LSD1-IN-20
LSD1-IN-20 (compound 1) is a potent dual non-covalent LSD1/G9a inhibitor, with Ki values of 0.44 and 0.68 μM, respectively. LSD1-IN-20 shows antiproliferative activity in THP-1 leukemia cells and MDA-MB-231 breast cancer cells, with IC50 (72 h) of 0.51 and 1.60 μM, respectively.
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- CAS No.: 1239589-91-3
- Formule: C27H38N6O2
- Masse moléculaire:478.63
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
Ki of 0.440 ± 0.05 μM (LSD1), 0.68 ± 0.02 μM (G9a)[1]
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Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| HEK293 | IC50 |
0.778 μM
Compound: 10
|
Inhibition of human G9a expressed in HEK293 cells
Inhibition of human G9a expressed in HEK293 cells
|
[PMID: 38401457] |
| MDA-MB-231 | IC50 |
1.6 μM
Compound: 1; MC3774
|
Antiproliferative activity against human MDA-MB-231 cells assessed as inhibition of cell growth measured after 72 hrs by MTT assay
Antiproliferative activity against human MDA-MB-231 cells assessed as inhibition of cell growth measured after 72 hrs by MTT assay
|
[PMID: 35525212] |
| MV4-11 | IC50 |
0.89 μM
Compound: 10
|
Antiproliferative activity against human MV4-11 cells assessed as reduction in cell viability measured after 48 hrs by CellTiter-Glo assay
Antiproliferative activity against human MV4-11 cells assessed as reduction in cell viability measured after 48 hrs by CellTiter-Glo assay
|
[PMID: 38401457] |
| MV4-11 | IC50 |
0.89 μM
Compound: 39; E11
|
Antiproliferative activity against human MV4-11 cells
Antiproliferative activity against human MV4-11 cells
|
[PMID: 34107385] |
| RD | IC50 |
2.82 μM
Compound: 1; MC3774
|
Antiproliferative activity against human RD cells assessed as inhibition of cell growth incubated for 144 hrs
Antiproliferative activity against human RD cells assessed as inhibition of cell growth incubated for 144 hrs
|
[PMID: 35525212] |
| RD | IC50 |
3.36 μM
Compound: 1; MC3774
|
Antiproliferative activity against human RD cells assessed as inhibition of cell growth incubated for 72 hrs
Antiproliferative activity against human RD cells assessed as inhibition of cell growth incubated for 72 hrs
|
[PMID: 35525212] |
| RD | IC50 |
6.4 μM
Compound: 1; MC3774
|
Antiproliferative activity against human RD cells assessed as inhibition of cell growth incubated for 24 hrs
Antiproliferative activity against human RD cells assessed as inhibition of cell growth incubated for 24 hrs
|
[PMID: 35525212] |
| SJRH30 | IC50 |
2.57 μM
Compound: 1; MC3774
|
Antiproliferative activity against human Rh30 cells assessed as inhibition of cell growth incubated for 144 hrs
Antiproliferative activity against human Rh30 cells assessed as inhibition of cell growth incubated for 144 hrs
|
[PMID: 35525212] |
| SJRH30 | IC50 |
2.92 μM
Compound: 1; MC3774
|
Antiproliferative activity against human Rh30 cells assessed as inhibition of cell growth incubated for 72 hrs
Antiproliferative activity against human Rh30 cells assessed as inhibition of cell growth incubated for 72 hrs
|
[PMID: 35525212] |
| SJRH30 | IC50 |
4.33 μM
Compound: 1; MC3774
|
Antiproliferative activity against human Rh30 cells assessed as inhibition of cell growth incubated for 24 hrs
Antiproliferative activity against human Rh30 cells assessed as inhibition of cell growth incubated for 24 hrs
|
[PMID: 35525212] |
| THP-1 | IC50 |
0.38 μM
Compound: 1; MC3774
|
Antiproliferative activity against human THP-1 cells assessed as inhibition of cell growth incubated for 144 hrs by CellTiter-Glo luminescent cell viability assay
Antiproliferative activity against human THP-1 cells assessed as inhibition of cell growth incubated for 144 hrs by CellTiter-Glo luminescent cell viability assay
|
[PMID: 35525212] |
| THP-1 | IC50 |
0.51 μM
Compound: 1; MC3774
|
Antiproliferative activity against human THP-1 cells assessed as inhibition of cell growth incubated for 72 hrs by CellTiter-Glo luminescent cell viability assay
Antiproliferative activity against human THP-1 cells assessed as inhibition of cell growth incubated for 72 hrs by CellTiter-Glo luminescent cell viability assay
|
[PMID: 35525212] |
| THP-1 | IC50 |
0.69 μM
Compound: 1; MC3774
|
Antiproliferative activity against human THP-1 cells assessed as inhibition of cell growth incubated for 24 hrs by CellTiter-Glo luminescent cell viability assay
Antiproliferative activity against human THP-1 cells assessed as inhibition of cell growth incubated for 24 hrs by CellTiter-Glo luminescent cell viability assay
|
[PMID: 35525212] |
Chemical Information
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CAS No. 1239589-91-3
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Masse moléculaire 478.63
-
Formule C27H38N6O2
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SMILES
COC1=CC2=C(C(NC3CCN(CC3)CC4=CC=CC=C4)=NC(NCCCN(C)C)=N2)C=C1OC
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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)