LB-100

Catalog No.S7537

For research use only.

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.

LB-100 Chemical Structure

CAS No. 1026680-07-8

Selleck's LB-100 has been cited by 33 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 NWHTV3dwTnWwY4Tpc44h[XO|YYm= MYCyJO69VQ>? MluxN{Bpd3W{czDhcoQhPiCqb4Xydy=> MlrjeJJm[XSvZX70JJdqfGhiMjFOwG0hVEJzMECgdoVlfWOnZDDQVFJCKGGldHn2bZR6KHSxIE[xKUBw\iClb370do9tKGOnbHzzJIFnfGW{IHLveIghfGi{ZXWgZY5lKHOreDDoc5VzeyCxZjDMRlExOCCneIDvd5Vz\S5? Ml3WQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV7M{m3OlIoRjJ3OUO5O|YzRC:jPh?=
D283 cells M1XYRWNmdGxidnnhZoltcXS7IHHzd4F6 MX\JR|UxRTBwOTFOwG0tKHW|aX7nJHhVXCCjc4PhfZM> NXP4UGYzRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMk[3PVk3PzBpPkK2O|k6PjdyPD;hQi=>
DAOY cells MV\D[YxtKH[rYXLpcIl1gSCjc4PhfS=> MnHxTWM2OD1{Lkmg{txONCC3c3nu[{BZXFRiYYPzZZl{ NH:wdmU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{Nke5PVY4OCd-Mk[3PVk3PzB:L3G+
D341 cells MXPD[YxtKH[rYXLpcIl1gSCjc4PhfS=> MonxTWM2OD1zLkmg{txONCC3c3nu[{BZXFRiYYPzZZl{ Mni3QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjZ5OUm2O|AoRjJ4N{m5OlcxRC:jPh?=
CH-157 cells NXvne2RjTnWwY4Tpc44h[XO|YYm= NGPzWlMzNjVizszN NYLKSoR4OyCqb4Xydy=> NX;YWIlCVEJvMUCwJJNq\26rZnnjZY51dHliZX7oZY5k\WRidHjlJJBzd3CxcoTpc44hd2ZiY3XscJMhcW5iR{KvUU4> MkO1QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjlzOUmwNFYoRjJ7MUm5NFA3RC:jPh?=
SKOV-3 NWDzNItWS3m2b4TvfIlkcXS7IHHzd4F6 NIC2bno4OiCq MXvJR|UxKD1iMUCuNUDDuSBzLkig{txO NXG5fYZVRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkWzO|Y3ODhpPkK1N|c3PjB6PD;hQi=>
OVCAR-8 MkfzR5l1d3SxeHnjbZR6KGG|c3H5 NXfGUoFVPzJiaB?= M3TDSmlEPTBiPTC1MlUhyrFiMD61JO69VQ>? NYP2W3BWRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkWzO|Y3ODhpPkK1N|c3PjB6PD;hQi=>
PEO-4 M2\CeWN6fG:2b4jpZ4l1gSCjc4PhfS=> MVi3NkBp NYrTRox4UUN3MDC9JFUhyrFiMD62JO69VQ>? MUO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTN5Nk[wPEc,OjV|N{[2NFg9N2F-
PEO-6 NI\J[YNEgXSxdH;4bYNqfHliYYPzZZk> NXTjcYtWPzJiaB?= NYHMSo43UUN3MDC9JFUvOSEEsTCwMlIh|ryP MXu8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTN5Nk[wPEc,OjV|N{[2NFg9N2F-
PEO1-Brca2 Missense M1PtUWN6fG:2b4jpZ4l1gSCjc4PhfS=> NYrW[VZIPzJiaB?= M2HrRWlEPTBiPTC2MlIhyrFiMT61JO69VQ>? MnTpQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV|N{[2NFgoRjJ3M{e2OlA5RC:jPh?=
PEO1-Brca2 STOP M2rSdWN6fG:2b4jpZ4l1gSCjc4PhfS=> MYK3NkBp NIHhdVJKSzVyIE2gOk4zKMLzIEGuNEDPxE1? MoLWQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV|N{[2NFgoRjJ3M{e2OlA5RC:jPh?=
Huh-7 MnvWVHAzSSCjY4Tpeol1gSCjc4PhfZM> M3\GOlUh|ryvb3yvUC=> Ml7RNkBp MV;y[YR2[2WmIITo[UBi[3Srdnn0fUBw\iCSUELBJJRwKGGkb4X0JFcxLQ>? NYS1b2R6RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS4OlczPDlpPkK0PFY4OjR7PD;hQi=>
HepG2 NUnGbJRoWFB{QTDhZ5Rqfmm2eTDhd5NigXN? Mkf0OUDPxG2xbD;M NWK0cpFGOiCq NELtOYZz\WS3Y3XkJJRp\SCjY4Tpeol1gSCxZjDQVFJCKHSxIHHic5V1KDdyJR?= NF;hSmU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEi2O|I1QSd-MkS4OlczPDl:L3G+
HL-7702 MV3QVFJCKGGldHn2bZR6KGG|c3H5dy=> MWm1JO69dW:uL1y= M2\oeVIhcA>? MkT4doVlfWOnZDD0bIUh[WO2aY\peJkhd2ZiUGCyRUB1dyCjYn;1eEA4OCV? NHTkUIw9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEi2O|I1QSd-MkS4OlczPDl:L3G+
Assay
Methods Test Index PMID
Western blot Cyclin D1 / c-myc / mcl-1 / Hsp90 29199006
Growth inhibition assay Cell division ; Cell viability 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 (from reference)

Kinase Assay:

[1]

  • 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]

  • 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.

Animal Research:

[1]

  • Animal Models: BALB/c nude mice bearing Panc-1 xenograft
  • Dosages: 2 mg/kg
  • Administration: i.p.

Solubility (25°C)

In vitro

Chemical Information

Molecular Weight 268.31
Formula

C13H20N2O4

CAS No. 1026680-07-8
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CN1CCN(CC1)C(=O)C2C3CCC(C2C(=O)O)O3

In vivo Formulation Calculator (Clear solution)

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

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Molarity Calculator

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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

(data from https://clinicaltrials.gov, updated on 2022-08-01)

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.

Handling Instructions

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