For research use only. Not for therapeutic Use.
TAK-243 (MLN7243)（Cat No.:I009684）is a first-in-class small-molecule inhibitor of ubiquitin-activating enzyme 1 (UBA1), a crucial enzyme in the ubiquitin-proteasome pathway. By blocking UBA1, TAK-243 disrupts the initiation of the ubiquitination process, leading to the accumulation of damaged proteins within cells, ultimately triggering apoptosis in cancer cells. Its unique mechanism targets a fundamental cellular process, making TAK-243 a promising candidate for treating various cancers, especially those reliant on heightened protein turnover. This selective inhibition approach enhances TAK-243’s therapeutic potential while minimizing effects on non-cancerous cells.
| Catalog Number | I009684 |
| CAS Number | 1450833-55-2 |
| Synonyms | TAK-243; TAK 243; TAK243; MLN7243; MLN-7243; MLN 7243; AOB87172; AOB-87172; AOB 87172. |
| Molecular Formula | C19H20F3N5O5S2 |
| Purity | ≥95% |
| Target | NF-κB |
| Solubility | Soluble in DMSO, not in water |
| Storage | 2-8°C(protect from light) |
| IUPAC Name | [(1R,2R,3S,4R)-2,3-dihydroxy-4-[[2-[3-(trifluoromethylsulfanyl)phenyl]pyrazolo[1,5-a]pyrimidin-7-yl]amino]cyclopentyl]methyl sulfamate |
| InChI | InChI=1S/C19H20F3N5O5S2/c20-19(21,22)33-12-3-1-2-10(6-12)13-8-16-24-5-4-15(27(16)26-13)25-14-7-11(17(28)18(14)29)9-32-34(23,30)31/h1-6,8,11,14,17-18,25,28-29H,7,9H2,(H2,23,30,31)/t11-,14-,17-,18+/m1/s1 |
| InChIKey | KJDAGXLMHXUAGV-DGWLBADLSA-N |
| SMILES | C1[C@@H]([C@H]([C@H]([C@@H]1NC2=CC=NC3=CC(=NN23)C4=CC(=CC=C4)SC(F)(F)F)O)O)COS(=O)(=O)N |
| Reference | </br>1.Preparation of ubiquitin-activating enzyme inhibitor and use alone and in combination with other chemotherapeutic agents for treatment of cancer by Bence, Neil; Huck, Jessica; Hyer, Marc; Milhollen, Michael; Shi, Judy Qiuju; Traore, Tary from PCT Int. Appl. (2016), WO 2016069392 A1 20160506. | Language: English, Database: CAPLUS</br>2.Preparation of ubiquitin-activating enzyme inhibitor and use in combination with radiation for treatment of cancer by Bence, Neil; Hyer, Marc; Milhollen, Michael; Samnotra, Vivek; Santillana Soto, Sergio Luis; Sappal, Darshan from PCT Int. Appl. (2016), WO 2016069393 A1 20160506. | Language: English, Database: CAPLUS</br>3.Preparation of pyrazolopyrimidinyl compounds as inhibitors of ubiquitin-activating enzyme by Afroze, Roushan; Bharathan, Indu T.; Ciavarri, Jeffrey P.; Fleming, Paul E.; Gaulin, Jeffrey L.; Girard, Mario; Langston, Steven P.; Soucy, Francois R.; Wong, Tzu-Tshin; Ye, Yingchun from PCT Int. Appl. (2013), WO 2013123169 A1 20130822. | Language: English, Database: CAPLUS |
