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pac-1
DC7477  (CAS:315183-21-2)
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100mg USD 450 In stock
250mg USD 900 In stock
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Fields of Application :
PAC-1 is a potent procaspase-3 activator with EC50 of 0.22 M and the first small molecule known to directly activate procaspase-3 to caspase-3.
CAS Number: 315183-21-2
Purity:

>98%

Molecular Weight: 392.49
Molecular Formula: C23H28N4O2
Quality Control: HPLCNMR LC/MS(Please contact us to get the QC report)
Synonyms:
Chemical Name: (E)-N'-(3-allyl-2-hydroxybenzylidene)-2-(4-benzylpiperazin-1-yl)acetohydrazide
Storage: 2 years -20C Powder, 2 weeks4C in DMSO,6 months-80C in DMSO
Note: Products for research use only, not for human use
Description:
PAC-1 activates procaspase-7 in a less efficient manner with EC50 of 4.5 M. 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 M For NCI-H226 cells to ~3.5 M For UACC-62 cells. PAC-1 induces apoptosis in the primary cancerous cells with IC50 values of 3 nM to 1.41 M, more potently than in the adjacent noncancerous cells with IC50 of 5.02 M to 9.98 M, 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.
References:
C(N/N=C/C1=CC=CC(CC=C)=C1O)(=O)CN1CCN(CC2=CC=CC=C2)CC1
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