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Cat. No. M1867
PAC-1 Structure

Procaspase activating compound 1

Size Price Availability Quantity
Free Sample (0.5-1 mg)  USD 0 In stock
10mg USD 60 In stock
50mg USD 170 In stock
100mg USD 280 In stock
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Quality Control
Biological Activity

PAC-1 is a procaspase-activating compound; activates procaspase-3 to produce caspase-3 (EC50 = 0.22 μM). PAC-1 enhances the activity of procaspase-3 in vitro and induces apoptotic death in cancer cells in culture and in mouse xenograft models. Signaling through the neuropeptide GPCR PAC(1) induces neuritogenesis via a single linear cAMP- and ERK-dependent pathway using a novel cAMP sensor. The data presented herein further bolster the hypothesis that PAC-1 induces apoptosis in cancer cells through the direct activation of procaspase-3, has implications for the design and discovery of next-generation procaspase-3 activating compounds, and sheds light on the anti-apoptotic role of cellular zinc.

Customer Product Validations & Biological Datas
Source Exp Hematol (2015). Figure 2.PAC-1
Method flow cytometry
Cell Lines MM cell lines
Concentrations 3 and 10 μmol/L
Incubation Time 24 hours
Results Both MM.1S and U266 cells demonstrated a time-dependent decrease in cell viability.
Cell Experiment
Cell lines U-937, HL-60, CRL-1872, ACHN, NCI-H226, Hs888Lu, Hs578Bst, MCF-10A, SK-MEL-5, BT-20, MDA-MB-231, UACC-62, SK-N-SH, B16-F10 , Hs 578t and PC-12
Preparation method Determination of IC50 values in various cell lines.
Various concentrations of etoposide or PAC-1 were added to cells and incubated for 24 h and 72 h for etoposide and PAC-1, respectively. Cell death was quantified by the addition of MTS/PMS CellTiter 96 Cell Proliferation Assay reagent (Promega). The plates were incubated at 37 1C for approximately 1 h (until the colored product formed), and the absorbance was measured at 490 nm.
Concentrations 0~20 µM
Incubation time 24 h and 72 h
Animal Experiment
Animal models nude mice bearing NCI-H226 xenograft model
Formulation mixture of 24:1 vegetable oil/DMSO
Dosages 50 and 100 mg/kg once a day for 21 d
Administration oral gavage
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 392.5
Formula C23H28N4O2
CAS Number 315183-21-2
Purity 98.72%
Solubility DMSO ≥48 mg/mL
Storage at -20°C

Signaling through the neuropeptide GPCR PAC1 induces neuritogenesis via a single linear cAMP- and ERK-dependent pathway using a novel cAMP sensor.
Emery et al. FASEB J. 2012 Aug;26(8):3199-211. PMID: 22532442.

Procaspase-3 activation as an anti-cancer strategy: structure-activity relationship of procaspase-activating compound 1 (PAC-1) and its cellular co-localization with caspase-3.
Peterson et al. J Med Chem. 2009 Sep 24;52(18):5721-31. PMID: 19708658.

Small-molecule activation of procaspase-3 to caspase-3 as a personalized anticancer strategy.
Putt KS, et al. Nat Chem Biol. 2006 Oct;2(10):543-50. PMID: 16936720.

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Keywords: PAC-1, Procaspase activating compound 1 supplier, Caspase, inhibitors

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