KDOAM-25 trihydrochloride


Catalog No. Size PriceQuantity
M17604-C Contact sales@xcessbio.com for quotation $100Unavailable

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.

Product information

Molecular Weight: 416.77

Formula: C15H28Cl3N5O2

Chemical Name: 2-[[[2-[2-(dimethylamino)ethyl-ethylamino]-2-oxoethyl]amino]methyl]pyridine-4-carboxamide;trihydrochloride

Smiles: Cl.Cl.Cl.CN(C)CCN(CC)C(=O)CNCC1=CC(=CC=N1)C(N)=O

InChiKey: DXHSLCAHOGWDPM-UHFFFAOYSA-N

InChi: InChI=1S/C15H25N5O2.3ClH/c1-4-20(8-7-19(2)3)14(21)11-17-10-13-9-12(15(16)22)5-6-18-13;;;/h5-6,9,17H,4,7-8,10-11H2,1-3H3,(H2,16,22);3*1H

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

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 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. 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.

Products are for research use only. Not for human use.

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