Home PI3K/Akt/mTOR PP2A inhibitor LB-100

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

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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+
Click to View More Cell Line Experimental Data
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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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

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