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

PAC-1  (Synonyms: Procaspase activating compound 1)

Cat. No.: HY-13523 Purity: 99.93%
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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
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 37 In-stock
Solution
10 mM * 1 mL in DMSO USD 37 In-stock
Solid
5 mg USD 34 In-stock
10 mg USD 55 In-stock
50 mg USD 154 In-stock
100 mg USD 275 In-stock
500 mg USD 1100 In-stock
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Based on 7 publication(s) in Google Scholar

PAC-1 Related Antibodies

Top Publications Citing Use of Products

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

    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.

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    View All Isoforms
    Caspase 1 Caspase 2 Caspase 3 Caspase 4 Caspase 5 Caspase 6 Caspase 7 Caspase 8 Caspase 9 Caspase 10 Caspase 12 Caspase Caspase 11 Caspase-13

    • 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].

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

    PAC-1 Related Antibodies
    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].

    MedChemExpress (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.
    Appearance

    Solid

    Color

    White to yellow

    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 2 years
    -20°C 1 year
    Solvent & Solubility
    In Vitro: 

    DMSO : 50 mg/mL (127.39 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    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
    View the Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

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    Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

    Mass
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    Concentration
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    Volume
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    Molecular Weight *

    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

    C1

    ×
    Volume (start)

    V1

    =
    Concentration (final)

    C2

    ×
    Volume (final)

    V2

    In Vivo:

    Select the appropriate dissolution method based on your experimental animal and administration route.

    For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
    To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
    The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

    • Protocol 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

      This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

      Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
    • Protocol 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

      This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

      Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
    In Vivo Dissolution Calculator
    Please enter the basic information of animal experiments:

    Dosage

    mg/kg

    Animal weight
    (per animal)

    g

    Dosing volume
    (per animal)

    μL

    Number of animals

    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Please enter your animal formula composition:
    %
    DMSO +
    % 
    +
    %
    Tween-80 +
    %
    Saline
    Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
    The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
    Calculation results:
    Working solution concentration: mg/mL
    Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
    The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
    Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
     If the continuous dosing period exceeds half a month, please choose this protocol carefully.
    Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
    Purity & Documentation

    Purity: 99.93%

    COA (242 KB) HNMR (200 KB) LCMS (111 KB)

    Handling Instructions (2659 KB)
    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

    Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 2.5478 mL 12.7392 mL 25.4784 mL 63.6959 mL
    5 mM 0.5096 mL 2.5478 mL 5.0957 mL 12.7392 mL
    10 mM 0.2548 mL 1.2739 mL 2.5478 mL 6.3696 mL
    15 mM 0.1699 mL 0.8493 mL 1.6986 mL 4.2464 mL
    20 mM 0.1274 mL 0.6370 mL 1.2739 mL 3.1848 mL
    25 mM 0.1019 mL 0.5096 mL 1.0191 mL 2.5478 mL
    30 mM 0.0849 mL 0.4246 mL 0.8493 mL 2.1232 mL
    40 mM 0.0637 mL 0.3185 mL 0.6370 mL 1.5924 mL
    50 mM 0.0510 mL 0.2548 mL 0.5096 mL 1.2739 mL
    60 mM 0.0425 mL 0.2123 mL 0.4246 mL 1.0616 mL
    80 mM 0.0318 mL 0.1592 mL 0.3185 mL 0.7962 mL
    100 mM 0.0255 mL 0.1274 mL 0.2548 mL 0.6370 mL
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    PAC-1 Related Classifications

    Help & FAQs
    • Do most proteins show cross-species activity?

      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

    Keywords:

    PAC-1315183-21-2Procaspase activating compound 1PAC1PAC 1Procaspase activating compound1Procaspase activating compound-1CaspaseAutophagyApoptosisInhibitorinhibitorinhibit

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