Difopein 

Difopein is a 14-3-3 protein inhibitor. Difopein acts as an apoptosis inducer, regulates apoptosis-related proteins, downregulates Bcl-2, upregulates Bax, activates caspase-9 and caspase-3, and induces nuclear fragmentation, membrane-enclosed apoptotic bodies and DNA ladder formation. Difopein serves as a tumor growth inhibitor, which inhibits the proliferation of glioma cells and induces their apoptosis in in vivo nude mouse models. Difopein is applicable to glioma-related research^[1].

Difopein (24-48 h) induces time-dependent apoptosis in human U251 and U87 glioma cells, causes time-dependent increases in both early and late apoptosis, and triggers apoptotic DNA fragmentation in U251 cells^[1].
Difopein (24-48 h) alters the cell cycle distribution of U251 cells, causing time-dependent cell arrest at the G1 phase, while the proportions of cells in the S and G2 phases decrease; at 24 h and 48 h post-transfection, the proportions of G1-phase cells reach 73.9% and 84.8%, respectively^[1].
Difopein (24-48 h) downregulates the anti-apoptotic protein Bcl-2 and upregulates the pro-apoptotic protein Bax at both mRNA and protein levels, and activates caspase-9 and caspase-3 in human U251 glioma cells^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Difopein (~5×10⁶ cfu/mL; intratumoral injection) inhibits tumor growth by 79.0% and reduces tumor cell proliferation while increasing apoptosis in athymic BALB/c nude mice^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

6387.13

C₂₇₃H₄₂₄N₇₆O₈₉S₆

396834-58-5

Ser-Ala-Asp-Gly-Ala-Pro-His-Cys-Val-Pro-Arg-Asp-Leu-Ser-Trp-Leu-Asp-Leu-Glu-Ala-Asn-Met-Cys-Leu-Pro-Gly-Ala-Ala-Gly-Leu-Asp-Ser-Ala-Asp-Gly-Ala-Pro-His-Cys-Val-Pro-Arg-Asp-Leu-Ser-Trp-Leu-Asp-Leu-Glu-Ala-Asn-Met-Cys-Leu-Pro-Gly-Ala-Ala-Gly-Leu-Glu

SADGAPHCVPRDLSWLDLEANMCLPGAAGLDSADGAPHCVPRDLSWLDLEANMCLPGAAGLE

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• [1]. Cao W, et al. Targeting 14-3-3 protein, difopein induces apoptosis of human glioma cells and suppresses tumor growth in mice. Apoptosis. 2010;15(2):230-241.