LB-100

• CAT Number: I002117
• CAS Number: 1632032-53-1
• Molecular Formula: C13H20N2O4
• Molecular Weight: 268.313
• Purity: ≥95%
• Target: PP2A inhibitor
• Solubility: 10 mM in H2O, DMSO: ＜ 2.9 mg/mL
• Storage: Desiccate at +4C
• IUPAC Name: (1S,4R)-2-(4-methylpiperazine-1-carbonyl)-7-oxabicyclo[2.2.1]heptane-3-carboxylic acid
• InChI: InChI=1S/C13H20N2O4/c1-14-4-6-15(7-5-14)12(16)10-8-2-3-9(19-8)11(10)13(17)18/h8-11H,2-7H2,1H3,(H,17,18)/t8-,9+,10?,11?/m0/s1
• InChIKey: JUQMLSGOTNKJKI-IZUQBHJASA-N
• SMILES: CN1CCN(CC1)C(=O)C2C3CCC(C2C(=O)O)O3

LB-100(CAT: I002117) is a small-molecule inhibitor of protein phosphatase 2A (PP2A). PP2A is a key enzyme involved in the regulation of cell signaling and plays a critical role in various cellular processes, including cell cycle control, cell growth, and apoptosis. By inhibiting PP2A, LB-100 modulates the activity of downstream signaling pathways and can potentially impact cellular processes and signaling cascades. LB-100 has shown promise in preclinical studies as a potential anticancer agent, and its inhibitory activity against PP2A makes it a valuable tool for studying PP2A-related cellular functions and signaling pathways.

Reference

1: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. Chung V, Mansfield AS, Braiteh F, Richards D, Durivage H, Ungerleider RS, Johnson F, Kovach JS.Clin Cancer Res. 2016 Dec 30. doi: 10.1158/1078-0432.CCR-16-2299. [Epub ahead of print] PMID: 28039265 2:LB-100 sensitizes hepatocellular carcinoma cells to the effects of sorafenib during hypoxia by activation of Smad3 phosphorylation. Fu QH, Zhang Q, Zhang JY, Sun X, Lou Y, Li GG, Chen ZL, Bai XL, Liang TB.Tumour Biol. 2016 Jun;37(6):7277-86. doi: 10.1007/s13277-015-4560-2. Epub 2015 Dec 14. PMID: 26666823