| Hazard Information | Back Directory | [Description]
TX2-121-1 acts to inhibit HER3-dependent signalling and growth, to target HER3 for proteasome-mediated degradation. TX2-121-1 targets degradation reduces the amount of HER3 available to form the HER3 heterodimers believed to be required for cellular activity. TX2-121-1 is an analogue of TX1-85-1. | [Uses]
TX2-121-1 is a potent and selective Her3 (ErbB3) degrader that contains a hydrophobic adamantane moiety. TX2-121-1 has an IC50 of 49 nM for Her3. TX2-121-1 inhibits Her3-dependent signaling and heterodimerization of Her3. TX2-121-1 has the ability to inhibit cell proliferation. TX2-121-1 can be used in the study of tumors. (Pink: Her3 inhibitor (HY-164988); Black: Linker; Blue: Adamantane (HY-N2427))[1]. | [IC 50]
HER3: 49 nM (IC50) | [References]
[1] Lim SM, et, al. Development of small molecules targeting the pseudokinase Her3. Bioorg Med Chem Lett. 2015 Aug 15;25(16):3382-9. DOI:10.1016/j.bmcl.2015.04.103 |
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