Structure of LB-100
CAS No.: 1632032-53-1
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The BI-3802 was designed by Boehringer Ingelheim and could be obtained free of charge through the Boehringer Ingelheim open innovation portal opnMe.com, associated with its negative control.
LB-100 is a small-molecular protein phosphatase 2A (PP2A) inhibitor with IC50 of 0.85 μM and 3.87 μM in BxPc-3 and Panc-1 cells.
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Batch number can be found on the product's label following the word 'Batch'.
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Batch number can be found on the product's label following the word 'Batch'.
Search for reports by entering the product batch number.
Batch number can be found on the product's label following the word 'Batch'.
Search for reports by entering the product batch number.
Batch number can be found on the product's label following the word 'Batch'.
Search for reports by entering the product batch number.
Batch number can be found on the product's label following the word 'Batch'.
CAS No. : | 1632032-53-1 |
Formula : | C13H20N2O4 |
M.W : | 268.31 |
SMILES Code : | OC(C1C(C(N2CCN(C)CC2)=O)[C@]3([H])CC[C@]1(O3)[H])=O |
MDL No. : | MFCD28167839 |
GHS Pictogram: |
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Signal Word: | Warning |
Hazard Statements: | H302-H315-H319-H335 |
Precautionary Statements: | P261-P305+P351+P338 |
Description |
LB-100, acting as an inhibitor of protein phosphatase 2A (PP2A), shows IC50 values of 0.85 μM and 3.87 μM in BxPc-3 and Panc-1 cells, respectively, indicating its potent inhibitory action[1].[2].[3].
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In Vitro:
Cell Line
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Concentration | Treated Time | Description | References |
OT-1 CD8+ T cells | 2 μM | 4 hours | LB-100 enhances antigen-specific CTL cytotoxicity. | PMC5974350 |
CD4+ T cells | 1 μM | 5 days | LB-100 promotes CD4+ T cell proliferation and Th1 differentiation. | PMC5974350 |
GBMNS (Glioblastoma Neurospheres) | 5 µM | 24 hours | LB100 enhanced G1 cell cycle arrest induced by PRMT5 depletion and increased the anti-GBM effect through necroptotic cell killing. | PMC8408848 |
MiaPaCa-2 cells | 1 or 3 μmol/L | 2 hours pre- and 24 hours post-IR | LB100 treatment resulted in significant radiosensitization, with RERs ranging from 1.2 to 1.4. | PMC3754450 |
Panc-1 cells | 1 or 3 μmol/L | 2 hours pre- and 24 hours post-IR | LB100 treatment resulted in significant radiosensitization, with RERs ranging from 1.2 to 1.4. | PMC3754450 |
U-CH1 | 0–20 µM | 24, 48, 72 hours | To evaluate the effect of LB100 on chordoma cell proliferation, results showed that LB100 alone had a limited effect on cell proliferation, but in combination with radiation, it significantly inhibited cell proliferation. | PMC5961117 |
CCL-241 cells | 1 or 3 μmol/L | LB100 treatment produced little to no radiosensitization in normal cells. | PMC3754450 | |
UM-Chor1 | 0–20 µM | 24, 48, 72 hours | To evaluate the effect of LB100 on chordoma cell proliferation, results showed that LB100 alone had a limited effect on cell proliferation, but in combination with radiation, it significantly inhibited cell proliferation. | PMC5961117 |
JHC7 | 0–20 µM | 24, 48, 72 hours | To evaluate the effect of LB100 on chordoma cell proliferation, results showed that LB100 alone had a limited effect on cell proliferation, but in combination with radiation, it significantly inhibited cell proliferation. | PMC5961117 |
HCC cells | 10 μM | LB-100 significantly decreased PP2Ac activity in high PDCD10 expressing cells | PMC8440642 | |
IOμM-LEE cells | 2.5 µM | 4 hours | LB-100 enhanced the radiosensitivity of meningioma cells and reduced survival fraction in clonogenic assays. | PMC5748254 |
GAR cells | 2.5 µM | 4 hours | LB-100 enhanced the radiosensitivity of meningioma cells and reduced survival fraction in clonogenic assays. | PMC5748254 |
CH-157 cells | 2.5 µM | 4 hours | LB-100 enhanced the radiosensitivity of meningioma cells and reduced survival fraction in clonogenic assays. | PMC5748254 |
In Vivo:
Species
|
Animal Model
|
Administration | Dosage | Frequency | Description | References |
Mice | CT26 colon cancer model | Intraperitoneal injection | 2 mg/kg | Once daily for 2 weeks | LB-100 combined with aPD-1 significantly inhibits tumor growth and prolongs survival in the CT26 model. | PMC5974350 |
Mice | Intracranial GBM mouse model | Intraperitoneal injection | 10 mg/kg | Once daily for 4 days | Combination treatment of LB100 with PRMT5 depletion significantly reduced tumor size and prolonged survival in mice, while LB100 treatment alone had no survival benefit. | PMC8408848 |
mice | Ube3am−/p+ mice model | intraperitoneal injection | 0.16 mg/kg | Every 2 days for 30 days | LB-100 significantly ameliorated the deficits in motor coordination and learning in Ube3am?/p+ mice, and restored the deficits in excitatory synaptic transmission and dendritic spine morphology | PMC6589679 |
nude mice | MiaPaCa-2 xenograft model | I.P. | 1.5 mg/kg | Every other day, until the end of the study | LB100 alone significantly delayed tumor growth, and when combined with radiation, the time required for tumor volume doubling was significantly extended. | PMC3754450 |
NSG mice | Subcutaneous xenograft model | Intraperitoneal injection | 1 mg/kg | every 2 days starting at P14 and continuing until P30 | To evaluate the effect of LB100 in combination with radiation on chordoma xenograft growth, results showed that the combination treatment significantly delayed tumor growth. | PMC5961117 |
BALB/c nude mice | Orthotopic tumor model | Intraperitoneal injection | 1.5 mg/kg | once a day, 5 days a week for 2 weeks | LB-100 significantly inhibited tumor growth and lung metastasis of orthotopic tumors derived from HCC cells with high PDCD10 expression | PMC8440642 |
BALB/c nude mice | Intracranial orthotopic meningioma mouse model | Intraperitoneal injection | 1 mg/kg | Twice daily for 3 days | The combined treatment of LB-100 and radiation significantly prolonged the survival of mice with xenografts. | PMC5748254 |
Clinical Trial:
NCT Number | Conditions | Phases | Recruitment | Completion Date | Locations |
NCT03886662 | Myelodysplastic Syndromes | PHASE1|PHASE2 | RECRUITING | 2025-07-21 | H. Lee Moffitt Cancer Center &... More >> Research Institute, Tampa, Florida, 33612, United States Less << |
NCT03027388 | Astrocytoma, Grades II, III an... More >>d IV|Glioblastoma Multiforme|Giant Cell Glioblastoma|Glioma|Oligodendrogliomas Less << | PHASE2 | COMPLETED | 2022-08-31 | National Institutes of Health ... More >>Clinical Center, Bethesda, Maryland, 20892, United States Less << |
Bio Calculators | ||||
Preparing Stock Solutions | ![]() |
1mg | 5mg | 10mg |
1 mM 5 mM 10 mM |
3.73mL 0.75mL 0.37mL |
18.64mL 3.73mL 1.86mL |
37.27mL 7.45mL 3.73mL |
Tags: LB-100 | LB100 | LB 100 | Phosphatase | PP2A inhibitor | protein phosphatase 2A | PP2A inhibition | cell growth regulation | apoptosis | 1632032-53-1
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P301 + P312 | IF SWALLOWED: call a POISON CENTER or doctor/physician IF you feel unwell. |
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P302 + P334 | IF ON SKIN: Immerse in cool water/wrap in wet bandages. |
P302 + P350 | IF ON SKIN: Gently wash with plenty of soap and water. |
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P304 + P340 | IF INHALED: Remove victim to fresh air and Keep at rest in a position comfortable for breathing. |
P304 + P341 | IF INHALED: If breathing is difficult, remove victim to fresh air and keep at rest in a position comfortable for breathing. |
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P332 + P313 | IF SKIN irritation occurs: Get medical advice/attention. |
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P337 + P313 | IF eye irritation persists: Get medical advice/attention. |
P342 + P311 | IF experiencing respiratory symptoms: call a POISON CENTER or doctor/physician. |
P370 + P376 | In case of fire: Stop leak if safe to Do so. |
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P410 + P412 | Protect from sunlight. Do not expose to temperatures exceeding 50 oC/122oF. |
P411 + P235 | Keep cool. |
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H242 | Heating may cause a fire |
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H335 | May cause respiratory irritation |
H336 | May cause drowsiness or dizziness |
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H373 | May cause damage to organs through prolonged or repeated exposure |
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H411 | Toxic to aquatic life with long-lasting effects |
H412 | Harmful to aquatic life with long-lasting effects |
H413 | May cause long-lasting harmful effects to aquatic life |
H420 | Harms public health and the environment by destroying ozone in the upper atmosphere |
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