review the publication )

Mediators Inflamm, 2017, 2017:5706152

PubMed: 29056830 ( click the link to review the publication )

Oncotarget, 2017, 9(7):7312-7321

PubMed: 29484112 ( click the link to review the publication )

2 Customer Reviews

LB-100 induced HDAC2 S394 phosphorylation.

Exp Mol Med, 2018, 50(7):83. LB-100 purchased from Selleck.
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 PP2A 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]

Cell Data

Cell Lines	Assay Type	Concentration	Incubation Time	Activity Description	PMID
CH-157 cells	MmDxSpVv[3Srb36gZZN{[Xl?	MVeyMlUh\|ryP	NXzPem9zOyCqb4Xydy=>	MlnvUGIuOTByIIPp[45q\mmlYX70cJkh\W6qYX7j[YQhfGinIIDyc5BwenSrb36gc4Yh[2WubIOgbY4hTzJxTT6=	MVKyPVE6QTByNh?=
DAOY cells	MYXD[YxtKH[rYXLpcIl1gSCjc4PhfS=>			NGjvfFlKSzVyPUKuPUDPxE1uIIXzbY5oKFiWVDDhd5NigXN?	MYSyOlc6QTZ5MB?=
D341 cells	MlTOR4VtdCC4aXHibYxqfHliYYPzZZk>			M3Wyb2lEPTB;MT65JO69VSxidYPpcochYFSWIHHzd4F6ew>?	NWm3bGgzOjZ5OUm2O\|A>
D283 cells	MkDSR4VtdCC4aXHibYxqfHliYYPzZZk>			NUH3[5d3UUN3ME2wMlkh\|ryPLDD1d4lv\yC[VGSgZZN{[Xm\|	NWmwTHl4OjZ5OUm2O\|A>
U251 cells	MXHGeY5kfGmxbjDhd5NigQ>?	NXHKR2NUOiEQvF2=	M{\xdFMhcG:3coOgZY5lKDZiaH;1dpM>	MXP0doVifG2nboSge4l1cCB{IN88UUBNSjFyMDDy[YR2[2WmIGDQNmEh[WO2aY\peJkhfG9iNkGlJI9nKGOxboTyc4wh[2WubIOgZYZ1\XJiYn;0bEB1cHKnZTDhcoQhe2m6IHjveZJ{KG:oIFzCNVAxKGW6cH;zeZJmNg>?	MXiyOVk{QTd4Mh?=
SKOV-3	NHzWVIpEgXSxdH;4bYNqfHliYYPzZZk>		NFqyZZk4OiCq	MoXuTWM2OCB;IEGwMlEhyrFiMT64JO69VQ>?	MUmyOVM4PjZyOB?=
OVCAR-8	NEHpXmZEgXSxdH;4bYNqfHliYYPzZZk>		NVL6c4xzPzJiaB?=	NUnl[3pbUUN3MDC9JFUvPSEEsTCwMlUh\|ryP	MoLENlU{PzZ4MEi=
PEO-4	NF3NWYVEgXSxdH;4bYNqfHliYYPzZZk>		M1ey[lczKGh?	MYTJR\|UxKD1iNTFCtUAxNjZizszN	NXKwXlRHOjV\|N{[2NFg>
PEO-6	NF7jTXhEgXSxdH;4bYNqfHliYYPzZZk>		NUTiR\|F3PzJiaB?=	M4rQOWlEPTBiPTC1MlEhyrFiMD6yJO69VQ>?	Mmf4NlU{PzZ4MEi=
PEO1-Brca2 Missense	Mm\tR5l1d3SxeHnjbZR6KGG\|c3H5		Mki2O\|IhcA>?	MWTJR\|UxKD1iNj6yJOKyKDFwNTFOwG0>	NF7FWFczPTN5Nk[wPC=>
PEO1-Brca2 STOP	MUnDfZRwfG:6aXPpeJkh[XO\|YYm=		MWe3NkBp	Mn;XTWM2OCB;IE[uNkDDuSBzLkCg{txO	NYP6T\|E6OjV\|N{[2NFg>
Huh-7	NUK0[VBpWFB{QTDhZ5Rqfmm2eTDhd5NigXN?	MV61JO69dW:uL1y=	M3q1S\|IhcA>?	NX\ycXp6emWmdXPl[EB1cGViYXP0bZZqfHlib3[gVHAzSSC2bzDhZo92fCB5MDW=	NFPxdFAzPDh4N{K0PS=>
HepG2	NU\SVGcxWFB{QTDhZ5Rqfmm2eTDhd5NigXN?	NG[4XIM2KM7:bX;sM2w>	M3XkfFIhcA>?	M1rLU5Jm\HWlZXSgeIhmKGGldHn2bZR6KG:oIGDQNmEhfG9iYXLveZQhPzBn	MVeyOFg3PzJ2OR?=
HL-7702	M2LKRXBROkFiYXP0bZZqfHliYYPzZZl{	NF7rUoQ2KM7:bX;sM2w>	NV3JXpFrOiCq	NGS5cHdz\WS3Y3XkJJRp\SCjY4Tpeol1gSCxZjDQVFJCKHSxIHHic5V1KDdyJR?=	NHvnTHQzPDh4N{K0PS=>

... Click to View More Cell Line Experimental Data

Assay

Methods	Test Index	PMID
Western blot	p-AMPKα1 / AMPKα1 / p-ACC / ACC / p-p70S6K1 / p-4EBP1 ; PubMed: 29221169 Oncotarget HCT-116 cells were treated with LB-100 at 10 μM, cells were further cultured for the designated time. Expressions of listed proteins were tested by Western blotting assay. Cyclin D1 / c-myc / mcl-1 / Hsp90 ; PubMed: 29199006 Cancer Lett LB-100 down-regulates expression of STAT3 target genes. Western blot analysis of IOMM-LEE, GAR and CH-157 cells treated with increasing LB100 concentration demonstrates dose-dependent decrease in STAT3 target genes, including mcl-1, c-myc, and cyclin D.	29221169 29199006
Growth inhibition assay	Cell division ; PubMed: 29844427 Nat Commun In vitro proliferation of CD4+ T cells in the presence of LB-100 dose titration, measured by dilution of the cytosolic CFSE. Percentage of cells divided was plotted against concentration of LB-100. Cell viability ; PubMed: 29199006 Cancer Lett Three meningioma cell lines IOMM-LEE, GAR and CH-157 were used in vitro. XTT assays were performed after 48 hours of treatment. Increasing concentrations of LB-100 reduced cell viability, but cytotoxic effect was seen only at high drug concentration with 䲧疝Ỵ疞㧀	29844427 29199006

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]	- Collapse 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]	- Collapse 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]	- Collapse Animal Models: BALB/c nude mice bearing Panc-1 xenograft Dosages: 2 mg/kg Administration: i.p. (Only for Reference)

References

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

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 Download LB-100 SDF

Molecular Weight	268.31
Formula	C₁₃H₂₀N₂O₄
CAS No.	1026680-07-8
Storage	3 years-20°C powder 2 years-80°C in solvent
Synonyms	N/A
Smiles	CN1CCN(CC1)C(=O)C2C3CCC(C2C(=O)O)O3

In vivo Formulation Calculator (Clear solution)

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

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Step 2: Enter the in vivo formulation (Different batches have different solubility ratios, please contact Selleck to provide you with the correct ratio)

% DMSO+ % + % Tween 80+ % ddH₂O

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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 DMSO master liquid, next addμL PEG300， mix and clarify, next addμL Tween 80，mix and clarify, next add μL ddH₂O，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.

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Molarity Calculator

Calculate the mass, volume or concentration required for a solution. The Selleck molarity calculator is based on the following equation:

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Dilution Calculator

Calculate the dilution required to prepare a stock solution. The Selleck dilution calculator is based on the following equation:

Concentration _(start) x Volume _(start) = Concentration _(final) x Volume _(final)

This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )

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The Serial Dilution Calculator Equation

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Computed Result

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Molecular Weight Calculator

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Tip: Chemical formula is case sensitive. C10H16N2O2 c10h16n2o2

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Molarity Calculator

Clinical Trial Information (data from https://clinicaltrials.gov, updated on 2020-09-01)

NCT Number	Recruitment	interventions	Conditions	Sponsor/Collaborators	Start Date	Phases
NCT03027388	Recruiting	Drug: LB-100	Astrocytoma Grades II III and IV\|Glioblastoma Multiforme\|Giant Cell Glioblastoma\|Glioma\|Oligodendrogliomas	National Cancer Institute (NCI)\|National Institutes of Health Clinical Center (CC)	May 9 2019	Phase 2
NCT03886662	Recruiting	Drug: LB-100	Myelodysplastic Syndromes	Lixte Biotechnology Holdings Inc.	April 2019	Phase 1\|Phase 2
NCT01837667	Completed	Drug: LB-100 for Injection\|Drug: Docetaxel	Tumors\|Neoplasms\|Cancer	Lixte Biotechnology Holdings Inc.	February 2013	Phase 1

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LB-100