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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Cited by 3 Publications

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 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]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
CH-157 cells MX7GeY5kfGmxbjDhd5NigQ>? NGCwfYczNjVizszN MoDhN{Bpd3W{cx?= NWr5TGV4VEJvMUCwJJNq\26rZnnjZY51dHliZX7oZY5k\WRidHjlJJBzd3CxcoTpc44hd2ZiY3XscJMhcW5iR{KvUU4> MmDHNlkyQTlyME[=
DAOY cells MYXD[YxtKH[rYXLpcIl1gSCjc4PhfS=> MnS2TWM2OD1{Lkmg{txONCC3c3nu[{BZXFRiYYPzZZl{ NUXHXIdOOjZ5OUm2O|A>
D341 cells NWTJbFFiS2WubDD2bYFjcWyrdImgZZN{[Xl? MVLJR|UxRTFwOTFOwG0tKHW|aX7nJHhVXCCjc4PhfZM> NX3WNnFoOjZ5OUm2O|A>
D283 cells NF7G[|RE\WyuII\pZYJqdGm2eTDhd5NigQ>? MmDmTWM2OD1yLkmg{txONCC3c3nu[{BZXFRiYYPzZZl{ MViyOlc6QTZ5MB?=
U251 cells MnnVSpVv[3Srb36gZZN{[Xl? NXjRVoQzOiEQvF2= M2DaUlMhcG:3coOgZY5lKDZiaH;1dpM> NITrdnh1emWjdH3lcpQhf2m2aDCyJO69VSCOQkGwNEBz\WS3Y3XkJHBROkFiYXP0bZZqfHlidH:gOlEmKG:oIHPvcpRzd2xiY3XscJMh[W[2ZYKgZo91cCC2aILl[UBidmRic3n4JIhwfXK|IH;mJGxDOTByIHX4dI9{fXKnLh?= MoezNlU6Ozl5NkK=
SKOV-3 M{j6VGN6fG:2b4jpZ4l1gSCjc4PhfS=> NGDDcpA4OiCq MUDJR|UxKD1iMUCuNUDDuSBzLkig{txO NWTKV5plOjV|N{[2NFg>
OVCAR-8 MkDmR5l1d3SxeHnjbZR6KGG|c3H5 NVr6OYNrPzJiaB?= NFnhd|BKSzVyIE2gOU42KMLzIECuOUDPxE1? M2HRN|I2Ozd4NkC4
PEO-4 NXPBZmJkS3m2b4TvfIlkcXS7IHHzd4F6 NFm3OYk4OiCq NELYNVRKSzVyIE2gOUDDuSByLk[g{txO NXLmVIZuOjV|N{[2NFg>
PEO-6 NILhSFZEgXSxdH;4bYNqfHliYYPzZZk> NXn4cW5nPzJiaB?= Mk\6TWM2OCB;IEWuNUDDuSByLkKg{txO MkD6NlU{PzZ4MEi=
PEO1-Brca2 Missense M4DOXGN6fG:2b4jpZ4l1gSCjc4PhfS=> MXq3NkBp M3zPPGlEPTBiPTC2MlIhyrFiMT61JO69VQ>? M3\TXFI2Ozd4NkC4
PEO1-Brca2 STOP M{G1[mN6fG:2b4jpZ4l1gSCjc4PhfS=> MlfhO|IhcA>? MlG1TWM2OCB;IE[uNkDDuSBzLkCg{txO NFv2UYgzPTN5Nk[wPC=>
Huh-7 M{LVRnBROkFiYXP0bZZqfHliYYPzZZl{ MWS1JO69dW:uL1y= MYOyJIg> NFLPSXFz\WS3Y3XkJJRp\SCjY4Tpeol1gSCxZjDQVFJCKHSxIHHic5V1KDdyJR?= M1L5TVI1QDZ5MkS5
HepG2 NEntVINRWDKDIHHjeIl3cXS7IHHzd4F6ew>? MVK1JO69dW:uL1y= NYLVRnNJOiCq MUHy[YR2[2WmIITo[UBi[3Srdnn0fUBw\iCSUELBJJRwKGGkb4X0JFcxLQ>? M1Toe|I1QDZ5MkS5
HL-7702 NX\WfYJTWFB{QTDhZ5Rqfmm2eTDhd5NigXN? MWO1JO69dW:uL1y= NWTZbJJVOiCq MnvHdoVlfWOnZDD0bIUh[WO2aY\peJkhd2ZiUGCyRUB1dyCjYn;1eEA4OCV? Ml;PNlQ5Pjd{NEm=

... 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     


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     


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     


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     


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]

+ Expand

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]

+ Expand
  • 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]

+ Expand
  • 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 Recruiting Astrocytoma Grade IV|Glioblastoma Multiforme|Giant Cell Glioblastoma National Cancer Institute (NCI)|National Institutes of Health Clinical Center (CC) May 1 2019 Phase 2
NCT03027388 Recruiting Astrocytoma Grade IV|Glioblastoma Multiforme|Giant Cell Glioblastoma National Cancer Institute (NCI)|National Institutes of Health Clinical Center (CC) May 1 2019 Phase 2
NCT03886662 Not yet recruiting Myelodysplastic Syndromes Lixte Biotechnology Holdings Inc. April 2019 Phase 1|Phase 2
NCT03886662 Not yet recruiting Myelodysplastic Syndromes Lixte Biotechnology Holdings Inc. April 2019 Phase 1|Phase 2
NCT01837667 Completed Tumors|Neoplasms|Cancer Lixte Biotechnology Holdings Inc. February 2013 Phase 1
NCT01837667 Completed Tumors|Neoplasms|Cancer Lixte Biotechnology Holdings Inc. February 2013 Phase 1

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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.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID