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商品描述
APS-2-79 hydrochloride
- Catalog No.：MC1221
- Data Sheet
- MSDS
- Support
- Description
- References ( 0 )
- Protocol
- CasNo：
- 2002381-31-7
- MolecularFormula：
- C23H21N3O3.HCl
- Purity：
- >98%
- Target：
- ERK
- IC50：
- IC50: 120±23 nM (KSR2), 418±40 nM (MEK1)[1]
- In Vitro：
- APS-2-79 modulate KSR-dependent MAPK signalling by antagonizing RAF heterodimerization as well as the conformational changes required for phosphorylation and activation of KSR-bound MEK (mitogenactivated protein kinase kinase). Furthermore, APS-2-79 increases the potency of several MEK inhibitors specifically within Rasmutant cell lines by antagonizing release of negative feedback signalling, demonstrating the potential of targeting KSR to improve the efficacy of current MAPK inhibitors. These results reveal conformational switching in KSR as a druggable regulator of oncogenic Ras, and further suggest co-targeting of enzymatic and scaffolding activities within Ras–MAPK signalling complexes as a therapeutic strategy for overcoming Ras-driven cancers[1].
- In Vivo：
- Fields：
- APS-2-79 is a novel modulator of KSR-dependent MAPK signalling,KSR2,IC50=120 nM
- Specificity：
- Target:ERK. Fields: APS-2-79 is a novel modulator of KSR-dependent MAPK signalling,KSR2,IC50=120 nM
- Source：
- Rabbit
- Dilution：
- IC50: 120±23 nM (KSR2), 418±40 nM (MEK1)[1]
- Concentration：
- >98%
- Storage Stability：
- 2 years -20°C Powder, 2 weeks4°C in DMSO,6 months-80°C in DMSO
- Other Name：
- APS 2 79,APS279,APS-279
- MolecularWeight(Da)：
- 423.89
- References：
- [1]. Dhawan NS, et al. Small molecule stabilization of the KSR inactive state antagonizes oncogenic Ras signalling. Nature. 2016 Sep 1;537(7618):112-116.
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