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3-Deazaneplanocin A (DZNep) hydrochloride

Cat No.
CEI-1191
Description
3-Deazaneplanocin A hydrochloride is an inhibitor of histone methyltransferase.
Product Overview
3-Deazaneplanocin A (DZNep) hydrochloride is a selective inhibitor of ENZ2 inhibitor with IC50 value of 0.08-0.24 μM. ENZ2 is a sub-unit of PRC2 and plays an important role in regulating cell proliferation and cell-cycle progression. It has been reported that ENZ2 is over-expressed in many tumors, including prostate, breast, bladder cancers and AML. In HepG2 cell lines, DZNep treatment markedly induced the intracellular lipids increasement and TNF-α and TGF-β expression in mRNA level by augmenting PA/OA-dependent lipid accumulation. DZNep is a potent ENZ2 inhibitor. When tested with human acute myeloid leukemia (AML) HL-60 and OCI-AML3 cell lines, administration of DZNep induced cell apoptosis by depleting ENZ2, cyclin E and HOXA9 expressions and inducing p16, p21,p27 and FBXO32 expressions in a dose-dependent manner. In high-fat/high-fructose diet fed (HFa/HFr-D) rat mouse model that resembles human NAFLD metabolically and histologically, DZNep functioned as the effective agent to anti-inflammatory and anti-fibrotic roles by inhibiting ENZ2.It is also reported that DZNep has the inhibitory activity for (SAHH (S-adenosylhomocysteine hydrolase) with Ki value of 50 pM.
CAS No.
120964-45-6
Molecular Weight
298.73
Purity
0.98
Storage
Store at -20°C
Synonyms
NSC 617989 hydrochloride,DZNep,3-Deazaneplanocin A
Targets
SAHH; ENZ2
Molecular Formula
C12H14N4O3.HCl
Chemical Name
(1S,2R,5R)-5-(4-aminoimidazo[4,5-c]pyridin-1-yl)-3-(hydroxymethyl)cyclopent-3-ene-1,2-diol; hydrochloride
Solubility
Soluble in DMSO > 10 mM
Shipping Conditions
Evaluation sample solution: ship with blue ice. All other available size: ship with RT, or blue ice upon request
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