LSD1-IN-20

Cat. No.: HY-146285: FAQs
Data Sheet Handling Instructions Technical Support

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.

LSD1-IN-20 Chemical Structure

CAS No. : 1239589-91-3

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•Related Small Molecules:

•Related Proteins:

View All Histone Demethylase Isoform Specific Products:

View All Isoforms

KDM1/LSD1 KDM2 KDM3 KDM4 KDM5 KDM6 KDM7

View All Histone Methyltransferase Isoform Specific Products:

View All Isoforms

EZH1 EZH2 DOT1L SMYD2 SMYD3 SUV39H2/KMT1B EHMT2/G9a/KMT1C EHMT1/GLP/KMT1D SETDB1/KMT2G SETD2/KMT3A NSD2/MMSET/WHSC1 SETD7/KMT7 SETD8/KMT5A PRMT1 PRMT3 PRMT4 PRMT5 PRMT6 PRMT7 PRMT8

Biological Activity
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Target

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

Cellular Effect

Cell Line	Type	Value	Description	References
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]
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]

Molecular Weight

478.63

Formula

C₂₇H₃₈N₆O₂

CAS No.

1239589-91-3

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

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]

LSD1-IN-20 Related Classifications

Molarity Calculator
Dilution Calculator

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass		Concentration		Volume		Molecular Weight *
	=		×		×

The dilution calculator equation

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)	×	Volume _(start)	=	Concentration _(final)	×	Volume _(final)
	×		=		×
C1		V1		C2		V2

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-201239589-91-3Histone DemethylaseHistone MethyltransferaseTHP-1 cellsMV4-11 cellsMDA-MB-231 cellsbreast cancerMDA-MB-231TNBC cell lineLysine-specific demethylase 1 (LSD1)histone methyltransferase histone demethylaseInhibitorinhibitorinhibit

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