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DZNep (3-Deazaneplanocin A) --- Histone Methyltransferase Inhibitor

DZNep (3-Deazaneplanocin A) --- Histone Methyltransferase Inhibitor

$129.00
An S-adenosylhomocysteine hydrolase inhibitor, indirectly inhibiting histone methyltransferases and decreasing global DNA methylation
Catalog No. Unit Price Qty
M60141-2s 2mg solid $129.00
M60141-2 10 mM in DMSO (0.760 mL) $129.00
M60141-25s 25mg solid $950.00

Details

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: 4oC 1 year. DMSO: 4oC 3 month; -20oC 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. 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. 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. 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. 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. 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.

Description

Details

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: 4oC 1 year. DMSO: 4oC 3 month; -20oC 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. 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. 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. 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. 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. 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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