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 番号: 2983011-81-8
- 分子式: C33H42N6O2
- 分子量:554.73
-
保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
生物活性
|
KDM1/LSD1 |
|
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] |
化学情報
-
CAS 番号 2983011-81-8
-
分子量 554.73
-
分子式 C33H42N6O2
-
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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輸送条件
Room temperature in continental US; may vary elsewhere.
-
保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
純度とドキュメンテーション
参考文献
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)