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この商品について
実験式(ヒル表記法):
C15H25N5O2 · xHCl · yH2O
分子量:
307.39 (anhydrous free base basis)
UNSPSC Code:
12352200
NACRES:
NA.77
MDL number:
製品名
KDOAM25 hydrochloride hydrate, ≥98% (HPLC)
SMILES string
N(CCN(CC)C(=O)CNCc1nccc(c1)C(=O)N)(C)C
InChI key
PNFMVADNCOGWME-UHFFFAOYSA-N
assay
≥98% (HPLC)
form
powder
storage condition
desiccated
color
white to beige
solubility
H2O: 2 mg/mL, clear
storage temp.
−20°C
Quality Level
Biochem/physiol Actions
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.
保管分類
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
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
ライフサイエンス、有機合成、材料科学、クロマトグラフィー、分析など、あらゆる分野の研究に経験のあるメンバーがおります。.
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