SJFα

• CAT Number: I019462
• CAS Number: 2254609-27-1
• Molecular Formula: C₅₉H₆₇F₂N₇O₁₁S
• Molecular Weight: 1120.27
• Purity: ≥95%
• Storage: Store at -20°C
• 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
• 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
• InChIKey: GXDYWQXTEYENEU-WFYKIECOSA-N
• 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

SJFα（Cat No.:I019462） is a linker molecule used in the construction of proteolysis-targeting chimeras (PROTACs). With a 13-atom linker length, SJFα specifically targets and degrades p38α, a member of the p38 MAPK family. It demonstrates potent degradation activity against p38α with a DC50 (dose required for 50% degradation) of 7.16 nM. However, it is significantly less effective in degrading p38δ (DC50=299 nM) and does not induce degradation of the other p38 isoforms (β and γ) even at concentrations up to 2.5 µM. SJFα shows selectivity for p38α degradation within the p38 MAPK family.

Reference

[1]. Smith BE, et al. Differential PROTAC substrate specificity dictated by orientation of recruited E3 ligase. Nat Commun. 2019 Jan 10;10(1):131.