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SJFα

Cat. No. 7268 Submit a Review Datasheet / COA / SDS
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Description: Potent and selective p38α PROTAC®
Alternative Names: SJFa PROTAC,SJFalpha PROTAC,SJFα PROTAC
Chemical Name: 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
Purity: ≥98% (HPLC)
Datasheet
Citations
Reviews
Literature (2)
Biological Activity Technical Data Solubility Calculators Datasheets References

Biological Activity 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.

Technical Data for SJFα

M. Wt 1120.28
Formula C59H67F2N7O11S
Storage Store at -20°C
Purity ≥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

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

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

Solubility Data for SJFα

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 112.03 100

Preparing Stock Solutions for SJFα

The following data is based on the product molecular weight 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.

Select a batch to recalculate based on the batch molecular weight:
Concentration / Solvent Volume / Mass 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

Molarity Calculator

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References for SJFα

References are publications that support the biological activity of the product.

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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Citations for SJFα

Citations are publications that use Tocris products.

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Literature in this Area

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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