XJ-4-85

Chemical Structure : XJ-4-85

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货号: PC-27712Not For Human Use, Lab Use Only.

XJ-4-85 is a highly selective, covalent, allosteric phosphofructokinase-1 liver type (PFKL) activator with EC50 of 342.3 nM in substrate assays (4h), releases carnitine palmitoyltransferase 2 (CPT2) inhibitor destabilize cancer cell metabolism.

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25 mg		Get quote
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100 mg		Get quote

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生物&药学活性

XJ-4-85 is a highly selective, covalent, allosteric phosphofructokinase-1 liver type (PFKL) activator with EC50 of 342.3 nM in substrate assays (4h), releases carnitine palmitoyltransferase 2 (CPT2) inhibitor destabilize cancer cell metabolism.
XJ-4-85 selectively modifies K677 in the allosteric effector site to stabilize the R-state tetramer of PFKL.
XJ-4-85 exhibits dose- and time-dependent activation of PFKL.
XJ-4-85 potently engages PFKL in HEK293T cells with IC50 of 141 nM in gel-based competitive ABPP data, but no other detectable PFK1 isoforms.
XJ-4-85 activates glycolysis across multiple cell types, induces rapid alterations in glycolytic metabolism.
XJ-4-85 (5 uM. 2h) markedly elevated intracellular FBP levels in THP-1, Jurkat, MOLM-14 and SH-SY5Y cells relative to vehicle control.
XJ-4-85 releases a selective CPT2-targeting payload, inhibits cell proliferation against B16-F10-Luc2 and MOLM-14 cells with IC50 of ~2 uM.
XJ-4-85 (10-50 mg/kg, intraperitoneal injection) inhibits melanoma tumor outgrowth in C57BL/6 mice bearing B16-F10-Luc2 tumors.

物理化学性质&存储条件

分子量	628.64
分子式	C31H28F4N4O4S
外观性状	Solid
CAS No.
储存条件	固体粉末 -20°C 12 个月; 4°C 6 个月	配置液 -80°C 6 个月; -20°C 6 个月
Shipping
Solubility	10 mM in DMSO
Chemical Name/SMILES	Piperidine, 1-[4-[1-(1,3-benzodioxol-5-ylsulfonyl)-1H-1,2,3-triazol-4-yl]butyl]-4-[bis(3,4-difluorophenyl)methylene]-

参考文献

1. Jiang X, et al. A covalent PFKL activator suppresses tumor growth. Nat Chem Biol. 2026 Aug 5. doi: 10.1038/s41589-026-02289-9.

XJ-4-85

生物&药学活性

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XJ-4-85

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