1. Epigenetics
  2. Histone Demethylase
  3. 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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LSD1-IN-19

LSD1-IN-19 Chemical Structure

CAS No. : 2983011-81-8

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Description

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[1].

IC50 & Target

KDM1/LSD1

 

Cellular Effect
Cell Line Type Value Description References
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]
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]
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]
Molecular Weight

554.73

Formula

C33H42N6O2

CAS No.
SMILES

COC1=CC2=C(N=C(N=C2NC3CCN(CC3)CC4=CC=CC=C4)NCCCN(C)C)C=C1OCC5=CC=CC=C5

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation
References
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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Product Name:
LSD1-IN-19
Cat. No.:
HY-146284
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