UNC1999, EZH2 methyltransferase inhibitor (ab146152)
Key features and details
- Potent, selective cell-permeable EZH2 methyltransferase inhibitor
- CAS Number: 1431612-23-5
- Purity: > 98%
Soluble in DMSO (up to 10 mg/ml)
- Form / State: Solid
- Source: Synthetic
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 dual inhibitor of EZH2 and EZH1 methyltransferase inhibitor (IC50 = 45 nM and 2 nM respectively) (Konze et al. ). Inhibits H3K27 methylation (IC50 = 124 nM, MCF10A cells). Competitive with the cofactor SAM, and non-competitive with the peptide substrate. Inhibition of EZH2 with UNC1999 enhanced the efficacy of gefitinib in suppressing the proliferation of colon cancer cells (Katona et al.). It suppresses global H3K27 trimethylation/demethylation and inhibits the growth of mixed lineage leukemia (MLL)-rearranged leukemia cells ( Xu et al.). Orally bioavailable.
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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
