UNC1999, EZH2 methyltransferase inhibitor (ab146152)
- Datasheet
- References
Overview
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Product name
UNC1999, EZH2 methyltransferase inhibitor -
Description
Potent, selective cell-permeable EZH2 methyltransferase inhibitor -
Biological description
Potent, selective cell-permeable EZH2 methyltransferase inhibitor (IC50 = 2 nM). Inhibits H3K27 methylation (IC50 = 124 nM, MCF10A cells). Competitive with the cofactor SAM, and non-competitive with the peptide substrate. Orally bioavailable. -
Purity
> 98% -
CAS Number
1431612-23-5 -
Chemical structure
Properties
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Chemical name
N-[(6-Methyl-2-oxo-4-propyl-1H-pyridin-3-yl)methyl]-1-propan-2-yl-6-[6-(4-propan-2-ylpiperazin-1-yl)pyridin-3-yl]indazole-4-carboxamide
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Molecular weight
569.74 -
Molecular formula
C33H43N7O2 -
PubChem identifier
72551585 -
Storage instructions
Store at -20°C. Store under desiccating conditions. The product can be stored for up to 12 months. -
Solubility overview
Soluble in DMSO (up to 10 mg/ml)
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Handling
Wherever possible, you should prepare and use solutions on the same day. However, if you need to make up stock solutions in advance, we recommend that you store the solution as aliquots in tightly sealed vials at -20°C. Generally, these will be useable for up to one month. Before use, and prior to opening the vial we recommend that you allow your product to equilibrate to room temperature for at least 1 hour.
Need more advice on solubility, usage and handling? Please visit our frequently asked questions (FAQ) page for more details.
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SMILES
CCCC1=C(C(=O)NC(=C1)C)CNC(=O)C2=C3C=NN(C3=CC(=C2)C4=CN=C(C=C4)N5CCN(CC5)C(C)C)C(C)C -
Source
Synthetic
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Research areas
References
This product has been referenced in:
- Xu B et al. Selective inhibition of EZH2 and EZH1 enzymatic activity by a small molecule suppresses MLL-rearranged leukemia. Blood 125:346-57 (2015). Read more (PubMed: 25395428) »
- Katona BW et al. EZH2 inhibition enhances the efficacy of an EGFR inhibitor in suppressing colon cancer cells. Cancer Biol Ther 15:1677-87 (2014). Read more (PubMed: 25535899) »
- Konze KD et al. An orally bioavailable chemical probe of the Lysine Methyltransferases EZH2 and EZH1. ACS Chem Biol 8:1324-34 (2013). Read more (PubMed: 23614352) »
