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Submit ReviewZLD 1039 is a potent and selective EZH2 inhibitor (IC50 = 5.6 nM). Displays selectivity for EZH2 over a panel of HMTs (inhibition less than 30% at 16 μM). Blocks H3K27 methylation in breast cancer cell lines. Induces tumor regression and metastasis in breast cancer xenograft-bearing mice. Reactivates silenced tumor suppressors in vivo. Orally bioavailable.
M. Wt | 612.8 |
Formula | C36H48N6O3 |
Storage | Store at -20°C |
Purity | ≥98% (HPLC) |
CAS Number | 1826865-46-6 |
PubChem ID | 132517142 |
InChI Key | SZAYCVHJDOWSNY-UHFFFAOYSA-N |
Smiles | CCN(C1=CC(C2=CN=C(N3CCN(CC3)C)C=C2)=CC(C(NCC4=C5CCCCC5=C(NC4=O)C)=O)=C1C)C6CCOCC6 |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solvent | Max Conc. mg/mL | Max Conc. mM | |
---|---|---|---|
Solubility | |||
DMSO | 12.26 | 20 with gentle warming | |
ethanol | 12.26 | 20 with gentle warming |
The following data is based on the product molecular weight 612.8. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
---|---|---|---|
0.2 mM | 8.16 mL | 40.8 mL | 81.59 mL |
1 mM | 1.63 mL | 8.16 mL | 16.32 mL |
2 mM | 0.82 mL | 4.08 mL | 8.16 mL |
10 mM | 0.16 mL | 0.82 mL | 1.63 mL |
References are publications that support the biological activity of the product.
Song et al (2016) Corrigendum: Selective inhibition of EZH2 by ZLD1039 blocks H3K27methylation and leads to potent anti-tumor activity in breast cancer. Sci.Rep. 29 24893 PMID: 27128979
If you know of a relevant reference for ZLD 1039, please let us know.
Keywords: ZLD 1039, ZLD 1039 supplier, ZLD1039, Potent, selective, EZH2, inhibitors, inhibits, orally, bioavailable, H3K27, methylation, 5847, Tocris Bioscience
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Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!
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