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SJFα - CAS 2254609-27-1

Inquiry

SJFα is a novel isoform-selective PROTAC p38α degrader. SJFα degrades p38α with a DC50 of 7.16 nM, but is far less effective at degrading p38δ (DC50 = 299 nM) and does not degrade the other p38 isoforms (β and γ) at concentrations up to 2.5 µM.

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Molecular Formula

C59H67F2N7O11S

Molecular Weight

1120.27

SJFα

- Specification
  - Purity
    
    ≥95%
    
    Solubility
    
    Soluble in DMSO
    
    Appearance
    
    White Solid
    
    Storage
    
    Store at 2-8°C for short term (days to weeks) or -20°C for long term (months to years)
    
    Shipping
    
    Room temperature in continental US; may vary elsewhere.
    
    IUPAC Name
    
    1-N'-[3-fluoro-4-[7-[4-[4-[2-[[(2S)-1-[(2S,4R)-4-hydroxy-2-[[4-(4-methyl-1,3-thiazol-5-yl)phenyl]methylcarbamoyl]pyrrolidin-1-yl]-3,3-dimethyl-1-oxobutan-2-yl]amino]-2-oxoethoxy]butoxy]butoxy]-6-methoxyquinolin-4-yl]oxyphenyl]-1-N-(4-fluorophenyl)cyclopropane-1,1-dicarboxamide
    
    Synonyms
    
    N-[(4-{4-[(4-{2-Fluoro-4-[({1-[(4-fluorophenyl)carbamoyl]cyclopropyl}carbonyl)amino]phenoxy}-6-methoxy-7-quinolinyl)oxy]butoxy}butoxy)acetyl]-3-methyl-L-valyl-(4R)-4-hydroxy-N-[4-(4-methyl-1,3-thiazol-5-yl)benzyl]-L-prolinamide; L-Prolinamide, N-[2-[4-[4-[[4-[2-fluoro-4-[[[1-[[(4-fluorophenyl)amino]carbonyl]cyclopropyl]carbonyl]amino]phenoxy]-6-methoxy-7-quinolinyl]oxy]butoxy]butoxy]acetyl]-3-methyl-L-valyl-4-hydroxy-N-[[4-(4-methyl-5-thiazolyl)phenyl]methyl]-, (4R)-; SJFa PROTAC; SJFalpha PROTAC; SJFα PROTAC; SJF-6696
- Properties
  - Boiling Point
    
    1230.3±65.0°C at 760 mmHg
    
    Density
    
    1.3±0.1 g/cm3
    
    InChI Key
    
    GXDYWQXTEYENEU-WFYKIECOSA-N
    
    InChI
    
    InChI=1S/C59H67F2N7O11S/c1-36-52(80-35-64-36)38-12-10-37(11-13-38)32-63-54(71)46-29-42(69)33-68(46)55(72)53(58(2,3)4)67-51(70)34-77-26-7-6-24-76-25-8-9-27-78-50-31-45-43(30-49(50)75-5)47(20-23-62-45)79-48-19-18-41(28-44(48)61)66-57(74)59(21-22-59)56(73)65-40-16-14-39(60)15-17-40/h10-20,23,28,30-31,35,42,46,53,69H,6-9,21-22,24-27,29,32-34H2,1-5H3,(H,63,71)(H,65,73)(H,66,74)(H,67,70)/t42-,46+,53-/m1/s1
    
    Canonical SMILES
    
    CC1=C(SC=N1)C2=CC=C(C=C2)CNC(=O)C3CC(CN3C(=O)C(C(C)(C)C)NC(=O)COCCCCOCCCCOC4=CC5=NC=CC(=C5C=C4OC)OC6=C(C=C(C=C6)NC(=O)C7(CC7)C(=O)NC8=CC=C(C=C8)F)F)O
    
    Pub Chem ID
    
    137628677
- Reference Reading
  - 1. Differential PROTAC substrate specificity dictated by orientation of recruited E3 ligase.
    
    Smith, B.E., Wang, S.L., Jaime-Figueroa, S., Harbin, A., Wang, J., Hamman, B.D. and Crews, C.M., 2019. Nature communications, 10(1), pp.1-13.
    
    PROteolysis-TArgeting Chimeras (PROTACs) are hetero-bifunctional molecules that recruit an E3 ubiquitin ligase to a given substrate protein resulting in its targeted degradation. Many potent PROTACs with specificity for dissimilar targets have been developed; however, the factors governing degradation selectivity within closely-related protein families remain elusive. Here, we generate isoform-selective PROTACs for the p38 MAPK family using a single warhead (foretinib) and recruited E3 ligase (von Hippel-Lindau). Based on their distinct linker attachments and lengths, these two PROTACs differentially recruit VHL, resulting in degradation of p38α or p38δ. We characterize the role of ternary complex formation in driving selectivity, showing that it is necessary, but insufficient, for PROTAC-induced substrate ubiquitination. Lastly, we explore the p38δ:PROTAC:VHL complex to explain the different selectivity profiles of these PROTACs. Our work attributes the selective degradation of two closely-related proteins using the same warhead and E3 ligase to heretofore underappreciated aspects of the ternary complex model.
- Preparing Stock Solutions
  - ConcentrationVolumeMass 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

ConcentrationVolumeMass	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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