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Merck

SML2774

Sigma-Aldrich

KDOAM25 hydrochloride hydrate

≥98% (HPLC)

Synonym(e):

2-[[[2-[2-(Dimethylamino)ethyl-ethyl-amino]-2-oxidanylidene-ethyl]amino]methyl]pyridine-4-carboxamide hydrochloride hydrate, 2-[[[2-[2-(Dimethylamino)ethyl-ethylamino]-2-oxoethyl]amino]methyl]pyridine-4-carboxamide hydrochloride hydrate, KDOAM-25 hydrochloride hydrate

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About This Item

Empirische Formel (Hill-System):
C15H25N5O2 · xHCl · yH2O
Molekulargewicht:
307.39 (anhydrous free base basis)
MDL-Nummer:
UNSPSC-Code:
12352200
NACRES:
NA.77

Qualitätsniveau

Assay

≥98% (HPLC)

Form

powder

Lagerbedingungen

desiccated

Farbe

white to beige

Löslichkeit

H2O: 2 mg/mL, clear

Lagertemp.

−20°C

SMILES String

N(CCN(CC)C(=O)CNCc1nccc(c1)C(=O)N)(C)C

InChIKey

PNFMVADNCOGWME-UHFFFAOYSA-N

Biochem./physiol. Wirkung

KDOAM25 is a selective inihbitor of the KDM5 family histone demethylases JARID1A, JARID1B, JARID1C and JARID1D with IC50 values < 60 nM. JARID1A and JARID1B are independently overexpressed in some cancers with JARID1B (KDM5B, PLU1) also identified as a potential oncogene, a repressor of tumour repressor genes. JARID1C (KDM5C) and JARID1D (KDM5D) are located on the X- and Y-chromosomes respectively. KDOAM25′s closest off-target is JMJD2C (selectivity >400 fold). It shows no activity on other tested 2-OG family members, including FIH, NO66, MINA53 and PHD2. KDOAM25 is active in cells.
Selective inihbitor of the KDM5 family histone demethylases JARID1A, JARID1B, JARID1C and JARID1D.

Lagerklassenschlüssel

11 - Combustible Solids

WGK

WGK 3

Flammpunkt (°F)

Not applicable

Flammpunkt (°C)

Not applicable


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Anthony Tumber et al.
Cell chemical biology, 24(3), 371-380 (2017-03-07)
Methylation of lysine residues on histone tail is a dynamic epigenetic modification that plays a key role in chromatin structure and gene regulation. Members of the KDM5 (also known as JARID1) sub-family are 2-oxoglutarate (2-OG) and Fe2+-dependent oxygenases acting as
Simone Pippa et al.
Molecules (Basel, Switzerland), 24(9) (2019-05-08)
Background: KDM5 enzymes are H3K4 specific histone demethylases involved in transcriptional regulation and DNA repair. These proteins are overexpressed in different kinds of cancer, including breast, prostate and bladder carcinomas, with positive effects on cancer proliferation and chemoresistance. For these

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