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Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) |
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SKU | Size | Availability | Price | Qty |
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U125711-5mg | 5mg | Available within 4-8 weeks(?) Items will be manufactured post-order and can take 4-8 weeks. Thank you for your patience! | $88.90 | |
U125711-25mg | 25mg | In stock | $400.90 | |
U125711-100mg | 100mg | Available within 4-8 weeks(?) Items will be manufactured post-order and can take 4-8 weeks. Thank you for your patience! | $835.90 |
Potent, selective cell-permeable EZH2 methyltransferase inhibitor
Synonyms | UNC1999|1431612-23-5|UNC-1999|UNC 1999|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|1-Isopropyl-6-(6-(4-isopropylpiperazin-1-yl)pyridin-3-yl)-N-((6-methyl-2-oxo-4-p |
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Specifications & Purity | ≥98% |
Storage Temp | Store at -20°C |
Shipped In | Dry ice |
Grade | Moligand™ |
Action Type | INHIBITOR |
Mechanism of action | Inhibitor of enhancer of zeste 2 polycomb repressive complex 2 subunit |
Product Description | UNC1999 is a potent, orally bioavailable and selective inhibitor of EZH2 and EZH1 with IC50 of 2 nM and 45 nM in cell-free assays, respectively, showing >1000-fold selectivity over a broad range of epigenetic and non-epigenetic targets. |
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) |
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Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) |
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IUPAC 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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INCHI | InChI=1S/C33H43N7O2/c1-7-8-24-15-23(6)37-33(42)28(24)19-35-32(41)27-16-26(17-30-29(27)20-36-40(30)22(4)5)25-9-10-31(34-18-25)39-13-11-38(12-14-39)21(2)3/h9-10,15-18,20-22H,7-8,11-14,19H2,1-6H3,(H,35,41)(H,37,42) |
InChi Key | DPJNKUOXBZSZAI-UHFFFAOYSA-N |
Canonical 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 |
Isomeric 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 |
WGK Germany | 3 |
PubChem CID | 72551585 |
Molecular Weight | 569.74 |
CAS Registry No. | 1431612-23-5 |
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PubChem CID | 72551585 |
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Solubility | DMSO |
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Pictogram(s) | GHS07 |
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Signal | Warning |
Hazard Statements | H302:Harmful if swallowed |
Precautionary Statements | P501:Dispose of contents/container to ... P264:Wash hands [and …] thoroughly after handling. P270:Do not eat, drink or smoke when using this product. P330:Rinse mouth. P301+P317:IF SWALLOWED: Get medical help. |
WGK Germany | 3 |
1. Konze KD, Ma A, Li F, Barsyte-Lovejoy D, Parton T, Macnevin CJ, Liu F, Gao C, Huang XP, Kuznetsova E et al.. (2013) An orally bioavailable chemical probe of the Lysine Methyltransferases EZH2 and EZH1.. ACS Chem Biol, 8 (6): (1324-34). [PMID:23614352] |
2. Marsolier J et al.. (2022) H3K27me3 conditions chemotolerance in triple-negative breast cancer.. Nat Genet, 54 (4): (459-468). [PMID:35410383] |
3. Zijlmans DW et al.. (2022) Integrated multi-omics reveal polycomb repressive complex 2 restricts human trophoblast induction.. Nat Cell Biol, 24 (6): (858-871). [PMID:35697783] |