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Chemical Structure : TMX-2172
Catalog No.: PC-21526Not For Human Use, Lab Use Only.
TMX-2172 is a potent, selective CDK2 and CDK5 dual PROTAC degrader with IC50 of 6.5 nM and 6.8 nM for CDK2/cyclin A and CDK5/p25, respectively.
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TMX-2172 is a potent, selective CDK2 and CDK5 dual PROTAC degrader with IC50 of 6.5 nM and 6.8 nM for CDK2/cyclin A and CDK5/p25, respectively.
TMX-2172 shows high degradation selectivity for CDK2 and CDK5 over other cell cycle CDKs (CDK1, CDK4, and CDK6) and transcriptional CDKs (CDK7 and CDK9).
TMX-2172 exhibits antiproliferative activity against OVCAR8 with IC50 of 33.1 nM, an ovarian cancer cell line that overexpresses CCNE1 (a well-established activator of CDK2).
TMX-2172 exhibits an IC50 of 46.9 nM in cellular CRBN engagement assays.
TMX-2172 induced CDK2 degradation at a concentration of 250 nM in Jurkat cells with no effect against other cell cycle CDKs.
| M.Wt | 970.83 | |
| Formula | C41H45BrFN9O11S | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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1. Teng M, et al. Angew Chem Int Ed Engl. 2020 Aug 10;59(33):13865-13870.
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