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LB100

Catalog No. T4449   CAS 1632032-53-1
Synonyms: LB-100, LB 100

LB100 (LB-100) is a water soluble protein phosphatase 2A (PP2A) inhibitor.

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LB100 Chemical Structure
LB100, CAS 1632032-53-1
Pack Size Availability Price/USD Quantity
1 mg In stock $ 51.00
2 mg In stock $ 71.00
5 mg In stock $ 108.00
10 mg In stock $ 198.00
25 mg In stock $ 316.00
50 mg In stock $ 469.00
100 mg In stock $ 687.00
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Purity: 98.63%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description LB100 (LB-100) is a water soluble protein phosphatase 2A (PP2A) inhibitor.
Targets&IC50 PP2A(BxPc-3):0.85 μM, PP2A(Panc-1):3.87 μM
In vitro In xenograft mouse models of pancreatic cancer, LB-100 (2 mg/kg, i.p.) enhances the therapeutic efficacy of the chemotherapy agent doxorubicin. LB-100 increases both the blood flow velocity on the tumor surface and the microvascular density of the tumor.
In vivo Compared to the control group, LB-100 significantly increased the intracellular concentration of doxorubicin by approximately 2.5 times, enhancing the tumor cells' sensitivity to doxorubicin. Additionally, LB-100 amplified the secretion of vascular endothelial growth factor, thereby promoting angiogenesis mediated by HIF-1α-VEGF. LB-100 also demonstrated a notable inhibitory effect on the growth of BxPc-3 (IC50: 2.3 μM) and Panc-1 (IC50: 1.7 μM) cells. Following treatment with LB-100, a reduction of 30-50% in PP2A activity was observed in BxPc-3, SW1990, and Panc-1 tumor cells.
Kinase Assay 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 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 speci?c controls. (Only for Reference)
Synonyms LB-100, LB 100
Molecular Weight 268.31
Formula C13H20N2O4
CAS No. 1632032-53-1

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

H2O: 49 mg/mL (182.6 mM)

DMSO: < 1 mg/mL (insoluble or slightly soluble)

Ethanol: < 1 mg/mL (insoluble or slightly soluble)

TargetMolReferences and Literature

1. Bai X, et al. Inhibition of protein phosphatase 2A sensitizes pancreatic cancer to chemotherapy by increasing drug perfusion via HIF-1α-VEGF mediated angiogenesis. Cancer Lett. 2014 Oct 7. pii: S0304-3835(14)00589-8. 2. Bai XL, et al. Inhibition of protein phosphatase 2A enhances cytotoxicity and accessibility of chemotherapeutic drugs to hepatocellular carcinomas. Mol Cancer Ther. 2014 Aug;13(8):2062-72. 3. Fu QH, et al. LB-100 sensitizes hepatocellular carcinoma cells to the effects of sorafenib during hypoxia by activation of Smad3 phosphorylation. Tumour Biol. 2016 Jun;37(6):7277-8

TargetMolCitations

1. Zhang J, Cen L, Zhang X, et al. MPST deficiency promotes intestinal epithelial cell apoptosis and aggravates inflammatory bowel disease via AKT. Redox Biology. 2022: 102469.

Related compound libraries

This product is contained In the following compound libraries:
Glycometabolism Compound Library Lipid Metabolism Compound Library NO PAINS Compound Library Anti-Obesity Compound Library

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Keywords

LB100 1632032-53-1 Metabolism Phosphatase LB-100 LB 100 inhibitor inhibit

 

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