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 32 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 MorBSpVv[3Srb36gZZN{[Xl? MmPnNkDPxE1? NGLaeZg{KGixdYLzJIFv\CB4IHjveZJ{ MnHheJJm[XSvZX70JJdqfGhiMjFOwG0hVEJzMECgdoVlfWOnZDDQVFJCKGGldHn2bZR6KHSxIE[xKUBw\iClb370do9tKGOnbHzzJIFnfGW{IHLveIghfGi{ZXWgZY5lKHOreDDoc5VzeyCxZjDMRlExOCCneIDvd5Vz\S5? M4GyUVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3OUO5O|YzLz5{NUmzPVc3OjxxYU6=
D283 cells MV\D[YxtKH[rYXLpcIl1gSCjc4PhfS=> M2HWVGlEPTB;MD65JO69VSxidYPpcochYFSWIHHzd4F6ew>? M2LvRVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ4N{m5OlcxLz5{Nke5PVY4ODxxYU6=
DAOY cells MVHD[YxtKH[rYXLpcIl1gSCjc4PhfS=> M2\XT2lEPTB;Mj65JO69VSxidYPpcochYFSWIHHzd4F6ew>? M1y1[|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ4N{m5OlcxLz5{Nke5PVY4ODxxYU6=
D341 cells M4DUWmNmdGxidnnhZoltcXS7IHHzd4F6 NUjGb2k2UUN3ME2xMlkh|ryPLDD1d4lv\yC[VGSgZZN{[Xm| MYe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPjd7OU[3NEc,OjZ5OUm2O|A9N2F-
CH-157 cells NFnEUXdHfW6ldHnvckBie3OjeR?= NFnhPWMzNjVizszN M1vJ[lMhcG:3coO= NHraPVJNSi1zMECgd4lodmmoaXPhcpRtgSCnbnjhcoNm\CC2aHWgdJJweG:{dHnvckBw\iClZXzsd{BqdiCJMj;NMi=> M4joUFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7MUm5NFA3Lz5{OUG5PVAxPjxxYU6=
SKOV-3 M2G0PWN6fG:2b4jpZ4l1gSCjc4PhfS=> M2jTV|czKGh? NUizRlZTUUN3MDC9JFExNjFiwsGgNU45KM7:TR?= NUTERWhvRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkWzO|Y3ODhpPkK1N|c3PjB6PD;hQi=>
OVCAR-8 NVTtT2RsS3m2b4TvfIlkcXS7IHHzd4F6 M2rrOFczKGh? MWPJR|UxKD1iNT61JOKyKDBwNTFOwG0> MV[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTN5Nk[wPEc,OjV|N{[2NFg9N2F-
PEO-4 NGPvTmhEgXSxdH;4bYNqfHliYYPzZZk> MmTjO|IhcA>? NVu3PYRXUUN3MDC9JFUhyrFiMD62JO69VQ>? NILie5Y9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUO3OlYxQCd-MkWzO|Y3ODh:L3G+
PEO-6 NFPRe5VEgXSxdH;4bYNqfHliYYPzZZk> NFe0XXo4OiCq M1rTdWlEPTBiPTC1MlEhyrFiMD6yJO69VQ>? NUi5cpBGRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkWzO|Y3ODhpPkK1N|c3PjB6PD;hQi=>
PEO1-Brca2 Missense NV\iN5luS3m2b4TvfIlkcXS7IHHzd4F6 NHPIUI04OiCq MojqTWM2OCB;IE[uNkDDuSBzLkWg{txO Ml;vQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV|N{[2NFgoRjJ3M{e2OlA5RC:jPh?=
PEO1-Brca2 STOP MVfDfZRwfG:6aXPpeJkh[XO|YYm= NFLWWnI4OiCq NWK3WWF7UUN3MDC9JFYvOiEEsTCxMlAh|ryP NFe2[Yk9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUO3OlYxQCd-MkWzO|Y3ODh:L3G+
Huh-7 NI\0OoVRWDKDIHHjeIl3cXS7IHHzd4F6ew>? NWfzPWxpPSEQvH3vcE9N M2r1UVIhcA>? Ml\YdoVlfWOnZDD0bIUh[WO2aY\peJkhd2ZiUGCyRUB1dyCjYn;1eEA4OCV? Ml[4QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR6NkeyOFkoRjJ2OE[3NlQ6RC:jPh?=
HepG2 M1G0R3BROkFiYXP0bZZqfHliYYPzZZl{ NIjselQ2KM7:bX;sM2w> MkfyNkBp NWnLW4YyemWmdXPl[EB1cGViYXP0bZZqfHlib3[gVHAzSSC2bzDhZo92fCB5MDW= MVm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDh4N{K0PUc,OjR6NkeyOFk9N2F-
HL-7702 NIG0[JhRWDKDIHHjeIl3cXS7IHHzd4F6ew>? MnrPOUDPxG2xbD;M NWfKWYI3OiCq NYfJWWJLemWmdXPl[EB1cGViYXP0bZZqfHlib3[gVHAzSSC2bzDhZo92fCB5MDW= NGK1WHI9[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 Enrolling by invitation 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 2022-01-17)

Tech Support

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