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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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G126541-5mg | 5mg | Available within 4-8 weeks(?) Items will be manufactured post-order and can take 4-8 weeks. Thank you for your patience! | $64.90 | |
G126541-25mg | 25mg | Available within 4-8 weeks(?) Items will be manufactured post-order and can take 4-8 weeks. Thank you for your patience! | $214.90 | |
G126541-100mg | 100mg | Available within 4-8 weeks(?) Items will be manufactured post-order and can take 4-8 weeks. Thank you for your patience! | $639.90 |
Potent, selective, cell-permeable\xa0histone H3-lysine 27 (H3K27) methyltransferase EZH2 inhibitor
Synonyms | N-[(6-methyl-2-oxo-4-propyl-1H-pyridin-3-yl)methyl]-6-[2-(4-methylpiperazin-1-yl)pyridin-4-yl]-1-propan-2-ylindazole-4-carboxamide | S7164 | HMS3740C09 | GSK343 | GSK-343 | 1-isopropyl-N-[(6-methyl-2-oxo-4-propyl-1,2-dihydropyridin-3-yl)methyl]-6-[2-(4-me |
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Specifications & Purity | Moligand™, ≥98% |
Biochemical and Physiological Mechanisms | It is a potent, specific inhibitor of the histone H3-lysine 27 (H3K27) methyltransferase EZH2. GSK343 inhibits EZH2 enzymatic activity with an IC50 of 4 nM. The compound displays 60 fold selectivity for EZH2 vs. EZH1, and 1000 fold or greater selectivity |
Storage Temp | Store at 2-8°C |
Shipped In | Wet ice |
Grade | Moligand™ |
Action Type | INHIBITOR |
Mechanism of action | Inhibitor of enhancer of zeste 1 polycomb repressive complex 2 subunit;Inhibitor of enhancer of zeste 2 polycomb repressive complex 2 subunit |
Note | 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. |
Product Description | It is an epigenetic chemical probe available through a partnership between Sigma Life Science and the Structural Genomics Consortium (SGC). |
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Mechanism of Action | Action Type | target ID | Target Name | Target Type | Target Organism | Binding Site Name | References |
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IUPAC Name | N-[(6-methyl-2-oxo-4-propyl-1H-pyridin-3-yl)methyl]-6-[2-(4-methylpiperazin-1-yl)pyridin-4-yl]-1-propan-2-ylindazole-4-carboxamide |
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INCHI | InChI=1S/C31H39N7O2/c1-6-7-23-14-21(4)35-31(40)26(23)18-33-30(39)25-15-24(16-28-27(25)19-34-38(28)20(2)3)22-8-9-32-29(17-22)37-12-10-36(5)11-13-37/h8-9,14-17,19-20H,6-7,10-13,18H2,1-5H3,(H,33,39)(H,35,40) |
InChi Key | ULNXAWLQFZMIHX-UHFFFAOYSA-N |
Canonical SMILES | CCCC1=C(C(=O)NC(=C1)C)CNC(=O)C2=C3C=NN(C3=CC(=C2)C4=CC(=NC=C4)N5CCN(CC5)C)C(C)C |
Isomeric SMILES | CCCC1=C(C(=O)NC(=C1)C)CNC(=O)C2=C3C=NN(C3=CC(=C2)C4=CC(=NC=C4)N5CCN(CC5)C)C(C)C |
WGK Germany | 3 |
PubChem CID | 71268957 |
Molecular Weight | 541.69 |
ChEMBL Ligand | CHEMBL2204995 |
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PubChem CID | 71268957 |
CAS Registry No. | 1346704-33-3 |
RCSB PDB Ligand | A97 |
Enter Lot Number to search for COA:
Find and download the COA for your product by matching the lot number on the packaging.
Lot Number | Certificate Type | Date | Item |
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H1610013 | Certificate of Analysis | Jan 16, 2024 | G126541 |
Solubility | DMSO: soluble15 mg/mL, clear |
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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. Verma SK, Tian X, LaFrance LV, Duquenne C, Suarez DP, Newlander KA, Romeril SP, Burgess JL, Grant SW, Brackley JA et al.. (2012) Identification of Potent, Selective, Cell-Active Inhibitors of the Histone Lysine Methyltransferase EZH2.. ACS Med Chem Lett, 3 (12): (1091-6). [PMID:24900432] [10.1021/op500134e] |
2. Zhou J, Huang S, Wang Z, Huang J, Xu L, Tang X, Wan YY, Li QJ, Symonds ALJ, Long H et al.. (2019) Targeting EZH2 histone methyltransferase activity alleviates experimental intestinal inflammation.. Nat Commun, 10 (1): (2427). [PMID:31160593] [10.1021/op500134e] |