Viscosalactone B
Viscosalactone B is an orally active LSD1 inhibitor with an IC50 of 970.27 nM. Viscosalactone B targets COX-2, inhibits cyclooxygenase activity, and inhibits p97 ATPase activity in a cysteine-dependent manner. Viscosalactone B can be used in cancer-related research such as prostate cancer, lung cancer, and breast cancer.
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- CAS No.: 76938-46-0
- Formule: C28H40O7
- Masse moléculaire:488.61
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Activité biologique
Description
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LSD1 970.27 nM (IC50) |
COX-2 |
p97 ATPase |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| PC-3 | IC50 |
1.17 μM
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Antiproliferative activity against human PC3 prostate cancer cells assessed as viability reduction incubated 72 hrs by TBT assay.
Antiproliferative activity against human PC3 prostate cancer cells assessed as viability reduction incubated 72 hrs by TBT assay.
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36692618 |
| DU-145 | IC50 |
0.72 μM
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Antiproliferative activity against human DU145 prostate cancer cells assessed as viability reduction incubated 72 hrs by TBT assay.
Antiproliferative activity against human DU145 prostate cancer cells assessed as viability reduction incubated 72 hrs by TBT assay.
|
36692618 |
| NCI-H460 | IC50 |
0.32 μg/mL
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Antiproliferative activity against human NCI-H460 lung tumor cells assessed as viability reduction incubated 48 hrs by MTT assay.
Antiproliferative activity against human NCI-H460 lung tumor cells assessed as viability reduction incubated 48 hrs by MTT assay.
|
14575818 |
| HCT-116 | IC50 |
0.47 μg/mL
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Antiproliferative activity against human HCT-116 colon tumor cells assessed as viability reduction incubated 48 hrs by MTT assay.
Antiproliferative activity against human HCT-116 colon tumor cells assessed as viability reduction incubated 48 hrs by MTT assay.
|
14575818 |
| SF-268 | IC50 |
0.45 μg/mL
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Antiproliferative activity against human SF-268 CNS tumor cells assessed as viability reduction incubated 48 hrs by MTT assay.
Antiproliferative activity against human SF-268 CNS tumor cells assessed as viability reduction incubated 48 hrs by MTT assay.
|
14575818 |
| MCF7 | IC50 |
0.40 μg/mL
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Antiproliferative activity against human MCF-7 breast tumor cells assessed as viability reduction incubated 48 hrs by MTT assay.
Antiproliferative activity against human MCF-7 breast tumor cells assessed as viability reduction incubated 48 hrs by MTT assay.
|
14575818 |
In Vitro
Viscosalactone B (0.25-32 µM; 72 h) inhibits DU145 cell proliferation partly through inhibiting LSD1, with an IC50 of 0.81 µM in DU145&shControl cells and 4.12 µM in DU145&shLSD1 cells[2].
Viscosalactone B (0.3-0.9 µM; 48 h) increases the levels of H3K9me1, H3K9me2, and H3K4me1 in DU145 cells in a concentration-dependent manner[2].
Viscosalactone B (compound 12) (48 h) inhibits the proliferation of NCI-H460, HCT-116, SF-268, and MCF-7 human tumor cell lines, with IC50 values of 0.32, 0.47, 0.45, and 0.40 µg/mL, respectively[4].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:DU145&shLSD1 and DU145&shControl prostate cancer cell lines
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Concentration:0.25, 0.5, 1, 2, 4, 8, 16, 32 µM
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Incubation Time:72 h (TBT assay)
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Result:LSD1 gene expression rates were 9.3% in DU145&shLSD1 cells and 99.7% in DU145&shControl cells.
Inhibited DU145&shControl cells with an IC50 of 0.81 µM and DU145&shLSD1 cells with an IC50 of 4.12 µM, approximately 5-fold less potent in LSD1-knockdown cells.
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Cell Line:DU145 prostate cancer cells
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Concentration:0.3, 0.6, 0.9 µM
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Incubation Time:48 h
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Result:Induced concentration-dependent accumulation of LSD1 substrates H3K9me1, H3K9me2, and H3K4me1 in DU145 cells.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:BALB/c nude (18-25 g)[2]
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Dosage:30 mg/kg
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Administration:intragastric (i.g.); for 21 days
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Result:At 30 mg/kg, DU145 tumor growth was suppressed.
At 30 mg/kg, tumor weight was inhibited in BALB/c nude mice.
Chemical Information
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CAS No. 76938-46-0
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Masse moléculaire 488.61
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Formule C28H40O7
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SMILES
C[C@]12[C@@]3([C@H]([C@H](CC2=O)O)O)[C@](C[C@]4([H])[C@]1([H])CC[C@]5([C@@]4([H])CC[C@]5([H])[C@@H]([C@@]6([H])CC(C)=C(C(O6)=O)CO)C)C)([H])O3
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Structure Classification
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Initial Source
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)