| Field | Specification |
|---|---|
| CAS no. | |
| Applications | |
| Molecular weight | |
| Molecular formula | C13H20N2O4 |
| Purity | |
| SMILES | |
| Form | Solid |
| Storage | |
| Shipping | |
| Catalog no. (Mfr.) | |
| Main SKU |
Compound Overview
LB-100 is a protein phosphatase 2A (PP2A) inhibitor, with IC50 values of 0.85 μM in BxPc-3 cells and 3.87 μM in Panc-1 cells[1][2][3]. It is supplied as a white to off-white solid (C13H20N2O4, MW 268.31) at 99.77% purity.
Physical & Chemical Properties
| CAS Number | 1632032-53-1 |
|---|---|
| Molecular Formula | C13H20N2O4 |
| Molecular Weight | 268.31 g/mol |
| Purity | 99.77% |
| Appearance | Solid |
| Color | White to off-white |
| SMILES | O=C(N(CC1)CCN1C)C2[C@@](CC3)([H])O[C@@]3([H])C2C(O)=O |
| Signaling Pathway | Metabolic Enzyme/Protease |
| Solubility | In Vitro: H2O: ≥ 48 mg/mL (178.90 mM) * "≥" means soluble, but saturation unknown. |
| Storage | Powder: -20°C, 3 years; 4°C, 2 years. In solvent: -80°C, 2 years; -20°C, 1 year. |
| Shipping | Room temperature in continental US; may vary elsewhere. |
Biological Activity
IC50 & Target
IC50: 0.85 μM (PP2 in BxPc-3 cell), 3.87 μM (PP2 in Panc-1 cell)
Literature Cited
Sources cited in this description and in the In Vitro & In Vivo Data tab. Peer-reviewed publications that used this product are listed under References.
Safety
For Research Use Only. Not for use in diagnostic or therapeutic procedures, and not for human or veterinary use. Handle in accordance with the Safety Data Sheet and your institution's chemical hygiene plan.
In Vitro
| Solvent | Solubility | Notes |
|---|---|---|
| H2O | ≥ 48 mg/mL (178.90 mM) | — |
Aliquot the stock solution and store it at -80°C (up to 2 years) or -20°C (up to 1 year); avoid repeated freeze-thaw cycles.
If water is used as the stock solvent, dilute to the working solution and sterilize it through a 0.22 μm filter before use.
Data provided by the manufacturer.
In Vitro
LB-100 inhibits cell growth, with IC50 values of 2.3 μM in BxPc-3 cells and 1.7 μM in Panc-1 cells. PP2A activity falls by 30-50% with LB-100 in BxPc-3, Panc-1, and SW1990 cells. LB-100 raises the intracellular concentration of doxorubicin (2.5 fold versus control) and sensitizes tumor cells to doxorubicin cytotoxicity. LB-100 also increases VEGF secretion and so enhances HIF-1α-VEGF mediated angiogenesis[1]. Endothelial VE-cadherin integrity is altered by LB-100, and pretreatment with LB-100 leads to a nearly 40% rise in dye passing through the HUVECs monolayer. LB-100 raises the paracellular permeability of vascular endothelial cells, which may account for LB-100 raising doxorubicin concentration in tumor cells[2]. Bcl-2 expression is downregulated by LB-100, which also enhances sorafenib-induced apoptosis in HCC cells[3].
In Vivo
In nude mice, LB-100 (2 mg/kg, i.p.) lowers PP2A activity in xenografts and livers in a time-dependent manner. Immunoblotting confirms that LB-100 leaves the expression of the three PP2A subunits (PP2A_A, PP2A_B, and PP2A_C) unchanged in cell lines, xenografts, and livers. Doxorubicin (1.5 kg/mL, every other day) combined with LB-100 (2 mg/kg, every other day) significantly slows tumor growth and reduces tumor volume in two animals, whereas animals given either single agent show no effect on tumor growth[2].
Data provided by the manufacturer. Numbered citations refer to the Literature Cited list in the product description.
Kinase Assay[1]
Treat cultured pancreatic cancer cells with the IC50 of LB-100 for each cell line, or an equal volume of vehicle, for 2 hours. Perform PP2A activity assays with a Ser/Thr phosphatase assay kit. Lyse the cells with an ultrasonic cell disruptor and measure the PP2A concentration with the Ser/Thr phosphatase assay kit according to its instructions. Run the assays for each cell line in triplicate.
Animal Administration[2]
Inject 1×106 Huh-7 cells, suspended in 200 μL PBS per mouse, subcutaneously into the right flank of BALB/c nude mice. Once tumor volume reaches 100 to 200 mm3, randomly allocate the tumor-bearing mice to four groups: control, doxorubicin/cisplatin, LB-100, and doxorubicin/cisplatin plus LB-100. For the doxorubicin plus LB-100 study (n=6 to 8), inject doxorubicin at 1.5 mg/kg and LB-100 at 2 mg/kg i.p. on alternate days for a total of 16 days. In the cisplatin plus LB-100 study (n=8 to 10), inject cisplatin at 3 mg/kg and LB-100 at 2.5 mg/kg, i.p.; give cisplatin every 4 days and LB-100 every other day for 16 days. Inject control mice with DMSO (doxorubicin plus LB-100 study) or PBS (cisplatin plus LB-100 study) on the same schedule as the drug-treated animals. Monitor tumor size every 3 or 4 days and calculate tumor volume as length × width × height/2. Sacrifice all mice at day 16, then collect, weigh, and fix the xenografts with 10% formaldehyde.
Data provided by the manufacturer. Numbered citations refer to the Literature Cited list in the product description.
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Native long-read RNA sequencing of human monocytes reveals activation-induced alternative splicing toward functional isoforms. Nat Commun 2026 May 29. PMID: 42215459
Systematic discovery of mutation-specific synthetic lethals by mining pan-cancer human primary tumor data. Nat Commun 2017 May 31:8:15580.
SARS-CoV-2 membrane protein recruits PP2A to dephosphorylate the nucleocapsid and promote virion production. J Biomed Sci 2026 May 15;33(1):51. PMID: 42141450
Environmental Dose MEOHP Promotes Bladder Cancer Progress through Hybrid EMT Mechanism: Based on the Adverse Outcome Pathway. Environ Sci Technol 2026 Mar 3;60(8):5979-5990. PMID: 41650175
Synaptotagmin 1-mediated cell membrane penetration and dopamine release enhancement by latroeggtoxin-VI. Int J Biol Macromol 2022 Sep 1:216:906-915. PMID: 35914553
The Antitumor Drug LB-100 Is a Catalytic Inhibitor of Protein Phosphatase 2A (PPP2CA) and 5 (PPP5C) Coordinating with the Active-Site Catalytic Metals in PPP5C. Mol Cancer Ther 2019 Mar;18(3):556-566.
Phosphatase inhibition by LB-100 enhances BMN-111 stimulation of bone growth. JCI Insight 2021 May 10;6(9):e141426. PMID: 33986191
Nuclear translocation of ISG15 regulated by PPP2R2B inhibits cisplatin resistance of bladder cancer. Cell Mol Life Sci 2024 Jul 8;81(1):292. PMID: 38976080
Phosphatase PP2A promotes RTA dephosphorylation to impair KSHV lytic replication. PLoS Pathog 2025 Dec 3;21(12):e1013731. PMID: 41337097
Synergistic Efficacy of Chidamide and LB100 in Sézary Syndrome via TNC Downregulation and PI3K/AKT/mTOR Dephosphorylation. Cancer Sci 2025 Sep 3. PMID: 40903394
