PAC-1

Catalog No.S2738

PAC-1 Chemical Structure

Molecular Weight(MW): 392.49

PAC-1 is a potent procaspase-3 activator with EC50 of 0.22 μM and the first small molecule known to directly activate procaspase-3 to caspase-3.

Size Price Stock Quantity  
In DMSO USD 120 In stock
USD 90 In stock
USD 170 In stock
USD 250 In stock
USD 770 In stock
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1 Customer Review

  • The effects of PAC-1 (activator of ROS) administration on the newborn pups' weight and the plasma IGF-1 and ROS levels in graviditas gp91phox-/- mice. The values are presented as the means ± SD derived from six animals. *P<0.05 in comparison to the non-treatment mice.

    Biol Med, 2015, 7(5).doi: 10.4172/0974-8369.1000259.. PAC-1 purchased from Selleck.

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Biological Activity

Description PAC-1 is a potent procaspase-3 activator with EC50 of 0.22 μM and the first small molecule known to directly activate procaspase-3 to caspase-3.
Features The first small molecule known to directly activate procaspase-3 to caspase-3.
Targets
Procaspase-3 [1]
0.22 μM(EC50)
In vitro

PAC-1 activates procaspase-7 in a less efficient manner with EC50 of 4.5 μM. 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 μM for NCI-H226 cells to ~3.5 μM for UACC-62 cells. PAC-1 induces apoptosis in the primary cancerous cells with IC50 values of 3 nM to 1.41 μM, more potently than in the adjacent noncancerous cells with IC50 of 5.02 μM to 9.98 μM, which is also directly related to the distinct procaspase-3 concentration. [1] 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. [2] 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. [3]

In vivo 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. [1]

Protocol

Kinase Assay:[1]
+ Expand

In vitro procaspase-3 activation:

Procaspase-3 is expressed and purified in Escherichia coli. Various concentrations of PAC-1 are added to 90 μL of a 50 ng/mL of procaspase-3 in caspase assay buffer in a 96-well plate, The plate is incubated for 12 hours at 37 °C. A 10 μL volume of a 2 mM solution of caspase-3 peptidic substrate acetyl Asp-Glu-Val-Asp-p-nitroanilide (Ac-DEVD-pNa) in caspase assay buffer is then added to each well. The plate is read every 2 minutes at 405 nm for 2 hours in a Spectra Max Plus 384 well plate reader. The slope of the linear portion for each well is determined, and the relative increase in activation from untreated control wells is calculated.
Cell Research:[1]
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  • 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
  • Concentrations: Dissolved in DMSO, final concentrations ~100 μM
  • Incubation Time: 72 hours
  • Method: Cells are exposed to various concentrations of PAC-1 for 72 hours. Cell death is quantified by the addition of MTS/PMS CellTiter 96 Cell Proliferation Assay reagent. The plates are incubated at 37 °C for approximately 1 hour (until the colored product formed), and the absorbance is measured at 490 n
    (Only for Reference)
Animal Research:[1]
+ Expand
  • Animal Models: Ovariectomized female athymic BALB/c (nude, nu/nu) mice injected subcutaneously with ACHN cells, male athymic BALB/c nude mice injected subcutaneously with NCI-H226 cells, and male athymic BALB/c–/– mice injected intravenously with NCI-H226 cells
  • Formulation: Mixed with cholesterol and pelleted into a 3-mm-diameter 20-mg (total weight) pellet, or dissolved in a mixture of 24:1 vegetable oil/DMSO
  • Dosages: ~100 mg/kg
  • Administration: Pellet implantation subcutaneously or oral gavage
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 78 mg/mL (198.73 mM)
Ethanol 16 mg/mL (40.76 mM)
Water Insoluble
In vivo Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
30% PEG400+0.5% Tween80+5% propylene glycol
For best results, use promptly after mixing.
30 mg/mL

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 392.49
Formula

C23H28N4O2

CAS No. 315183-21-2
Storage powder
in solvent
Synonyms N/A

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT02355535 Recruiting Breast Cancer|Lymphoma|Gastrointestinal Cancers|Genitourinary Cancers|Gynecologic Cancers|Head and Neck Cancers|Melanoma|Thoracic Cancers|Solid Tumors|Lymphomas Vanquish Oncology Inc.|University of Illinois at Chicago February 2015 Phase 1
NCT03332355 Recruiting Glioblastoma Multiforme|Anaplastic Astrocytoma Vanquish Oncology Inc.|University of Illinois at Chicago October 1 2017 Phase 1

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID