For research use only. Not for therapeutic Use.
TMX-4153 is a bivalent degrader. TMX-4153 rapidly and selectively degrades endogenous PIP4K2C by recruiting the von Hippel-Lindau (VHL) E3 ligase complex, with a KD value of 42 nM. TMX-4153 can be used to synthesize PROTAC[1].
TMX-4153 (0.01, 0.05, 0.1, 0.5, 1 µM; 6 h) can selectively degrades PIP4K2C in MOLT4 cells[1].
| Catalog Number | I041180 |
| CAS Number | 2867519-91-1 |
| Synonyms | (2S,4R)-1-[(2S)-2-[[7-[2-[5-[[5-chloro-4-(3-phenylphenyl)pyrimidin-2-yl]amino]pyridin-3-yl]-1-oxo-2,8-diazaspiro[4.5]decan-8-yl]-7-oxoheptanoyl]amino]-3,3-dimethylbutanoyl]-4-hydroxy-N-[(1S)-1-[4-(4-methyl-1,3-thiazol-5-yl)phenyl]ethyl]pyrrolidine-2-carboxamide |
| Molecular Formula | C59H67ClN10O6S |
| Purity | ≥95% |
| InChI | InChI=1S/C59H67ClN10O6S/c1-37(39-19-21-41(22-20-39)52-38(2)63-36-77-52)64-54(74)48-31-46(71)35-70(48)55(75)53(58(3,4)5)66-49(72)17-10-7-11-18-50(73)68-26-23-59(24-27-68)25-28-69(56(59)76)45-30-44(32-61-33-45)65-57-62-34-47(60)51(67-57)43-16-12-15-42(29-43)40-13-8-6-9-14-40/h6,8-9,12-16,19-22,29-30,32-34,36-37,46,48,53,71H,7,10-11,17-18,23-28,31,35H2,1-5H3,(H,64,74)(H,66,72)(H,62,65,67)/t37-,46+,48-,53+/m0/s1 |
| InChIKey | NIQFZCJNEODJTE-CSIWTOAPSA-N |
| SMILES | CC1=C(SC=N1)C2=CC=C(C=C2)C(C)NC(=O)C3CC(CN3C(=O)C(C(C)(C)C)NC(=O)CCCCCC(=O)N4CCC5(CC4)CCN(C5=O)C6=CN=CC(=C6)NC7=NC=C(C(=N7)C8=CC=CC(=C8)C9=CC=CC=C9)Cl)O |
| Reference | [1]. Teng M, et al. Targeting the Dark Lipid Kinase PIP4K2C with a Potent and Selective Binder and Degrader. Angew Chem Int Ed Engl. 2023 Apr 24;62(18):e202302364. |
