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KDOAM-25 citrate

Catalog No. T11750   CAS 2448475-08-7

KDOAM-25 citrate is a potent and highly selective histone lysine demethylases 5 (KDM5) inhibitor with IC 50 s of 71 nM, 19 nM, 69 nM, 69 nM for KDM5A, KDM5B, KDM5C, KDM5D, respectively. Multiple myeloma MM1S cells treated with KDOAM-25 citrate show increased global H3K4 methylation at transcriptional start sites and impaired proliferation [1].

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KDOAM-25 citrate Chemical Structure
KDOAM-25 citrate, CAS 2448475-08-7
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100 mg 10-14 weeks $ 996.00
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Biological Description
Chemical Properties
Storage & Solubility Information
Description KDOAM-25 citrate is a potent and highly selective histone lysine demethylases 5 (KDM5) inhibitor with IC 50 s of 71 nM, 19 nM, 69 nM, 69 nM for KDM5A, KDM5B, KDM5C, KDM5D, respectively. Multiple myeloma MM1S cells treated with KDOAM-25 citrate show increased global H3K4 methylation at transcriptional start sites and impaired proliferation [1].
Targets&IC50 KDM5A:71 nM , KDM5D:69 nM , KDM5B:19 nM , KDM5C:69 nM
In vitro KDOAM-25 citrate inhibits most potently KDM5B with an IC 50 of ~50 μM and the other KDM5 family members at concentrations above 100 μM. KDOAM-25 citrate is inactive against any of the other tested JmjC family members [1]. KDOAM-25 citrate is able to reduce the viability of MM1S cells with an IC 50 of ~30 μM after a delay of 5-7 days [1]. KDOAM-25 citrate 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 citrate (50 μM) increases with approximately twice as much H3K4me3 in in multiple myeloma cells [1].
Molecular Weight 499.51
Formula C21H33N5O9
CAS No. 2448475-08-7

Storage

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

Solubility Information

DMSO: 200 mg/mL (400.39 mM), Sonication is recommended.

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 citrate 2448475-08-7 Others KDOAM25 citrate KDOAM 25 citrate KDOAM-25 Citrate KDOAM25 Citrate KDOAM 25 Citrate inhibitor inhibit

 

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