LB-100

For research use only.

Catalog No.S7537

29 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.

Selleck's LB-100 has been cited by 29 publications

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
U251 cells Mo\4SpVv[3Srb36gZZN{[Xl? MYeyJO69VQ>? NHmxcWc{KGixdYLzJIFv\CB4IHjveZJ{ M3TIO5Rz\WG2bXXueEB4cXSqIEKg{txOKEyEMUCwJJJm\HWlZXSgVHAzSSCjY4Tpeol1gSC2bzC2NUUhd2ZiY3;ueJJwdCClZXzsd{Bi\nSncjDic5RpKHSqcnXlJIFv\CC|aYigbI92enNib3[gUGIyODBiZYjwc5N2emVw M1q1UlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3OUO5O|YzLz5{NUmzPVc3OjxxYU6=
D283 cells M{H4UWNmdGxidnnhZoltcXS7IHHzd4F6 M4jDUGlEPTB;MD65JO69VSxidYPpcochYFSWIHHzd4F6ew>? MV[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPjd7OU[3NEc,OjZ5OUm2O|A9N2F-
DAOY cells NF3ZN5pE\WyuII\pZYJqdGm2eTDhd5NigQ>? MXPJR|UxRTJwOTFOwG0tKHW|aX7nJHhVXCCjc4PhfZM> MmrWQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjZ5OUm2O|AoRjJ4N{m5OlcxRC:jPh?=
D341 cells MlHFR4VtdCC4aXHibYxqfHliYYPzZZk> MVPJR|UxRTFwOTFOwG0tKHW|aX7nJHhVXCCjc4PhfZM> NFXJW4I9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{Nke5PVY4OCd-Mk[3PVk3PzB:L3G+
CH-157 cells Mmr1SpVv[3Srb36gZZN{[Xl? MUiyMlUh|ryP NUf0Tll4OyCqb4Xydy=> NFjqSVRNSi1zMECgd4lodmmoaXPhcpRtgSCnbnjhcoNm\CC2aHWgdJJweG:{dHnvckBw\iClZXzsd{BqdiCJMj;NMi=> M3[1UVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7MUm5NFA3Lz5{OUG5PVAxPjxxYU6=
SKOV-3 NHf5VYJEgXSxdH;4bYNqfHliYYPzZZk> MUi3NkBp NHjBW2NKSzVyIE2gNVAvOSEEsTCxMlgh|ryP M2DRNlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3M{e2OlA5Lz5{NUO3OlYxQDxxYU6=
OVCAR-8 MXfDfZRwfG:6aXPpeJkh[XO|YYm= M{XJS|czKGh? MlLSTWM2OCB;IEWuOUDDuSByLkWg{txO NYC0[3BURGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkWzO|Y3ODhpPkK1N|c3PjB6PD;hQi=>
PEO-4 MXnDfZRwfG:6aXPpeJkh[XO|YYm= M{GxTlczKGh? NWraeIFwUUN3MDC9JFUhyrFiMD62JO69VQ>? MkPSQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV|N{[2NFgoRjJ3M{e2OlA5RC:jPh?=
PEO-6 NEHubWJEgXSxdH;4bYNqfHliYYPzZZk> MWq3NkBp MXPJR|UxKD1iNT6xJOKyKDBwMjFOwG0> MXS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTN5Nk[wPEc,OjV|N{[2NFg9N2F-
PEO1-Brca2 Missense NXj1NHNwS3m2b4TvfIlkcXS7IHHzd4F6 MkXhO|IhcA>? NF;lPVJKSzVyIE2gOk4zKMLzIEGuOUDPxE1? NIrKc2s9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUO3OlYxQCd-MkWzO|Y3ODh:L3G+
PEO1-Brca2 STOP NHfMU4lEgXSxdH;4bYNqfHliYYPzZZk> NVHOUmFFPzJiaB?= M4rN[GlEPTBiPTC2MlIhyrFiMT6wJO69VQ>? NHHvepE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUO3OlYxQCd-MkWzO|Y3ODh:L3G+
Huh-7 M1\SVXBROkFiYXP0bZZqfHliYYPzZZl{ NGHIPFc2KM7:bX;sM2w> M{jmVVIhcA>? Ml:0doVlfWOnZDD0bIUh[WO2aY\peJkhd2ZiUGCyRUB1dyCjYn;1eEA4OCV? NHrFdWc9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEi2O|I1QSd-MkS4OlczPDl:L3G+
HepG2 Ml\wVHAzSSCjY4Tpeol1gSCjc4PhfZM> NEK1eXE2KM7:bX;sM2w> NWHEUFZDOiCq MlHCdoVlfWOnZDD0bIUh[WO2aY\peJkhd2ZiUGCyRUB1dyCjYn;1eEA4OCV? NVzBcnpIRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS4OlczPDlpPkK0PFY4OjR7PD;hQi=>
HL-7702 MlTEVHAzSSCjY4Tpeol1gSCjc4PhfZM> NFPv[2E2KM7:bX;sM2w> M2P3V|IhcA>? MVjy[YR2[2WmIITo[UBi[3Srdnn0fUBw\iCSUELBJJRwKGGkb4X0JFcxLQ>? NW\nfoxpRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS4OlczPDlpPkK0PFY4OjR7PD;hQi=>

... 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
NCT03886662 Unknown status Drug: LB-100 Myelodysplastic Syndromes Lixte Biotechnology Holdings Inc. April 2019 Phase 1|Phase 2
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) January 9 2019 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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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID