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Cat. No.: HY-146285

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LSD1-IN-20

LSD1-IN-20 (compound 1) is a potent dual non-covalent LSD1/G9a inhibitor, with K_i 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

Storage:

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

Data Sheet (266 KB)

LSD1-IN-20 Chemical Structure

CAS No.: 1239589-91-3

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Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- IC₅₀ & Target
- Cellular Effect
Chemical Information
Purity & Documentation
References
Calculators
Help & FAQs
Classifications
Bioz

Biological Activity

Description

IC₅₀ & Target

K_i of 0.440 ± 0.05 μM (LSD1), 0.68 ± 0.02 μM (G9a)^[1]

All Histone Demethylase Isoforms :

All Histone Methyltransferase Isoforms :

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

CAS No. 1239589-91-3
Molecular Weight 478.63
Formula C₂₇H₃₈N₆O₂
SMILES

COC1=CC2=C(C(NC3CCN(CC3)CC4=CC=CC=C4)=NC(NCCCN(C)C)=N2)C=C1OC
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

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (266 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[1]. Menna M, et al. Novel non-covalent LSD1 inhibitors endowed with anticancer effects in leukemia and solid tumor cellular models. Eur J Med Chem. 2022 Jul 5;237:114410. [Content Brief]

Calculators

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Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

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Biological Activity
- Description
- IC₅₀ & Target
Chemical Information
Purity & Documentation
References

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LSD1-IN-20

All Histone Demethylase Isoforms

All Histone Methyltransferase Isoforms

Biological Activity

Chemical Information

Purity & Documentation

References

Calculators

Help & FAQs

LSD1-IN-20 Related Classifications

HY-146285 Related Classifications