Description
KDOAM-25 citrate 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 citrate increases global H3K4 methylation at transcriptional start sites and impairs proliferation in multiple myeloma MM1S cells.
Product information
CAS Number: 2448475-08-7
Molecular Weight: 499.51
Formula: C21H33N5O9
Chemical Name: 2-hydroxypropane-1,2,3-tricarboxylic acid; 2-{[({[2-(dimethylamino)ethyl](ethyl)carbamoyl}methyl)amino]methyl}pyridine-4-carboxamide
Smiles: CN(C)CCN(CC)C(=O)CNCC1=CC(=CC=N1)C(N)=O.OC(=O)C(O)(CC(O)=O)CC(O)=O
InChiKey: LOVVSPOOXGDJRT-UHFFFAOYSA-N
InChi: InChI=1S/C15H25N5O2.C6H8O7/c1-4-20(8-7-19(2)3)14(21)11-17-10-13-9-12(15(16)22)5-6-18-13;7-3(8)1-6(13,5(11)12)2-4(9)10/h5-6,9,17H,4,7-8,10-11H2,1-3H3,(H2,16,22);13H,1-2H2,(H,7,8)(H,9,10)(H,11,12)
Technical Data
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
Solubility: DMSO : 200 mg/mL (400.39 mM; Need ultrasonic).
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥12 months if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined
HS Tariff Code: 382200
How to use
In Vitro:
KDOAM-25 citrate inhibits most potently KDM5B with an IC50 of ∼50 μM and the other KDM5 family members at concentrations above 100 μM. KDOAM-25 citrate shows no cellular activity on any of the other tested JmjC family members. KDOAM-25 citrate is able to reduce the viability of MM1S cells with an IC50 of ∼30 μM after a delay of 5-7 days. 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. KDOAM-25 citrate (50 μM) increases with approximately twice as much H3K4me3 in in multiple myeloma cells.
Products are for research use only. Not for human use.
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