A PP2A inhibitor with anticancer activity
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LB-100

Item No. 29105

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
(1R,4S)-rel-3-[(4-methyl-1-piperazinyl)carbonyl]-7-oxabicyclo[2.2.1]heptane-2-carboxylic acid
CAS Number
1632032-53-1
Molecular Formula
C13H20N2O4
Formula Weight
268.3
Purity
≥98%
Formulation
A crystalline solid
Solubility(Learn about Variance in Solubility)
Ethanol: Partially solublePBS (pH 7.2): 10 mg/ml
SMILES
CN1CCN(C(C2C(C(O)=O)[C@H]3CC[C@@H]2O3)=O)CC1
InChi Code
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
InChi Key
JUQMLSGOTNKJKI-IZUQBHJASA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    5 mg

    $134

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    10 mg

    $240

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    25 mg

    $530

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    50 mg

    $926

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    Cayman Chemical
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    Product Description

    LB-100 is an inhibitor of protein phosphatase 2A (PP2A) with anticancer activity.1 It reduces PP2A activity and is cytotoxic to BxPC-3 and PANC-1 cells (IC50s = 0.85 and 3.87 μM, respectively). LB-100 inhibits radiation-induced Rad51 focus formation and homologous recombination repair in PANC-1 and MiaPaCa-2 cells.2 In vivo, it increases tumor microvessel density and VEGF secretion and decreases tumor volume in a PANC-1 mouse xenograft model when administered at a dose of 2 mg/kg.1 LB-100 (1.5 mg/kg) enhances radiation-induced reductions in tumor volume in CNE1 and CNE2 radioresistant nasopharyngeal carcinoma mouse xenograft models.3

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Bai, X., Zhi, X., Zhang, Q., et al. Inhibition of protein phosphatase 2A sensitizes pancreatic cancer to chemotherapy by increasing drug perfusion via HIF-1α-VEGF mediated angiogenesis. Cancer Lett. 355(2), 281-287 (2014).

    2. Wei, D., Parsels, L.A., Karnak, D., et al. Inhibition of protein phosphatase 2A radiosensitizes pancreatic cancers by modulating CDC25C/CDK1 and homologous recombination repair. Clin. Cancer Res. 19(16), 4422-4432 (2013).

    3. Hong, C.S., Ho, W., Zhang, C., et al. LB100, a small molecule inhibitor of PP2A with potent chemo- and radio-sensitizing potential. Cancer Biol. Ther. 16(6), 821-833 (2015).