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KDOAM-25 trihydrochloride (2230731-99-2 free base)

Catalog No. T11750L CAS T11750L

Synonyms: KDOAM-25 trihydrochloride

KDOAM-25 trihydrochloride increases global H3K4 methylation at transcriptional start sites and impairs proliferation in multiple myeloma MM1S cells. KDOAM-25 trihydrochloride is a potent and highly selective histone lysine demethylases 5 (KDM5) inhibitor with IC50s of 71 nM, 19 nM, 69 nM, 69 nM for KDM5A, KDM5B, KDM5C, KDM5D, respectively.

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KDOAM-25 trihydrochloride (2230731-99-2 free base) Chemical Structure

KDOAM-25 trihydrochloride (2230731-99-2 free base), CAS T11750L

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Description	KDOAM-25 trihydrochloride increases global H3K4 methylation at transcriptional start sites and impairs proliferation in multiple myeloma MM1S cells. KDOAM-25 trihydrochloride is a potent and highly selective histone lysine demethylases 5 (KDM5) inhibitor with IC50s of 71 nM, 19 nM, 69 nM, 69 nM for KDM5A, KDM5B, KDM5C, KDM5D, respectively.
Targets&IC50	KDM5A:71 nM , KDM5D:69 nM , KDM5B:19 nM , KDM5C:69 nM
In vitro	KDOAM-25 trihydrochloride is able to reduce the viability of MM1S cells with an IC50 of ～30 μM after a delay of 5-7 days. KDOAM-25 trihydrochloride treatment results in a G1 cell-cycle arrest with an increased proportion of MM1S in G1 and a decrease of the proportion of cells in G2 without an increase in the proportion of cells in the apoptotic sub-G1 phase. KDOAM-25 trihydrochloride (50 μM) increases with approximately twice as much H3K4me3 in in multiple myeloma cells. KDOAM-25 trihydrochloride inhibits most potently KDM5B with an IC50 of ～50 μM and the other KDM5 family members at concentrations above 100 μM. KDOAM-25 trihydrochloride shows no cellular activity on any of the other tested JmjC family members.

Synonyms	KDOAM-25 trihydrochloride
Molecular Weight	416.77
Formula	C15H28Cl3N5O2
CAS No.	T11750L

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

References and Literature

1. Tumber A, et al. Potent and Selective KDM5 Inhibitor Stops Cellular Demethylation of H3K4me3 at Transcription Start Sites and Proliferation of MM1S Myeloma Cells. Cell Chem Biol. 2017 Mar 16;24(3):371-380.

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Keywords

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