1. Epigenetics
  2. Histone Demethylase
  3. KDOAM-25 trihydrochloride

KDOAM-25 trihydrochloride 

Cat. No.: HY-102047A
Handling Instructions

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. KDOAM-25 trihydrochloride increases global H3K4 methylation at transcriptional start sites and impairs proliferation in multiple myeloma MM1S cells.

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

KDOAM-25 trihydrochloride Chemical Structure

KDOAM-25 trihydrochloride Chemical Structure

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Description

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. KDOAM-25 trihydrochloride increases global H3K4 methylation at transcriptional start sites and impairs proliferation in multiple myeloma MM1S cells[1].

IC50 & Target

IC50: 71 nM (KDM5A), 19 nM (KDM5B), 69 nM (KDM5C), 69 nM (KDM5D)[1]

In Vitro

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[1].
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[1].
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[1].
KDOAM-25 trihydrochloride (50 μM) increases with approximately twice as much H3K4me3 in in multiple myeloma cells[1].

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

Molecular Weight

416.77

Formula

C₁₅H₂₈Cl₃N₅O₂

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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

References
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KDOAM-25 trihydrochloride
Cat. No.:
HY-102047A
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