||2 years -20¡ãC Powder, 2 weeks4¡ãC in DMSO,6 months-80¡ãC in DMSO
Note: Products for research use only, not for human use
PAC-1 activates procaspase-7 in a less efficient manner with EC50 of 4.5 ¦ÌM. Elevated caspase 3 level in cancer cell lines allows PAC-1 to selectively induce apoptosis in a manner proportional to procaspase-3 concentration with IC50 of 0.35 ¦ÌM For NCI-H226 cells to ~3.5 ¦ÌM For UACC-62 cells. PAC-1 induces apoptosis in the primary cancerous cells with IC50 values of 3 nM to 1.41 ¦ÌM, more potently than in the adjacent noncancerous cells with IC50 of 5.02 ¦ÌM to 9.98 ¦ÌM, which is also directly related to the distinct procaspase-3 concentration. PAC-1 activates procaspase-3 by chelating zinc ions, thus relieving the zinc-mediated inhibition and allowing procaspase-3 to auto-activate itself to caspase-3. PAC-1 is capable to induce cell death in Bax/Bak double-knockout cells and Bcl-2 and Bcl-xL-overexpressing cells with the same efficacy as its wild-type counterpart in a delayed manner. PAC-1 induces cytochrome c release in a caspase-3 independent manner, which subsequently triggers downstream caspase-3 activation and cell death. PAC-1 can not induce cell death and caspase-3 activation in Apaf-1 knockout cells, suggesting that apoptosome Formation is essential For caspase-3 activation by PAC-1-mediated cell death. Administration of PAC-1 at 5 mg with low and steady releasing significantly inhibits the growth of ACHN renal cancer xenograft in mice. Oral administration of PAC-1 (50 or 100 mg/kg) significantly retards tumor growth of NCI-H226 lung cancer xenograft in a dose-dependent manner, and markedly prevents the cancer cells from infiltrating the lung tissue. The in vivo anti-tumor effect of PAC-1 is ascribed to procaspase-3 activation and subsequently apoptosis induction consistent with the activity in vitro. For the detailed information of pac-1, the solubility of pac-1 in water, the solubility of pac-1 in DMSO, the solubility of pac-1 in PBS buffer, the animal experiment (test) of pac-1, the cell expriment (test) of pac-1, the in vivo, in vitro and clinical trial test of pac-1, the EC50, IC50,and Affinity of pac-1, Please contact DC Chemicals.