MLN7243
- TAK-243 - AOB 87172
- Optical Purity: 0.99
- Soluble in DMSO
- MF: C19H20F3N5O5S2
- MW: 519.52
Description
MLN7243 is a cell permeable small molecule inhibitor targeting ubiquitin-activating enzymes (UAE, also known as E1 enzymes). The enzymes, found more active in cancer cells than in normal, healthy cells, catalyze the first step in ubiquitination reaction, targeting a protein for degradation via Proteasome. This covalent attachment of ubiquitin or ubiquitin-like proteins to targeted proteins is a major mechanism for regulating protein function in eukaryotic organisms. Inhibition of the enzyme prevents both protein ubiquitination and subsequent ubiquitin-mediated proteasomal degradation, resulting in an excess of proteins in the cells that may lead to endoplasmic reticulum (ER) stress-mediated apoptosis, thus inhibit tumor (cancer) cell proliferation and survival.
More Information
| Parent CAS No. | 1450833-55-2 |
|---|---|
| Chemical Name | ((1R,2R,3S,4R)-2,3-dihydroxy-4-(2-(3-(trifluoromethylthio)phenyl)pyrazolo[1,5-a]pyrimidin-7-ylamino)cyclopentyl)methyl sulfamate |
| extra_info | Sold in collaboration with Chemietek |
| 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 |
| MFCD | N.A. |
| 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 |
| CID | 71715374 |
| Short Description | Ubiquitin-activating enzymes (UAE) Inhibitor |
