SJFα

Pricing Availability   Qty
说明: Potent and selective p38α PROTAC®
别名: SJFa PROTAC,SJFalpha PROTAC,SJFα PROTAC
化学名: N-(3-Fluoro-4-((7-(4-(4-(2-(((S)-1-((2S,4R)-4-hydroxy-2-((4-(4-methylthiazol-5-yl)benzyl)carbamoyl)pyrrolidin-1-yl)-3,3-dimethyl-1-oxobutan-2-yl)amino)-2-oxoethoxy)butoxy)butoxy)-6-methoxyquinolin-4-yl)oxy)phenyl)-N-(4-fluorophenyl)cyclopropane-1,1-dicarboxamide
纯度: ≥98% (HPLC)
说明书
引用文献
评论
文献 (2)

生物活性 for SJFα

SJFα is a potent and selective p38α PROTAC® Degrader (DC50 = 7.16 nM; Dmax = 97.4%). SJFα comprises the multikinase inhibitor foretinib joined by a linker to a VHL ligand. Displays significantly lower potency degradation at p38δ (DC50 = 299 nM). Exhibits no significant degradation of p38β, p38γ or related MAPKs, ERK1/2, or JNK1/2.

p38γ antibodies validated for Simple Western™ (automated Western) instruments also available: Catalog # AF1347 and MAB1347.

PROTAC® is a registered trademark of Arvinas Operations, Inc., and is used under license.

技术数据 for SJFα

分子量 1120.28
公式 C59H67F2N7O11S
储存 Store at -20°C
纯度 ≥98% (HPLC)
CAS Number 2254609-27-1
PubChem ID 137628677
InChI Key GXDYWQXTEYENEU-WFYKIECOSA-N
Smiles COC1=CC2=C(N=CC=C2OC3=C(C=C(C=C3)NC(C4(C(NC5=CC=C(C=C5)F)=O)CC4)=O)F)C=C1OCCCCOCCCCOCC(N[C@@H](C(C)(C)C)C(N6C[C@@H](C[C@H]6C(NCC7=CC=C(C8=C(N=CS8)C)C=C7)=O)O)=O)=O

上方提供的技术数据仅供参考。批次相关数据请参见分析证书。

Tocris products are intended for laboratory research use only, unless stated otherwise.

溶解性数据 for SJFα

溶剂 最高浓度 mg/mL 最高浓度 mM
溶解性
DMSO 112.03 100

制备储备液 for SJFα

以下数据基于产品分子量 1120.28。 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

选择批次从而根据批次分子量重新计算:
浓度/溶剂体积/质量 1 mg 5 mg 10 mg
1 mM 0.89 mL 4.46 mL 8.93 mL
5 mM 0.18 mL 0.89 mL 1.79 mL
10 mM 0.09 mL 0.45 mL 0.89 mL
50 mM 0.02 mL 0.09 mL 0.18 mL

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参考文献 for SJFα

参考文献是支持产品生物活性的出版物。

Smith et al (2019) Differential PROTAC substrate specificity dictated by orientation of recruited E3 ligase. Nat. Commun. 10 131 PMID: 30631068


If you know of a relevant reference for SJFα, please let us know.

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该领域的文献

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TPD and Induced Proximity Research Product Guide

TPD and Induced Proximity Research Product Guide

This brochure highlights the tools and services available from Bio-Techne to support your Targeted Protein Degradation and Induced Proximity research, including:

  • Active Degraders
  • TAG Degradation Platform
  • Degrader Building Blocks
  • Assays for Protein Degradation
  • Induced Proximity Tools
Targeted Protein Degradation Poster

Targeted Protein Degradation Poster

Degraders (e.g. PROTACs) are bifunctional small molecules, that harness the Ubiquitin Proteasome System (UPS) to selectively degrade target proteins within cells. They consist of three covalently linked components: an E3 ubiquitin ligase ligand, a linker and a ligand for the target protein of interest. Authored in-house, this poster outlines the generation of a toolbox of building blocks for the development of Degraders. The characteristics and selection of each of these components are discussed. Presented at EFMC 2018, Ljubljana, Slovenia