Free shipping on all orders over $ 500

PAC-1

Cat. No. M1867

PAC-1 Structure
Size Price Availability Quantity
10mg USD 60 In stock
50mg USD 170 In stock
100mg USD 280 In stock
Bulk Inquiry?

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.

Protocol
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
References

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.

Related Caspase Products
BOC-D-FMK

Boc-D-FMK is a cell-permeable, irreversible and broad spectrum caspase inhibitor; inhibits apoptosis stimulated by TNF-α with an IC50 of 39 µM.

Emricasan

Emricasan is a potent irreversible pan-caspase inhibitor.

NQDI-1

NQDI-1 is a selective inhibitor of ASK1 with a Ki of 500 nM.

VX-765

VX-765 is a potent and selective inhibitor of caspase-1 with Ki of 0.8 nM.

Betulinic acid

Betulinic acid is a pentacyclic triterpene which selectively induces apoptosis in tumor cells.It is a inhibitor of HIV-1 with EC50 of 1.4 μM.

  Catalog
Abmole Inhibitor Catalog 2017




Keywords: PAC-1 supplier, Caspase, inhibitors

Contact Us

Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2017 AbMole BioScience. All Rights Reserved.