2. Epigenetics Apoptosis
  3. Histone Demethylase Apoptosis
  4. LSD1-IN-25

LSD1-IN-25 (Compound 9j) is a potent, selective and orally active LSD1 inhibitor with an IC50 of 46 nM (Ki = 30.3 nM). LSD1-IN-25 induces cancer cell apoptosis.

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LSD1-IN-25 Chemical Structure

LSD1-IN-25 Chemical Structure

CAS No. : 2911585-60-7

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LSD1-IN-25 Related Antibodies

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Description

LSD1-IN-25 (Compound 9j) is a potent, selective and orally active LSD1 inhibitor with an IC50 of 46 nM (Ki = 30.3 nM). LSD1-IN-25 induces cancer cell apoptosis[1].

IC50 & Target[1]

LSD1

46 nM (IC50)

LSD1

30.3 nM (Ki)

In Vitro

LSD1-IN-25 (Compound 9j; 0-20 μM; 72 h) inhibits solid tumor cell proliferation[1].
LSD1-IN-25 (1-4 μM; 24 h) induces the elevation of cellular H3K4me2 and inhibits the EMT process of H1650 cells[1].
LSD1-IN-25 (1-4 μM; 24 h) induces apoptosis and S arrest in H1650 cells[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

LSD1-IN-25 Related Antibodies

Cell Proliferation Assay[1]

Cell Line: MGC-803, MGC-803LSD1-KO, SGC-7901, GES-1, MCF-7, H1650, A549, H460, PC-3 and EC-109
Concentration: 0-20 μM
Incubation Time: 72 h
Result: Antiproliferative activity of LSD1-IN-25 (Compound 9j) on solid tumor cell lines[1]
Cell line Origin IC50 (μM)
MGC-803 Gastric cancer 5.1 ± 0.7
MGC-803LSD1-KO Gastric cancer >20
SGC-7901 Gastric cancer 9.5 ± 2.1
GES-1 Normal gastric epithelial cell >20
MCF-7 Breast cancer 13.4 ± 2.4
H1650 Lung cancer 4.3 ± 0.9
A549 Lung cancer 7.9 ± 1.5
H460 Lung cancer 13.6 ± 4.2
PC-3 Prostate cancer 7.5 ± 1.1
EC-109 Esophageal cancer 15.2 ± 2.9

Western Blot Analysis[1]

Cell Line: H1650 cell
Concentration: 1, 2 and 4 μM
Incubation Time: 24 h
Result: Induced the elevation of cellular H3K4me2. Elevated the expression of the epithelial marker E-cadherin, decreased the expression of the mesenchymal markers such as N-cadherin, slug and vimentin.

Apoptosis Analysis[1]

Cell Line: H1650 cell
Concentration: 1, 2 and 4 μM
Incubation Time: 24 h
Result: Induced an evident increase in cell apoptosis, with the percentage of apoptotic cells of 43.9% (1 μM), 44.5% (2 μM) and 45.7% (4 μM), respectively, in comparison with 12.7% of the control.

Cell Cycle Analysis[1]

Cell Line: H1650 cell
Concentration: 1, 2 and 4 μM
Incubation Time: 24 h
Result: The percentage of cells in S phase were 29.97% 33.32%, 39.81%, 43.26% at concentrations of 0, 1 μM, 2 μM, 4 μM, respectively.
In Vivo

LSD1-IN-25 (Compound 9j; 10 and 20 mg/kg; oral; once daily for 21 days) shows antitumor activity in a mouse xenograft model of H1650 cells[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Nude mice, xenograft model of H1650 cells[1]
Dosage: 10 mg/kg and 20 mg/kg
Administration: Oral, once daily for 21 days
Result: Presented a remarkable reduction of average tumor weight by 41.5% and 64.0% at dosages of 10 and 20 mg/kg, respectively. Evidently prolonged the mice's survival.
Molecular Weight

617.16

Formula

C32H33ClN6O3S
CAS No.
SMILES

ClC1=CC=CC(CN2C(N=C(SCCC)N=C3OC4=C(OC)C=C(CN[C@H]5C[C@@H]5C6=CC=CC=C6)C=C4OC)=C3N=N2)=C1
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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LSD1-IN-25 Related Classifications

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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.

Keywords:

LSD1-IN-252911585-60-7Histone DemethylaseApoptosisH3K4me2EMTH1650MGC-803SGC-7901GES-1MCF-7A549H460PC-3EC-109Inhibitorinhibitorinhibit

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