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KDOAM-25

Catalog No. T11751   CAS 2230731-99-2

KDOAM-25 increases global H3K4 methylation at transcriptional start sites and impairs proliferation in multiple myeloma MM1S cells.KDOAM-25 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 Chemical Structure
KDOAM-25, CAS 2230731-99-2
Pack Size Availability Price/USD Quantity
5 mg 6-8 weeks $ 215.00
50 mg 6-8 weeks $ 818.00
100 mg 6-8 weeks $ 1,230.00
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Biological Description
Chemical Properties
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Description KDOAM-25 increases global H3K4 methylation at transcriptional start sites and impairs proliferation in multiple myeloma MM1S cells.KDOAM-25 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 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 (50 μM) increases with approximately twice as much H3K4me3 in in multiple myeloma cells. KDOAM-25 inhibits most potently KDM5B with an IC50 of ~50 μM and the other KDM5 family members at concentrations above 100 μM. KDOAM-25 shows no cellular activity on any of the other tested JmjC family members. KDOAM-25 is able to reduce the viability of MM1S cells with an IC50 of ~30 μM after a delay of 5-7 days.
Molecular Weight 307.39
Formula C15H25N5O2
CAS No. 2230731-99-2

Storage

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

TargetMolReferences 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

KDOAM-25 2230731-99-2 Microbiology/Virology Antibacterial KDOAM25 KDOAM 25 inhibitor inhibit

 

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