KDM5-C49 (Synonyms: KDOAM-20)

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KDM5-C49 (KDOAM-20) is a potent and selective inhibitor of KDM5 demethylases, with IC₅₀s of 40 nM, 160 nM, and 100 nM for KDM5A, KDM5B, and KDM5C enzymes, respectively. KDM5-C49 can be used for the research of cancer.

For research use only. We do not sell to patients.

KDM5-C49 Chemical Structure

CAS No. : 1596348-16-1

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Other Forms of KDM5-C49:

KDM5-C49 hydrochloride Get quote

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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

Biological Activity
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Target

KDM5

Cellular Effect

Cell Line	Type	Value	Description	References
MCF7	IC₅₀	1 μM Compound: 128	Antiproliferative activity against human MCF7 cells assessed as reduction in cell viability after 120 hrs by ATPlite assay Antiproliferative activity against human MCF7 cells assessed as reduction in cell viability after 120 hrs by ATPlite assay	[PMID: 26710088]
Sf9	IC₅₀	< 0.1 μM Compound: 128	Inhibition of human N-terminal GST-tagged KDM4B (1 to 500 residues) expressed in baculovirus infected sf9 cells using biotinylated histone H3 as substrate preincubated for 10 mins followed by substrate addition measured after 10 mins by AlphaLisa assay Inhibition of human N-terminal GST-tagged KDM4B (1 to 500 residues) expressed in baculovirus infected sf9 cells using biotinylated histone H3 as substrate preincubated for 10 mins followed by substrate addition measured after 10 mins by AlphaLisa assay	[PMID: 26710088]
Sf9	IC₅₀	< 0.1 μM Compound: 128	Inhibition of recombinant human N-terminal FLAG-tagged KDM5C (2 to 1560 residues) expressed in baculovirus infected sf9 cells using biotin-H3K4me3 as substrate preincubated for 10 mins followed by substrate addition measured after 10 mins by AlphaLisa ass Inhibition of recombinant human N-terminal FLAG-tagged KDM5C (2 to 1560 residues) expressed in baculovirus infected sf9 cells using biotin-H3K4me3 as substrate preincubated for 10 mins followed by substrate addition measured after 10 mins by AlphaLisa ass	[PMID: 26710088]
Sf9	IC₅₀	> 1 μM Compound: 128	Inhibition of recombinant KDM3B (842 to 1761 residues) (unknown origin) expressed in baculovirus infected sf9 cells using biotin-H3K9me as substrate preincubated for 10 mins followed by substrate addition measured after 10 mins by AlphaLisa assay Inhibition of recombinant KDM3B (842 to 1761 residues) (unknown origin) expressed in baculovirus infected sf9 cells using biotin-H3K9me as substrate preincubated for 10 mins followed by substrate addition measured after 10 mins by AlphaLisa assay	[PMID: 26710088]
Sf9	IC₅₀	> 1 μM Compound: 128	Inhibition of human C-terminal FLAG-tagged KDM6B (1043 residues) expressed in baculovirus infected sf9 cells using H3K27me3 as substrate preincubated for 10 mins followed by substrate addition measured after 10 mins by AlphaLisa assay Inhibition of human C-terminal FLAG-tagged KDM6B (1043 residues) expressed in baculovirus infected sf9 cells using H3K27me3 as substrate preincubated for 10 mins followed by substrate addition measured after 10 mins by AlphaLisa assay	[PMID: 26710088]
Sf9	IC₅₀	0.1 μM Compound: 128	Inhibition of recombinant human C-terminal FLAG-tagged KDM2B (1 to 650 residues) expressed in baculovirus infected sf9 cells using biotin-H3K36me2 as substrate preincubated for 10 mins followed by substrate addition measured after 10 mins by AlphaLisa ass Inhibition of recombinant human C-terminal FLAG-tagged KDM2B (1 to 650 residues) expressed in baculovirus infected sf9 cells using biotin-H3K36me2 as substrate preincubated for 10 mins followed by substrate addition measured after 10 mins by AlphaLisa ass	[PMID: 26710088]
U2OS	IC₅₀	1 μM Compound: 128	Inhibition of KDM5B in human U2OS cells assessed as reduction in demethylation of H3K4me3 after 20 hrs by Hoechst 33342 staining based immunofluorescence assay Inhibition of KDM5B in human U2OS cells assessed as reduction in demethylation of H3K4me3 after 20 hrs by Hoechst 33342 staining based immunofluorescence assay	[PMID: 26710088]
U2OS	IC₅₀	1 μM Compound: 128	Inhibition of KDM5C in human U2OS cells assessed as reduction in demethylation of H3K4me3 after 20 hrs by Hoechst 33342 staining based immunofluorescence assay Inhibition of KDM5C in human U2OS cells assessed as reduction in demethylation of H3K4me3 after 20 hrs by Hoechst 33342 staining based immunofluorescence assay	[PMID: 26710088]

In Vitro

KDM5-C49 display poor permeability. Convert the carboxylate group of KDM5-C49 into an ethyl ester, to get a cell-permeable prodrug (KDM5-C70)^[2].

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

Molecular Weight

308.38

Formula

C₁₅H₂₄N₄O₃

CAS No.

1596348-16-1

SMILES

O=C(C1=CC=NC(CNCC(N(CC)CCN(C)C)=O)=C1)O

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]. Horton JR, et, al. Structural Basis for KDM5A Histone Lysine Demethylase Inhibition by Diverse Compounds. Cell Chem Biol. 2016 Jul 21;23(7):769-781. [Content Brief]

[2]. Song YQ, et al. The role and prospect of lysine-specific demethylases in cancer chemoresistance. Med Res Rev. 2023 Apr 3. [Content Brief]

KDM5-C49 Related Classifications

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

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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:

KDM5-C491596348-16-1KDOAM-20KDOAM20KDOAM 20Histone DemethylaseInhibitorinhibitorinhibit

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