LB-100

For research use only.

Catalog No.S7537

14 publications

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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Selleck's LB-100 has been cited by 14 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 MlTDSpVv[3Srb36gZZN{[Xl? NEj1SpgzNjVizszN MnTTN{Bpd3W{cx?= NIHtfHVNSi1zMECgd4lodmmoaXPhcpRtgSCnbnjhcoNm\CC2aHWgdJJweG:{dHnvckBw\iClZXzsd{BqdiCJMj;NMi=> MV[yPVE6QTByNh?=
DAOY cells M1f1[mNmdGxidnnhZoltcXS7IHHzd4F6 M4HGb2lEPTB;Mj65JO69VSxidYPpcochYFSWIHHzd4F6ew>? NHTxT28zPjd7OU[3NC=>
D341 cells M4K1cmNmdGxidnnhZoltcXS7IHHzd4F6 Mn:4TWM2OD1zLkmg{txONCC3c3nu[{BZXFRiYYPzZZl{ MVGyOlc6QTZ5MB?=
D283 cells Mof0R4VtdCC4aXHibYxqfHliYYPzZZk> MnnZTWM2OD1yLkmg{txONCC3c3nu[{BZXFRiYYPzZZl{ M{f2RlI3Pzl7Nkew
U251 cells NWn1XnpCTnWwY4Tpc44h[XO|YYm= MnHsNkDPxE1? NYHRTZl5OyCqb4Xyd{BidmRiNjDoc5Vzew>? M4XXRpRz\WG2bXXueEB4cXSqIEKg{txOKEyEMUCwJJJm\HWlZXSgVHAzSSCjY4Tpeol1gSC2bzC2NUUhd2ZiY3;ueJJwdCClZXzsd{Bi\nSncjDic5RpKHSqcnXlJIFv\CC|aYigbI92enNib3[gUGIyODBiZYjwc5N2emVw NXLDclFsOjV7M{m3OlI>
SKOV-3 M{LrVmN6fG:2b4jpZ4l1gSCjc4PhfS=> MkjvO|IhcA>? M2XkfGlEPTBiPTCxNE4yKMLzIEGuPEDPxE1? NFzheGwzPTN5Nk[wPC=>
OVCAR-8 NX7IVmlXS3m2b4TvfIlkcXS7IHHzd4F6 MXG3NkBp MX\JR|UxKD1iNT61JOKyKDBwNTFOwG0> MnrBNlU{PzZ4MEi=
PEO-4 NGPjRodEgXSxdH;4bYNqfHliYYPzZZk> NUPDVW5bPzJiaB?= MoCzTWM2OCB;IEWgxtEhOC54IN88US=> M4fnWlI2Ozd4NkC4
PEO-6 NYXYOXpyS3m2b4TvfIlkcXS7IHHzd4F6 M1jx[|czKGh? NV3wd|VHUUN3MDC9JFUvOSEEsTCwMlIh|ryP MXmyOVM4PjZyOB?=
PEO1-Brca2 Missense MnPsR5l1d3SxeHnjbZR6KGG|c3H5 M4niXFczKGh? MoP6TWM2OCB;IE[uNkDDuSBzLkWg{txO MnHTNlU{PzZ4MEi=
PEO1-Brca2 STOP NI\WRXFEgXSxdH;4bYNqfHliYYPzZZk> M2K1XFczKGh? MWjJR|UxKD1iNj6yJOKyKDFwMDFOwG0> NVLoeFVCOjV|N{[2NFg>
Huh-7 MXPQVFJCKGGldHn2bZR6KGG|c3H5dy=> Mn[5OUDPxG2xbD;M MYGyJIg> MX7y[YR2[2WmIITo[UBi[3Srdnn0fUBw\iCSUELBJJRwKGGkb4X0JFcxLQ>? MUOyOFg3PzJ2OR?=
HepG2 NG\vNZZRWDKDIHHjeIl3cXS7IHHzd4F6ew>? MYq1JO69dW:uL1y= M1X5clIhcA>? M4DhRpJm\HWlZXSgeIhmKGGldHn2bZR6KG:oIGDQNmEhfG9iYXLveZQhPzBn MnvoNlQ5Pjd{NEm=
HL-7702 NGnhcnhRWDKDIHHjeIl3cXS7IHHzd4F6ew>? NGnWNoY2KM7:bX;sM2w> M3nPdlIhcA>? M{\jPZJm\HWlZXSgeIhmKGGldHn2bZR6KG:oIGDQNmEhfG9iYXLveZQhPzBn MlnzNlQ5Pjd{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]
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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(O3)C2C(O)=O

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID