LB-100

For research use only.

Catalog No.S7537

16 publications

LB-100 Chemical Structure

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.

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Selleck's LB-100 has been cited by 16 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 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 Formulation Activity Description PMID
CH-157 cells MXTGeY5kfGmxbjDhd5NigQ>? MnzxNk42KM7:TR?= Mn31N{Bpd3W{cx?= MUjMRk0yODBic3nncolncWOjboTsfUBmdmijbnPl[EB1cGVicILvdI9zfGmxbjDv[kBk\WyuczDpckBIOi:PLh?= Mm[1NlkyQTlyME[=
DAOY cells MlO4R4VtdCC4aXHibYxqfHliYYPzZZk> M3Lib2lEPTB;Mj65JO69VSxidYPpcochYFSWIHHzd4F6ew>? NVHO[5ZyOjZ5OUm2O|A>
D341 cells MXzD[YxtKH[rYXLpcIl1gSCjc4PhfS=> NGL0N3ZKSzVyPUGuPUDPxE1uIIXzbY5oKFiWVDDhd5NigXN? M1HZd|I3Pzl7Nkew
D283 cells NI\vfG1E\WyuII\pZYJqdGm2eTDhd5NigQ>? MnvDTWM2OD1yLkmg{txONCC3c3nu[{BZXFRiYYPzZZl{ MnH2NlY4QTl4N{C=
U251 cells MofrSpVv[3Srb36gZZN{[Xl? NI\lWVczKM7:TR?= MUSzJIhwfXK|IHHu[EA3KGixdYLz NH3hOJl1emWjdH3lcpQhf2m2aDCyJO69VSCOQkGwNEBz\WS3Y3XkJHBROkFiYXP0bZZqfHlidH:gOlEmKG:oIHPvcpRzd2xiY3XscJMh[W[2ZYKgZo91cCC2aILl[UBidmRic3n4JIhwfXK|IH;mJGxDOTByIHX4dI9{fXKnLh?= M1PSc|I2QTN7N{[y
SKOV-3 NIi4UVlEgXSxdH;4bYNqfHliYYPzZZk> MoXaO|IhcA>? M1TvOWlEPTBiPTCxNE4yKMLzIEGuPEDPxE1? M1;uW|I2Ozd4NkC4
OVCAR-8 M1;PO2N6fG:2b4jpZ4l1gSCjc4PhfS=> M4HXOFczKGh? M4rnWmlEPTBiPTC1MlUhyrFiMD61JO69VQ>? M3XnNlI2Ozd4NkC4
PEO-4 NWX5S2NOS3m2b4TvfIlkcXS7IHHzd4F6 NF:3PIo4OiCq Mof1TWM2OCB;IEWgxtEhOC54IN88US=> NIfKXnMzPTN5Nk[wPC=>
PEO-6 NVTHbWkyS3m2b4TvfIlkcXS7IHHzd4F6 MYO3NkBp NHzx[I1KSzVyIE2gOU4yKMLzIECuNkDPxE1? MnHMNlU{PzZ4MEi=
PEO1-Brca2 Missense MXHDfZRwfG:6aXPpeJkh[XO|YYm= NXH0S3VGPzJiaB?= MlriTWM2OCB;IE[uNkDDuSBzLkWg{txO NH3S[HkzPTN5Nk[wPC=>
PEO1-Brca2 STOP NWPE[2xZS3m2b4TvfIlkcXS7IHHzd4F6 M3npfVczKGh? MYHJR|UxKD1iNj6yJOKyKDFwMDFOwG0> NIToO4kzPTN5Nk[wPC=>
Huh-7 MUTQVFJCKGGldHn2bZR6KGG|c3H5dy=> NX;2b4NmPSEQvH3vcE9N MWeyJIg> M2W0VZJm\HWlZXSgeIhmKGGldHn2bZR6KG:oIGDQNmEhfG9iYXLveZQhPzBn NIj6XIwzPDh4N{K0PS=>
HepG2 NUjKcpd[WFB{QTDhZ5Rqfmm2eTDhd5NigXN? NIPRSnA2KM7:bX;sM2w> MXWyJIg> NHXRcYxz\WS3Y3XkJJRp\SCjY4Tpeol1gSCxZjDQVFJCKHSxIHHic5V1KDdyJR?= M1u0cVI1QDZ5MkS5
HL-7702 Ml3OVHAzSSCjY4Tpeol1gSCjc4PhfZM> MUK1JO69dW:uL1y= NETnUIczKGh? NIWyZ|Jz\WS3Y3XkJJRp\SCjY4Tpeol1gSCxZjDQVFJCKHSxIHHic5V1KDdyJR?= NUf2d404OjR6NkeyOFk>

... 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]

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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]

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  • 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]

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  • Animal Models: BALB/c nude mice bearing Panc-1 xenograft
  • 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
Smiles CN1CCN(CC1)C(=O)C2C3CCC(C2C(=O)O)O3

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Clinical Trial Information

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

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.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID