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Chemical Structure : TEAD inhibitor TM2
Catalog No.: PC-49537Not For Human Use, Lab Use Only.
TEAD inhibitor TM2 is a potent pan-TEAD auto-palmitoylation inhibitor with IC50 of 156 and 38 nM for TEAD2 palmitoylation and TEAD4 auto-palmitoylation, respectively, disrupts TEAD-YAP association and specifically inhibits YAP transcriptional activities.
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TEAD inhibitor TM2 is a potent pan-TEAD auto-palmitoylation inhibitor with IC50 of 156 and 38 nM for TEAD2 palmitoylation and TEAD4 auto-palmitoylation, respectively, disrupts TEAD-YAP association and specifically inhibits YAP transcriptional activities.
TM2 dramatically suppresses Myc-TEAD1 palmitoylation in cells in a dose-dependent manner, also significantly inhibits endogenous TEAD1-4 palmitoylation using an antibody recognizing pan-TEADs at as low as 100 nM.
TM2 adopts a novel binding mode compared to other known TEAD inhibitors (MGH-CP1, VT105 and K975).
TM2 showed striking anti-proliferation efficacy as a single agent in human MPM, a type of tumor that is highly associated with YAP activation, also shows synergy effects in combination with a MEK inhibitor in YAP-dependent cancer cells
| M.Wt | 435.568 | |
| Formula | C26H33N3O3 | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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1. Lu Hu, et al. Elife. 2022 Nov 18;11:e80210.
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