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
- 화학식: C27H38N6O2
- 분자량:478.63
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보관:
Please store the product under the recommended conditions in the Certificate of Analysis.
All Histone Methyltransferase Isoforms
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Biological Activity
Ki of 0.440 ± 0.05 μM (LSD1), 0.68 ± 0.02 μM (G9a)[1]
|
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
-
분자량 478.63
-
화학식 C27H38N6O2
-
SMILES
COC1=CC2=C(C(NC3CCN(CC3)CC4=CC=CC=C4)=NC(NCCCN(C)C)=N2)C=C1OC
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선적
Room temperature in continental US; may vary elsewhere.
-
보관
Please store the product under the recommended conditions in the Certificate of Analysis.
순도&문서
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)