PAC1 Inhibitor CAS No. 315183-21-2

Cat. No.	Name	Size	Price
KI1088	PAC1	10 mg	$144
	PAC1	50 mg	$200
	PAC1	50 mg	$400
	PAC1	250 mg	$1232

Chemical Characteristic

Product Name	PAC1
CAS No.	315183-21-2
Molecular Weight	392.49
Formula	C₂₃H₂₈N₄O₂
Chemical Name	2-(4-benzylpiperazin-1-yl)-N'-[(Z)-(6-oxo-5-prop-2-enylcyclohexa-2,4-dien-1-ylidene)methyl]acetohydrazide
Smiles	N1(CCN(CC1)Cc1ccccc1)CC(=O)N/N=C/c1c(c(ccc1)CC=C)O
Chemical Structure

Biological activities

PAC-1 is a procaspase-activating compound 1. PAC-1 is a potential agent treatment in cancer cell lines with elevated levels of procaspase-3. In cancer cells, PAC-1 induces primary cancerous cells death with an IC50 of minimal 3 nM.^[1] PAC-1 and zinc form a tight complex with one another, with a dissociation constant of approximately 42 nM. In vitro, PAC-1 activates procaspase-3 by sequestering inhibitory zinc ions. PAC-1 relieves the zinc-mediated inhibition of caspase-7, procaspase-7 and the procaspase-7 (D23A/D198A/D206A) mutant. ^[2] PAC1 specifically dephosphorylates and inactivates MAP kinases. PAC1 is necessary and sufficient for p53-mediated apoptosis. ^[3] In vivo, PAC-1 induces death in cancer cell lines and primary tumor samples in cell culture, and retards tumor growth. ^[2]

References

[1] Putt KS, et al. Small-molecule activation of procaspase-3 to caspase-3 as a personalized anticancer strategy. Nat Chem Biol. 2006, 2(10): 543-550. [2] Peterson QP, et al. PAC-1 activates procaspase-3 in vitro through relief of zinc-mediated inhibition. J Mol Biol. 2009, 388(1): 144-158. [3] Yin Y, et al. PAC1 phosphatase is a transcription target of p53 in signalling apoptosis and growth suppression. Nature. 2003, 422(6931): 527-531.

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