LSD1-IN-19
LSD1-IN-19 (compound 29) is a potent, non-covalent and selective LSD1 inhibitor, with Ki of 0.108 μM and KD of 0.068 μM, respectively. LSD1-IN-19 shows antiproliferative activity in THP-1 leukemia cells and MDA-MB-231 breast cancer cells, with IC50 (72 h) of 0.17 and 0.40 μM, respectively.
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- CAS. Nr.: 2983011-81-8
- Formel: C33H42N6O2
- Molecular Weight:554.73
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Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biologische Aktivität
Beschreibung
IC50 & Target
|
KDM1/LSD1 |
Cellular Effect
|
Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| HeLa | IC50 |
>100 μM
Compound: 29
|
Inhibition of DOTL1 (unknown origin) using [3H]SAM and HeLa oligo nucleosomes as substrates incubated for 1 hr
Inhibition of DOTL1 (unknown origin) using [3H]SAM and HeLa oligo nucleosomes as substrates incubated for 1 hr
|
[PMID: 35525212] |
| HeLa | IC50 |
100 μM
Compound: 29
|
Inhibition of SETD8 (unknown origin) using [3H]SAM and HeLa nucleosomes as substrates incubated for 1 hr
Inhibition of SETD8 (unknown origin) using [3H]SAM and HeLa nucleosomes as substrates incubated for 1 hr
|
[PMID: 35525212] |
| MDA-MB-231 | IC50 |
0.4 μM
Compound: 29
|
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] |
| RD | IC50 |
0.73 μM
Compound: 29
|
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 |
0.85 μM
Compound: 29
|
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 |
1.23 μM
Compound: 29
|
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 |
0.68 μM
Compound: 29
|
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 |
0.96 μM
Compound: 29
|
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 |
1.24 μM
Compound: 29
|
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 |
0.13 μM
Compound: 29
|
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 |
0.17 μM
Compound: 29
|
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 |
0.27 μM
Compound: 29
|
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. Nr. 2983011-81-8
-
Molecular Weight 554.73
-
Formel C33H42N6O2
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SMILES
COC1=CC2=C(N=C(N=C2NC3CCN(CC3)CC4=CC=CC=C4)NCCCN(C)C)C=C1OCC5=CC=CC=C5
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Protokoll
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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.
Reinheit & Dokumentation
Verweise
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)