- 商品介绍
- 规格参数
- 包装参数
General description
A cell-permeable compound that is shown (at 1 µM concentrations) to inhibit EZH2-mediated trimethylation of K27 on histone H3 and induces the expression of cell-cycle regulatory genes, p21 and p27, as well as the cell death regulator, FBXO32, in OCI-AML3 and HL-60 cells, whereby treatment with inhibitor increases p16 levels in the former, but not the latter of the two cultures. At concentrations between 200 nm and 2000 nM, this compound is found to dose-dependently deplete the expression of polycomb group proteins EZH2, SUZ12, and EED in cultured and primary AML cell extracts. At concentrations up to ≥ 1000 nM, DZNep dose-dependently increases the percentage of apoptotic cells up to > ~ 38%, with greater potency against OCI-AML3 than HL-60 cultures and inhibits colony growth up to > ~ 85% for both cell lines. In OCI-AML3 cultures, 1000 nM of treatment demonstrates a significant increase in the accumulation of cells in the G0/G1 phase (58.5%) with a concomitant decrease in the number of cells in S phase (35.2%) and G2/M phases (6.3%) of the cell cycle. When co-treated with panobinostat (PS), 200 nM to 1000nM DZNep is shown to decrease cell viability in OCI-AML3 and HL-60 cultures more effectively than DZNep alone, in a dose-dependent manner. DZNep (1mg/kg, twice per week, i.p.) and PS significantly prolong the survival of mice implanted with HL-60 cells compared to treatment with either compound alone. DZNep is also a known S-adenosyl-L-homocysteine (AdoHcy) hydrolase inhibitor.
Biochem/physiol Actions
Cell permeable: yes
Primary Target
EZH2
Reversible: yes
Packaging
Packaged under inert gas
Physical form
A 25 mM (1 mg/98 µL) sterile-filtered solution of Histone Methyltransferase EZH2 Inhibitor, DZNep (Cat. No. 252790) in H₂O.
Preparation Note
Following initial thaw, aliquot and freeze (-20°C). Aliquots are stable for up to 6 monthst at -20°C.
This product is a 25 mM (1 mg/98 µL) sterile-filtered solution in H2O.
Other Notes
Sun, F., et al. 2009. Mol. Cancer Ther.8, 3191.
Miranda, T.B., et al. 2009. Mol. Cancer Ther.8, 1579.
Fiscus, W., et al. 2009. Blood13, 2733.
Tan, J., et al. 2007. Genes Dev.21, 1050.
Chiang, P.K., et al. 1992. J. Biol. Chem.267, 4988.
Tseng, C.K., et al. 1989. J. Med. Chem.32, 1442.
Glazer, R.I., et al. 1986. Biochem. Biophys. Res. Commun.135, 688.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Disclaimer
Toxicity: Standard Handling (A)
| Quality Level | 100 |
| assay | ≥98% (HPLC) |
| form | liquid |
| manufacturer/tradename | Calbiochem® |
| storage condition | OK to freeze,avoid repeated freeze/thaw cycles,protect from light |
| storage temp. | −70°C |
| SMILES string | [n]2(c3c(nc2)c(ncc3)N)[C@H]1[C@@H]([C@@H](C(=C1)CO)O)O |
| InChI | 1S/C12H14N4O3/c13-12-9-7(1-2-14-12)16(5-15-9)8-3-6(4-17)10(18)11(8)19/h1-3,5,8,10-11,17-19H,4H2,(H2,13,14)/t8-,10-,11+/m1/s1 |
| InChI key | OMKHWTRUYNAGFG-IEBDPFPHSA-N |
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| 重量(kg) |
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¥ 2707.32
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¥ 2622.09
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¥ 2290.21
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¥ 2019.57
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¥ 1779.22
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¥ 6330.00
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¥ 3290.05
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¥ 2666.57
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¥ 1783.21
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