1. Apoptosis
    Autophagy
  2. Caspase
    Autophagy
    Apoptosis
  3. PAC-1

PAC-1 (Synonyms: Procaspase activating compound 1)

Cat. No.: HY-13523 Purity: 99.93%
Handling Instructions

PAC-1 is a procaspase-3 activator that induces apoptosis in cancer cells with an EC50 of 2.08 μM.

For research use only. We do not sell to patients.

PAC-1 Chemical Structure

PAC-1 Chemical Structure

CAS No. : 315183-21-2

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 55 In-stock
Estimated Time of Arrival: December 31
10 mg USD 50 In-stock
Estimated Time of Arrival: December 31
50 mg USD 140 In-stock
Estimated Time of Arrival: December 31
100 mg USD 250 In-stock
Estimated Time of Arrival: December 31
500 mg USD 1000 In-stock
Estimated Time of Arrival: December 31
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Customer Review

Based on 4 publication(s) in Google Scholar

Top Publications Citing Use of Products

    PAC-1 purchased from MCE. Usage Cited in: Oncotarget. 2017 Feb 14;8(7):12311-12322.

    NB4 cells are treated with 5 μM Z-10 or 50 μM PAC-1 for the indicated time, and the expression of PML-RARα and cleaved caspase3 is analyzed by western blot.
    • Biological Activity

    • Protocol

    • Purity & Documentation

    • References

    • Customer Review

    Description

    PAC-1 is a procaspase-3 activator that induces apoptosis in cancer cells with an EC50 of 2.08 μM.

    IC50 & Target[1]

    Procaspase-3

    2.08 μM (EC50)

    In Vitro

    PAC-1 activates procaspase-3 with an EC50 of 2.08 μM. PAC-1 exhibits an enhanced zinc chelating ability (EC50= 7.08 μM). PAC-1 induces leukemia cell death with IC50 of 4.03 μM, which is consistent with the values reported by other investigators. PAC-1 treatment also results in death of other malignant cells in a concentration-dependent manner with IC50s ranging from 4.03 to 53.44μM. The overall mean IC50 in the fifteen malignant cell lines is 0.88 mM for WF-210 and 19.40 μM for PAC-1. In contrast, the sensitivity of the normal human cells (PBL, L-02, HUVEC and MCF 10A) to WF-210 is 2.6-fold lower (mean IC50=412.34 μM) than PAC-1 (mean IC50=158.29 μM)[1]. Procaspase-activating compound-1 (PAC-1) is the first direct caspase-activating compound discovered. PAC-1 treatment upregulates Ero1α in multiple cell lines, whereas silencing of Ero1α significantly inhibits calcium release from ER and cell death[2].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    In Vivo

    To evaluate the in vivo effect of WF-210 on the growth of malignant tumors, we examined the ability of WF-210 to suppress tumor growth in mouse Hep3B and MDA-MB-435 xenograft models. These two cell lines express procaspase-3 at relatively high levels. Tumors induced by xenografts of the liver cancer cell Hep3B are allowed to develop and grow to a size of 100 mm3, after which WF-210 (2.5 mg/kg) or PAC-1 (5.0 mg/kg) is given daily for two weeks by intravenous (i.v.) administration. As shown in both PAC-1 and WF-210 significantly inhibits the growth of Hep3B tumor xenografts[1].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    Clinical Trial
    Molecular Weight

    392.49

    Formula

    C₂₃H₂₈N₄O₂

    CAS No.

    315183-21-2

    SMILES

    O=C(N/N=C/C1=CC=CC(CC=C)=C1O)CN2CCN(CC3=CC=CC=C3)CC2

    Shipping

    Room temperature in continental US; may vary elsewhere.

    Storage
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 6 months
    -20°C 1 month
    Solvent & Solubility
    In Vitro: 

    DMSO : 50 mg/mL (127.39 mM; Need ultrasonic)

    H2O : < 0.1 mg/mL (insoluble)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 2.5478 mL 12.7392 mL 25.4784 mL
    5 mM 0.5096 mL 2.5478 mL 5.0957 mL
    10 mM 0.2548 mL 1.2739 mL 2.5478 mL
    *Please refer to the solubility information to select the appropriate solvent.
    In Vivo:
    • 1.

      Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

      Solubility: ≥ 2.5 mg/mL (6.37 mM); Clear solution

    • 2.

      Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

      Solubility: 2.5 mg/mL (6.37 mM); Suspended solution; Need ultrasonic

    • 3.

      Add each solvent one by one:  10% DMSO    90% corn oil

      Solubility: ≥ 2.5 mg/mL (6.37 mM); Clear solution

    *All of the co-solvents are provided by MCE.
    References
    Kinase Assay
    [1]

    Various concentrations of WF-210 or PAC-1 are added to procaspase-3 in buffer containing 50 mM HEPES, 0.1% CHAPS, 10% glycerol, 100 mM NaCl, 0.1 mM EDTA, 10 mM DTT pH 7.4,and incubated for 12 h at 37°C. The final volume is 10 mL and the final concentration of procaspase-3 is 1 mM. Then 40 mL of the substrate Ac-DEVD-pNA (final concentration 0.4 mM) in buffer containing 50 mM HEPES pH 7.4, 100 mM NaCl, 10 mM DTT, 0.1 mM EDTA disodium salt, 0.10% CHAPS, 10% glycerol is added and the absorbance of the plate is read at 405 nm for a total of 1 h. The slope of the linear portion for each well is determined as the enzyme activity[1].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    Cell Assay
    [1]

    Cell viability is measured using the MTT method or the Cell Titer-Glo luminescent assay. For the MTT assay, the cells (1×105 cells/mL) are seeded into 96- well culture plates. After overnight incubation, cells are treated with various concentrations of agents (PAC-1, WF-210 or other agents) for 24 or 72 h. Then 10 mL MTT solution (2.5 mg/mL in PBS) is added to each well, and the plates are incubated for an additional 4 h at 37°C. After centrifugation (2500 rpm, 10min), the medium containing MTT is aspirated, and100mL DMSO is added. The optical density of each well is measured at 570 nm with a Biotek Synergy HT Reader. The Cell Titer-Glo kit is used to determine the relative levels of intracellular ATP as a biomarker for live cells[1].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    Animal Administration
    [1]

    Mice[1]
    To determine the in vivo anti-tumor activity of WF-210, viable human gallbladder cancer GBC-SD cells (5×106/100 mL PBS per mouse), human breast cancer MDA-MB-435 cells (1×107/100 mL PBS per mouse), human liver cancer Hep3B cells (5×106/100 mL PBS per mouse) and human breast cancer MCF-7 cells (1×107/100 mL PBS per mouse) are subcutaneously (s.c.) injected into the right flank of 7- to 8-week old male SCID mice or Balb/c nude mice. Cell numbers are confirmed by trypan blue staining prior to injection. Specially, MCF-7 xenograft mice are also administered with the hormone 17-beta-estradiol (3 mg/kg) on alternate days. When the average s.c. tumor volume reached 100 mm3, mice are randomly divided into various treatment and control groups (eight mice per group). Tumor size is measured once every two days with a caliper (calculated volume=shortest diameter2×longest diameter/2). Body weight, diet consumption and tumor size are recorded once every two days. After two or four weeks, mice are sacrificed and tumors are excised and stored at -80°C until further analysis.

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    References
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    Keywords:

    PAC-1Procaspase activating compound 1PAC1PAC 1Procaspase activating compound1Procaspase activating compound-1CaspaseAutophagyApoptosisInhibitorinhibitorinhibit

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