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.
For research use only. We do not sell to patients.
- CAS No.: 1239589-91-3
- Formula: C27H38N6O2
- Molecular Weight:478.63
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
All Histone Methyltransferase Isoforms
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Biological Activity
Description
IC50 & Target
Ki of 0.440 ± 0.05 μM (LSD1), 0.68 ± 0.02 μM (G9a)[1]
Cellular Effect
|
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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Molecular Weight 478.63
-
Formula 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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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Protocols
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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
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Breast Cancer Modeling
Breast cancer is a heterogeneous cancer, and it has been distinguished into four subtypes: luminal A, luminal B, HER2-positive and basal-like. Molecular mutations, epigenetic alterations, hormone exposure and immune microenvironment are related to the progression of breast cancer.
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Cell Viability Determination by MTT Colorimetric Assay
The following protocol uses the MTT colorimetric assay as a classic literature-established method for assessing cell viability/metabolic activity in cultured mammalian cells. MTT[3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide] is reduced by metabolically active cells to a colored formazan product; the amount of formazan is quantified spectrophotometrically and provides an indirect measure of metabolically active viable cells. Importantly, MTT reduction reflects cellular oxidoreductase/metabolic activity rather than an absolute direct count of living cells, so changes in cellular metabolism can alter the signal independently of cell number.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)