LB-100

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Chemical Information

Product name：LB-100	Purity：98% min
CAS NO：1026680-07-8	Solubility：Soluble in DMSO and water
Molecular Formula：C₁₃H₂₀N₂O₄	Package：Package according to customer requirements
Molecular Weight：268.309	Storage：Store at -20℃

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Remarks

LB-100 is a protein phosphatase 2A(PP2A)inhibitor. LB-100 sensitizes hepatocellular carcinoma cells to the effects of sorafenib during hypoxia by activation of Smad3 phosphorylation. LB-100 enhanced the effects of sorafenib in HCC cells only during hypoxic environments. LB-100 dramatically increased intracellular p-Smad3 level, which was responsible for the effect of LB-100 as a sensitizer. LB-100 downregulated Bcl-2 expression and enhanced sorafenib-induced apoptosis in HCC cells.

References

1: Fu QH, Zhang Q, Zhang JY, Sun X, Lou Y, Li GG, Chen ZL, Bai XL, Liang TB. LB-100 sensitizes hepatocellular carcinoma cells to the effects of sorafenib during hypoxia by activation of Smad3 phosphorylation. Tumour Biol. 2016 Jun;37(6):7277-86. doi: 10.1007/s13277-015-4560-2. Epub 2015 Dec 14. PubMed PMID: 26666823.

2: Chung V, Mansfield AS, Braiteh F, Richards D, Durivage H, Ungerleider RS, Johnson F, Kovach JS. Safety, Tolerability, and Preliminary Activity of LB-100, an Inhibitor of Protein Phosphatase 2A, in Patients with Relapsed Solid Tumors: An Open-Label, Dose Escalation, First-in-Human, Phase I Trial. Clin Cancer Res. 2016 Dec 30. doi: 10.1158/1078-0432.CCR-16-2299. [Epub ahead of print] PubMed PMID: 28039265.