3-Deazaneplanocin A (DZNep) hydrochloride

Catalog #
27618-1
$450 *
Size: 5 mg
Qty
*US Pricing only. For international pricing, please contact your local distributor.
Purchase
Description

3-Deazaneplanocin A (DZNep) is an S-Adenosylhomocysteine Hydrolase inhibitor and histone methyltransferase EZH2 inhibitor.

Synonyms
NSC 617989 hydrochloride; DZNep; 3-Deazaneplanocin A; (1S,2R,5R)-5-(4-aminoimidazo[4,5-c]pyridin-1-yl)-3-(hydroxymethyl)cyclopent-3-ene-1,2-diol;hydrochloride
Product Info
Storage and Usage
Citations
Purity

≥98% by HPLC

Target(s)
EZH2
Formula
C12H14N4O3 • HCl
MW
298.7 Da
Solubility
Soluble in Water
Biological Activity
3-deazaneplanocin A (DZNeP), an analog of adenosine, is a competitive inhibitor of S-adenosylhomocysteine hydrolase with Ki of 50 pM. DZNep treatment resulted in dose-dependent inhibition of proliferation in NSCLC cell lines with IC50 ranging from 0.08 to 0.24 µM.
CAS Registry #
120964-45-6
Background
3-Deazaneplanocin A (DZNep) is an S-Adenosylhomocysteine Hydrolase inhibitor and histone methyltransferase EZH2 inhibitor. It switches on repressed tumor suppressor genes and induces apoptosis by inhibiting the expression of EZH2. Blocks EZH2 activity and trimethylation of lysine 27 on histone H3 in vitro. Induces apoptotic cell death in cancer cells and inhibits s-adenosylhomocysteine (SAH) hydrolase. Decreases global DNA methylation and enhances Oct 4 expression in chemically induced pluripotent stem cells (CiPSCs). DZNeP decreased cell migration, which was additionally reduced by DZNeP/gemcitabine combination.
References
1. Fujiwara T, et al. J Biol Chem. 2014 Mar 21;289(12):8121-34.
2. Cui, B., et al. J Clin Endocrinol Metab. 2014 Jun;99(6):E962-70.
3. Cheng, L.L., et al. Clin Cancer Res. 2012 Aug 1;18(15):4201-12.
4. Nakagawa, S., et al. Oncol Rep. 2014 Feb;31(2):983-8.