CBB3001
CBB3001 is an inhibitor of LSD1/KDM1A. CBB3001 exerts its effect by inhibiting Histone Demethylase activity, with an IC50 of 21.25 μM. It downregulates the expression of pluripotency-related proteins and genes such as SOX2 and OCT4, and induces cell differentiation, growth arrest, and apoptosis. CBB3001 can be used for research on testicular germ cell tumors, teratomas, and embryonal carcinomas.
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- CAS No.: 1639358-50-1
- Formule: C19H27NO5
- Masse moléculaire:349.43
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
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Activité biologique
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Chemical Information
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Help & FAQs
Activité biologique
Description
IC50 & Target
[2]|
KDM1/LSD1 |
SOX2 |
OCT4 |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| PA-1 | IC50 |
20 μM
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Growth inhibition against human ovarian teratocarcinoma PA-1 cells.
Growth inhibition against human ovarian teratocarcinoma PA-1 cells.
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30765888 |
| F9 | IC50 |
20 μM
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Growth inhibition against mouse embryonal carcinoma F9 cells.
Growth inhibition against mouse embryonal carcinoma F9 cells.
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30765888 |
In Vitro
CBB3001 (1-100 μM) potently inhibits the demethylase activity of purified recombinant GST-LSD1 protein in vitro, with an IC50 of 21.25 μM[2].
CBB3001 (20 μM; 16 h) inhibits LSD1 histone demethylase activity in human colorectal cancer HCT116 cells and human ovarian teratocarcinoma PA-1 cells, thereby increasing the levels of monomethylated and dimethylated H3K4, but does not affect the level of trimethylated H3K4[2].
CBB3001 (20-40 μM; 16-30 h) downregulates the expression of the pluripotent stem cell proteins SOX2 and OCT4 in human ovarian teratocarcinoma PA-1 cells and mouse embryonal carcinoma F9 cells[2].
CBB3001 (20 μM; 20 h) reduces EZH2 protein levels in wild-type mouse embryonic fibroblasts[4].
CBB3001 (10 h treatment) reduces the protein levels of mSWI/SNF complex subunits in CAGGCre-ER/LSD1fl/fl mouse embryonic fibroblasts (MEFs) within 10 h[5].
CBB3001 (1-40 μM; 12-30 h) selectively inhibits the growth of human ovarian teratocarcinoma PA-1 cells and mouse embryonal carcinoma F9 cells, but exerts no significant effect on the growth of human colorectal cancer HCT116 cells or mouse fibroblast NIH3T3 cells[2].
CBB3001 (20-40 μM) potently inhibits the growth of human ovarian teratocarcinoma (PA-1) cells and mouse embryonal carcinoma (F9) cells, with an IC50 of approximately 20 μM. It also reduces the expression of pluripotency markers and exerts no effect on non-pluripotent tumor cells[3].
CBB3001, a histone demethylase inhibitor, inhibits cell growth, downregulates pluripotency, and upregulates differentiation in testicular germ cell tumor cell lines[7].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:human colorectal carcinoma HCT116 cells, human ovarian teratocarcinoma PA-1 cells
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Concentration:20 μM
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Incubation Time:16 h
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Result:Increased levels of mono-methylated H3K4 and di-methylated H3K4 in both HCT116 and PA-1 cells.
Left the level of trimethylated H3K4 unchanged in both HCT116 and PA-1 cells.
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Cell Line:human ovarian teratocarcinoma PA-1 cells, human colorectal carcinoma HCT116 cells, mouse embryonic carcinoma F9 cells, mouse fibroblast NIH3T3 cells
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Concentration:1, 5, 10, 20, 40 μM (PA-1 and HCT116 cells); 20, 40 μM (F9 and NIH3T3 cells)
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Incubation Time:16 hours (PA-1 and HCT116 cells); 30 hours (F9 and NIH3T3 cells)
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Result:Potently inhibited the growth of PA-1 cells at concentrations between 5-40 μM, with reduced relative cell percentages observed at each tested concentration.
Did not significantly affect the growth of HCT116 cells even at concentrations up to 40 μM.
Inhibited the growth of F9 cells at 20 and 40 μM.
Had no significant effect on NIH3T3 cell growth at 20 and 40 μM.
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Cell Line:human ovarian teratocarcinoma PA-1 cells, mouse embryonic carcinoma F9 cells
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Concentration:20, 40 μM (PA-1 cells); 40 μM (F9 cells)
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Incubation Time:16 hours (PA-1 cells); 30 hours (F9 cells)
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Result:Downregulated SOX2 and OCT4 protein levels in PA-1 cells compared to control-treated cells.
Downregulated SOX2 and OCT4 protein levels in F9 cells compared to control-treated cells.
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Cell Line:human ovarian teratocarcinoma PA-1 cells
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Concentration:20, 40 μM
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Incubation Time:24 hours initial incubation, followed by 24 hours recovery in fresh medium
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Result:Did not reverse growth inhibitory effects on PA-1 cells after removing the compound and allowing 24 hours of recovery in fresh medium.
Left reduced relative cell percentages remaining similar to levels immediately after treatment.
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Cell Line:wild-type mouse embryonic fibroblasts (MEFs)
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Concentration:20 μM
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Incubation Time:20 h
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Result:Reduced EZH2 protein level significantly.
Left KDM1A protein levels unchanged.
Chemical Information
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CAS No. 1639358-50-1
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Masse moléculaire 349.43
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Formule C19H27NO5
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SMILES
N(C(OC(C)(C)C)=O)[C@H]1[C@@H](C1)C2=CC=C(OC(OC(C)(C)C)=O)C=C2
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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)
CBB3001 Related Classifications
HY-124616 Related Classifications
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