Q-VD-Oph

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

Q-VD-Oph 是一种有效的泛 caspase 抑制剂，可抑制人重组 caspase-7，在无细胞测定中 IC50 为 48 nM。

Q-VD-Oph is a potent pan-caspase inhibitor, inhibits human recombinant caspase-7 with IC50 of 48 nM in cell-free assay, also inhibits caspase -1, 3, 8, 9, 10, and 12 with IC50 of 25-400 nM; reduces doxorubicin-induced caspase-3 activation, increases expression of p21/WAF1 and senescence -associated -beta-galactosidase activity, but does not alter Akt activation, Q-VD-Oph is significantly more effective in preventing apoptosis than the widely used inhibitors, ZVAD-fmk and Boc-D-fmk; prevents activated caspase-7 and caspase-cleaved fragments of tau in the TgCRND8 brain, as well as pathology associated with TgCRND8 mice.

Q-VD-OPh is a potent inhibitor of caspase-7 with an IC50 of 48 nM utilizing a cell-free assay consisting of human recombinant caspase-7, Q-VD-OPh, and the substrate AMC-DEVD-pNa. Q-VD-OPh fully inhibits caspase-3 and -7 activity at 0.05 μM. Caspase-8 is also inhibited at low Q-VD-OPh concentrations. The cleavage of PARP-1 is fully prevented at 10 μM Q-VD-OPh. DNA fragmentation and disruption of the cell membrane functionality are both prevented at 2 μM Q-VD-OPh. Q-VD-OPh is significantly more effective in preventing apoptosis than the widely used inhibitors, ZVAD-fmk and Boc-D-fmk, and is also equally effective in preventing apoptosis mediated by the three major apoptotic pathways, caspase 9/3, caspase 8/10, and caspase12. Q-VD-OPh is not toxic to cells even at extremely high concentrations. QVD is also able to increase the expression of differentiation markers in acute myeloid leukemia (AmL) blasts. QVD alone or combined with VDDs increases differentiation and HPK1-cJun signaling in AmL cell context-dependent manner.

Chronic treatment with Q-VD-OPh prevents caspase-7 activation and limits the pathological changes associated with tau, including caspase cleavage. Q-VD-OPh could be a potential therapeutic compound for the treatment of Alzheimer's disease.

QVD-OPH | Quinoline-Val-Asp-Difluorophenoxymethylketone

Apoptosis

Caspase

Caspase-1| Caspase-3| Caspase-8| Caspase-9

Inflammation/Immunology

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1135695-98-5

513.49

C26H25F2N3O6

>98% (HPLC)

DMSO: ≥ 25 mg/mL

O=C(O)C[C@H](NC([C@@H](NC(C1=NC2=CC=CC=C2C=C1)=O)C(C)C)=O)C(COC3=C(F)C=CC=C3F)=O

Pentanoic acid, 5-(2,6-difluorophenoxy)-3-[[(2S)-3-methyl-1-oxo-2-[(2-quinolinylcarbonyl)amino]butyl]amino]-4-oxo-, (3S)-

(-20℃)

With Ice Pack

≥ 2 years