LB-100
LB-100 is an inhibitor of protein phosphatase 2A (PP2A) with anticancer activity, with IC50 of 0.85 μM and 3.87 μM in BxPc-3 and Panc-1 cells, respectively[1].
In BxPc-3, Panc-1, and SW1990 cells, LB-100 treatment reduced PP2A activity by 30-50%. LB-100 increases the intracellular doxorubicin concentration (about 2.5 times that of the control group) and makes tumor cells more sensitive to the cytotoxicity of doxorubicin[1].
In a PANC-1 mouse xenograft model, LB-100 (2 mg / kg, intraperitoneal injection) improves the efficacy of the chemotherapy drug doxorubicin. LB-100 increases tumor microvessel density and blood flow velocity on the tumor surface, and decreases tumor volume[1].
Reference:
[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, 2014, 355(2): 281-287.
- 1. Yuan Fu, Xiaofan Jia, et al. "Fam72a functions as a cell-cycle-controlled gene during proliferation and antagonizes apoptosis through reprogramming PP2A substrates." Dev Cell. 2023 Mar 13;58(5):398-415.e7. PMID: 36868233
- 2. Gulisudumu Maitiabula, Feng Tian, et al. " Liver PP2A-Cα protects from parenteral nutrition-associated hepatic steatosis." Cell Mol Gastroenterol Hepatol. 2022 May 26;S2352-345X(22)00090-X. PMID: 35643235
| Physical Appearance | A solid |
| Storage | Store at -20°C |
| M.Wt | 268.31 |
| Cas No. | 1632032-53-1 |
| Formula | C13H20N2O4 |
| Solubility | ≥26.8 mg/mL in H2O; insoluble in EtOH; insoluble in DMSO |
| Chemical Name | 3-(4-methylpiperazine-1-carbonyl)-7-oxabicyclo[2.2.1]heptane-2-carboxylic acid |
| SDF | Download SDF |
| Canonical SMILES | CN1CCN(C(C(C2CCC3O2)C3C(O)=O)=O)CC1 |
| Shipping Condition | Small Molecules with Blue Ice, Modified Nucleotides with Dry Ice. |
| General tips | We do not recommend long-term storage for the solution, please use it up soon. |
| Cell experiment:[1] | |
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Cell lines |
Pancreatic cancer cell lines BxPc-3 and Panc-1 |
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Reaction Conditions |
0.85 and 3.87 μM LB-100 |
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Applications |
LB-100 showed dose-dependent inhibition of cell growth in both cell lines. The IC50 of LB-100 was 0.85 μM and 3.87 μM in BxPc-3 and Panc-1, respectively. While the IC50 of doxorubicin was 2.3 μM and 1.7 μM in BxPc-3 and Panc-1, respectively, LB-100 did not synergize with doxorubicin in both cell lines. |
| Animal experiment:[1] | |
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Animal models |
BALB/c nude mice bearing Panc-1 xenografts |
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Dosage form |
2 mg/kg Injected intraperitoneally (i.p.) on alternate days for a total of 16 days |
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Applications |
LB-100 synergistically enhanced the activity of doxorubicin in vivo. This effect was associated with increased microvessel density, blood perfusion, and doxorubicin concentrations within the xenografts. |
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Note |
The technical data provided above is for reference only. |
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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 Letters, 2014, 355(2): 281-287. |
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