2666940-97-0
2666940-97-0 structure
- Name: Trametiglue
- Chemical Name: Trametiglue
- CAS Number: 2666940-97-0
- Molecular Formula: C25H24FIN6O5S
- Molecular Weight: 666.46
- Catalog: Signaling Pathways MAPK/ERK Pathway MEK
- Create Date: 2023-06-04 10:54:20
- Modify Date: 2024-04-06 22:34:00
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Trametiglue, a derivative of Trametinib (HY-10999), targets both KSR-MEK and RAF-MEK with unprecedented potency and selectivity via unique interfacial binding interactions[1].
| Name | Trametiglue |
|---|
| Description | Trametiglue, a derivative of Trametinib (HY-10999), targets both KSR-MEK and RAF-MEK with unprecedented potency and selectivity via unique interfacial binding interactions[1]. |
|---|---|
| Related Catalog | |
| Target |
MEK1 MEK2 |
| In Vitro | Trametiglue 在 KSR 结合的 MEK 上保留了 Trametinib 较强的结合力和停留时间[1]。 Trametiglue 与 Trametinib 不同，但与 Avutometinib (HY-18652) 相似，可增强内源性 BRAF 与 MEK1 之间的相互作用[1]。 Trametiglue (1 μM) 在直接结合实验中对 MEK1 和 MEK2 具有高选择性。Trametiglue 在抑制上游激酶对 MEK1 和 MEK2 底物磷酸化或直接 MEK1 磷酸化的一组活性激酶中也显示出高选择性[1]。 Trametiglue (5 days) 抑制 HCT116、A375、A549 和 SK-MEL-239 细胞活力，IC50 分别为 0.07、0.07、0.12 和 0.47 nM[1]。 Trametiglue (10 nM; 10 days) 抑制 KRAS 突变和 BRAF 突变癌细胞的集落形成，其效力高于 Trametinib [1]。 Cell Viability Assay[1] Cell Line: SK-MEL-239, HCT116, A549 and A375 Concentration: Incubation Time: 5 days Result: Showed IC50s of 0.47, 0.07, 0.12 and 0.07 nM against SK-MEL-239, HCT116, A549 and A375 cells, respectively. Western Blot Analysis[1] Cell Line: A549, HCT-116, A375 and SK-MEL-239 Concentration: 0.4, 0.8, 1.6, 3.1, 6.25, 12.5, 25 and 50 nM Incubation Time: 1 h Result: Inhibited the expression of pERK. And the effect was better than Trametinib. |
| References |
| Molecular Formula | C25H24FIN6O5S |
|---|---|
| Molecular Weight | 666.46 |