LB-100

Name: LB-100
Brand: Selleck Chemicals
SKU: S7537
Rating: 5 (17 reviews)

For research use only.

Catalog No.S7537

17 publications

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 17 publications

J Cell Biol, 2020, 219(4)

PubMed: 32050025 ( click the link to review the publication )

Cancer Res, 2020, 10;canres.57.2020

PubMed: 32522823 ( click the link to review the publication )

Int J Mol Sci, 2020, 21(18)E6642

PubMed: 32927892 ( click the link to review the publication )

PLoS One, 2020, 29;15(5):e0233863

PubMed: 32470053 ( click the link to review the publication )

Neurosci Lett, 2020, 721:134817

PubMed: 32032748 ( click the link to review the publication )

Biochem Biophys Res Commun, 2020, 526(1):1-7

PubMed: 32192773 ( click the link to review the publication )

Sci Rep, 2020, 10(1):10992

PubMed: 32620893 ( click the link to review the publication )

World J Gastroenterol, 2019, 25(45):6607-6618

PubMed: 31832001 ( click the link to review the publication )

Eur J Pharmacol, 2019, 852:99-106

PubMed: 30851273 ( click the link to review the publication )

Mol Cell, 2018, 71(1):11-24

PubMed: 29937341 ( click the link to review the publication )

Mol Cancer, 2018, 17(1):44

PubMed: 29455644 ( click the link to review the publication )

Exp Mol Med, 2018, 50(7):83

PubMed: 30050113 ( click the link to review the publication )

Anticancer Res, 2018, 38(10):5791-5798

PubMed: 30275201 ( click the link to review the publication )

Am J Pathol, 2017, 187(8):1736-1749

PubMed: 28627412 ( click the link to review the publication )

Mediators Inflamm, 2017, 2017:5706152

PubMed: 29056830 ( click the link to review the publication )

PLoS One, 2017, 12(3):e0173386

PubMed: 28267764 ( click the link to review the publication )

Oncotarget, 2017, 9(7):7312-7321

PubMed: 29484112 ( click the link to review the publication )

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 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	Activity Description	PMID
U251 cells	MoXzSpVv[3Srb36gZZN{[Xl?	NHvaSHAzKM7:TR?=	MVWzJIhwfXK\|IHHu[EA3KGixdYLz	MmfreJJm[XSvZX70JJdqfGhiMjFOwG0hVEJzMECgdoVlfWOnZDDQVFJCKGGldHn2bZR6KHSxIE[xKUBw\iClb370do9tKGOnbHzzJIFnfGW{IHLveIghfGi{ZXWgZY5lKHOreDDoc5VzeyCxZjDMRlExOCCneIDvd5Vz\S5?	NF\U[lA9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUmzPVc3Oid-MkW5N\|k4PjJ:L3G+
D283 cells	MYTD[YxtKH[rYXLpcIl1gSCjc4PhfS=>			NXLIZlZEUUN3ME2wMlkh\|ryPLDD1d4lv\yC[VGSgZZN{[Xm\|	Mny4QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjZ5OUm2O\|AoRjJ4N{m5OlcxRC:jPh?=
DAOY cells	NFLpbZpE\WyuII\pZYJqdGm2eTDhd5NigQ>?			NH3uPJBKSzVyPUKuPUDPxE1uIIXzbY5oKFiWVDDhd5NigXN?	MYW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPjd7OU[3NEc,OjZ5OUm2O\|A9N2F-
D341 cells	NIPIcWlE\WyuII\pZYJqdGm2eTDhd5NigQ>?			NIfEb4FKSzVyPUGuPUDPxE1uIIXzbY5oKFiWVDDhd5NigXN?	M1fUcVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ4N{m5OlcxLz5{Nke5PVY4ODxxYU6=
CH-157 cells	MWXGeY5kfGmxbjDhd5NigQ>?	MUCyMlUh\|ryP	M{XCWlMhcG:3coO=	MoL5UGIuOTByIIPp[45q\mmlYX70cJkh\W6qYX7j[YQhfGinIIDyc5BwenSrb36gc4Yh[2WubIOgbY4hTzJxTT6=	MV[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTF7OUCwOkc,OjlzOUmwNFY9N2F-
SKOV-3	M3LhR2N6fG:2b4jpZ4l1gSCjc4PhfS=>		MUS3NkBp	MUPJR\|UxKD1iMUCuNUDDuSBzLkig{txO	NIn3PW89[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUO3OlYxQCd-MkWzO\|Y3ODh:L3G+
OVCAR-8	MnvYR5l1d3SxeHnjbZR6KGG\|c3H5		NUTuRWFqPzJiaB?=	M13FS2lEPTBiPTC1MlUhyrFiMD61JO69VQ>?	MnHBQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV\|N{[2NFgoRjJ3M{e2OlA5RC:jPh?=
PEO-4	MoPmR5l1d3SxeHnjbZR6KGG\|c3H5		M364eFczKGh?	MULJR\|UxKD1iNTFCtUAxNjZizszN	NEK0e3Y9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUO3OlYxQCd-MkWzO\|Y3ODh:L3G+
PEO-6	M{TTe2N6fG:2b4jpZ4l1gSCjc4PhfS=>		M4nPUVczKGh?	M{Pyb2lEPTBiPTC1MlEhyrFiMD6yJO69VQ>?	MU[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTN5Nk[wPEc,OjV\|N{[2NFg9N2F-
PEO1-Brca2 Missense	NH3kTVJEgXSxdH;4bYNqfHliYYPzZZk>		NILFUWE4OiCq	MkLCTWM2OCB;IE[uNkDDuSBzLkWg{txO	MVq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTN5Nk[wPEc,OjV\|N{[2NFg9N2F-
PEO1-Brca2 STOP	M1XMeWN6fG:2b4jpZ4l1gSCjc4PhfS=>		MXm3NkBp	NYrHNlR1UUN3MDC9JFYvOiEEsTCxMlAh\|ryP	NXv5bVhtRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkWzO\|Y3ODhpPkK1N\|c3PjB6PD;hQi=>
Huh-7	M3\aZnBROkFiYXP0bZZqfHliYYPzZZl{	M332VFUh\|ryvb3yvUC=>	M{PrclIhcA>?	MoXCdoVlfWOnZDD0bIUh[WO2aY\peJkhd2ZiUGCyRUB1dyCjYn;1eEA4OCV?	M17WWFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2OE[3NlQ6Lz5{NEi2O\|I1QTxxYU6=
HepG2	M4H1R3BROkFiYXP0bZZqfHliYYPzZZl{	NX\6XItYPSEQvH3vcE9N	M1XQWlIhcA>?	MYDy[YR2[2WmIITo[UBi[3Srdnn0fUBw\iCSUELBJJRwKGGkb4X0JFcxLQ>?	NHn1[m09[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEi2O\|I1QSd-MkS4OlczPDl:L3G+
HL-7702	M{H6UHBROkFiYXP0bZZqfHliYYPzZZl{	Mk\LOUDPxG2xbD;M	NYjwZmdlOiCq	MWTy[YR2[2WmIITo[UBi[3Srdnn0fUBw\iCSUELBJJRwKGGkb4X0JFcxLQ>?	NIC1bWM9[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	p-AMPKα1 / AMPKα1 / p-ACC / ACC / p-p70S6K1 / p-4EBP1 ; PubMed: 29221169 Oncotarget 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 Cancer Lett 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 Nat Commun 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 Cancer Lett 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]	- Collapse 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]	- Collapse 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]	- Collapse Animal Models: BALB/c nude mice bearing Panc-1 xenograft Dosages: 2 mg/kg Administration: i.p. (Only for Reference)

References

[1] Bai X, et al. Cancer Lett. 2014, 355(2), 281-287.

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 Download LB-100 SDF

Molecular Weight	268.31
Formula	C₁₃H₂₀N₂O₄
CAS No.	1026680-07-8
Storage	3 years-20°C powder 2 years-80°C in solvent
Synonyms	N/A
Smiles	CN1CCN(CC1)C(=O)C2C3CCC(C2C(=O)O)O3

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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.

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LB-100