An inhibitor of SAH hydrolase; depletes EZH2 levels and inhibits trimethylation of lysine 27 on histone H3 in acute myeloid leukemia cells in a dose-dependent manner (0.2-1 μM); increases expression of the cell-cycle regulators p21

3-Deazaneplanocin A – 5 mg

Brand:
Cayman
CAS:
102052-95-9
Storage:
-20
UN-No:
Non-Hazardous - /

3-Deazaneplanocin A is a cyclopentenyl analog of 3-deazaadenosine, originally synthesized as an inhibitor of S-adenosyl-L-homocysteine hydrolase.{18484} It has been shown to deplete EZH2 levels and to inhibit trimethylation of lysine 27 on histone H3 in cultured human acute myeloid leukemia (AML) HL-60 and OCI-AML3 cells and in primary AML cells in a dose-dependent manner (0.2-1 μM).{18478} 3-Deazaneplanocin A treatment of cultured human AML cells induces increased expression of the cell-cycle regulators p21, p27, and FBXO32, leading to cell cycle arrest and apoptosis.{18478} When used in combination with the pan-histone deacetylase inhibitor panobinostat (10 mg/kg), 3-deazaneplanocin A’s (1 mg/kg) antileukemic effects are synergistically enhanced in mice implanted with AML cells.{18478,18398}  

 

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Description

An inhibitor of SAH hydrolase; depletes EZH2 levels and inhibits trimethylation of lysine 27 on histone H3 in acute myeloid leukemia cells in a dose-dependent manner (0.2-1 μM); increases expression of the cell-cycle regulators p21, p27, and FBXO32 leading to cell cycle arrest and apoptosis

Formal name: 5R-(4-amino-1H-imidazo[4,5-c]pyridin-1-yl)-3-(hydroxymethyl)-3-cyclopentene-1S,2R-diol

Synonyms:  DZNep|NSC 617989

Molecular weight: 262.3

CAS: 102052-95-9

Purity: ≥97%

Formulation: A crystalline solid

Product Type|Biochemicals|Small Molecule Inhibitors|Methyltransferases||Research Area|Epigenetics, Transcription, & Translation|Writers|Histone Methylation

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