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DZNep(3-DeazaneplanocinA)---HistoneMethyltransferaseInhibitor

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DZNep(3-DeazaneplanocinA)---HistoneMethyltransferaseInhibitor

品牌：Xcessbio

貨號：M60141-2s

規(guī)格：2mg solid

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DZNep(3-DeazaneplanocinA)---HistoneMethyltransferaseInhibitor

商品詳情參考文獻(xiàn) 相關(guān)資料

Product Information

Molecular Weight:	262.62
Formula:	C₁₂H₁₄N₄O₃
Purity:	≥98%
CAS#:	102052-95-9
Solubility:	DMSO up to 100 mM
Chemical Name:	(1S,2R,5R)-5-(4-amino-1H-imidazo[4,5-c]pyridin-1-yl)-3-(hydroxymethyl)cyclopent-3-ene-1,2-diol
Storage:	Powder: 4^oC 1 year. DMSO: 4^oC 3 month; -20^oC 1 year.

Biological Activity:

DZNep (3-Deazaneplanocin A, NSC617989) is an S-adenosylhomocysteine hydrolase inhibitor, indirectly inhibiting histone methyltransferases and decreasing global DNA methylation. It competitively inhibits S-adenosylhomocysteine hydrolase (Ki ~50 pM), decreases EZH2 activities, and inhibits 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 (IC₅₀?~0.2-1 μM). In vivo it shows strong anticancer activity by IP injection alone or in combination with the pan-histone deacetylase inhibitor panobinostat. DZNep can also enhance Oct 4 expression in generating induced pluripotent stem cells (iPSCs).

How to Use:

In vitro:? DZNep was used at 1 μM final concentration in vitro and in cellular assays.
In vivo: DZNep was IP or IV dosed to mice at 120 mg/kg once per day in the xenograft tumor model of Hep-G2, H358, A549, MDA-MB468, HCT116, CAL-27, HepG2, or HPAC.

Reference:

1. Tseng CK, et al. Synthesis of 3-deazaneplanocin A, a powerful inhibitor of S-adenosylhomocysteine hydrolase with potent and selective in vitro and in vivo antiviral activities. (1989) J Med Chem. 32(7):1442-6.
2. Tan J, et al. Pharmacologic disruption of Polycomb-repressive complex 2-mediated gene repression selectively induces apoptosis in cancer cells. (2007) Genes Dev. 21(9):1050-63.
3. Miranda TB, et al. DZNep is a global histone methylation inhibitor that reactivates developmental genes not silenced by DNA methylation. (2009) Mol Cancer Ther. 8(6):1579-88.
4. He S, et al. Inhibition of histone methylation arrests ongoing graft-versus-host disease in mice by selectively inducing apoptosis of alloreactive effector T cells. (2012) Blood. 119(5):1274-82.
5. Hou P, et al. Pluripotent stem cells induced from mouse somatic cells by small-molecule compounds. (2013) Science. 341(6146):651-4.?

Products are for research use only. Not for human use.

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