PAC-1

SKU: orb1305385

Description

PAC-1 is a procaspase-3 activating compound investigated as an anticancer agent in preclinical research. It has demonstrated efficacy in inducing apoptosis in vitro and inhibiting tumor growth in vivo across various cancer models, including lymphoma, melanoma, breast, and solid tumors.

Research Area

Cell Biology, Protein Biochemistry

Key Properties

• CAS Number: 315183-21-2
• MW: 392.49
• Purity: 99.77%
• Formula: C₂₃H₂₈N₄O₂
• SMILES: Oc1c(CC=C)cccc1\C=N\NC(=O)CN1CCN(Cc2ccccc2)CC1
• Target: Caspase,Autophagy,Apoptosis
• Solubility: 10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (5.1 mM);DMSO:55 mg/mL (140.13 mM)

Bioactivity

• Target IC50:
  Procaspase-3:0.22 μM(EC50)
• In Vivo:
  PAC-1 was able to induce cell death in a delayed manner in Bax/Bak double knockout cells and Bcl-2 and Bcl-xL overexpressing cells with the same efficacy as its wild-type counterpart.PAC-1 induced the release of cytochrome c in a caspase-3 nondependent manner, which subsequently triggered the downstream activation of caspase-3 and cell death.PAC-1 did not induce cell death in Apaf-1 knockout cells. Apaf-1 knockout cells induced cell death and cystatinase-3 activation, suggesting that apoptosome formation is required for cystatinase-3 activation via PAC-1-mediated cell death.PAC-1 induced apoptosis in primary carcinoma cells with IC50 values ranging from 3 nM to 1.41 μM, and was more potent than that in neighboring noncancerous cells with IC50 values ranging from 5.02 μM to 9.98 μM, which is also consistent with procaspase-1-induced apoptosis in primary cancer cells with IC50 values ranging from 3 nM to 1.41 μM. This was also directly related to the concentration of procaspase-3. PAC-1 activated procaspase-3, producing caspase-3 with an EC50 of 0.22 μM, and activated procaspase-7 with an EC50 of 4.5 μM. Increased levels of caspase 3 in the cancer cell lines caused PAC-1 to selectively induce apoptosis according to the ratio of the concentration of procaspase-3 to the concentration of procaspase-3. PAC-1 selectively induces apoptosis in a manner proportional to procaspase-3 concentration, with an IC50 of 0.35 μM in NCI-H226 cells and approximately 3.5 μM in UACC-62 cells.PAC-1 activates cystatinase-3 by chelating zinc ions, which attenuates zinc-mediated inhibition and permits the self-activation of cystatinogen-3 to cystatinase-3.PAC-1 is also known to activate cystatinogen-3 by chelating zinc ions, which is a zinc-mediated inhibition.
• In Vitro:
  PAC-1 was able to induce cell death in a delayed manner in Bax/Bak double knockout cells and Bcl-2 and Bcl-xL overexpressing cells with the same efficacy as its wild-type counterpart.PAC-1 induced the release of cytochrome c in a caspase-3 nondependent manner, which subsequently triggered the downstream activation of caspase-3 and cell death.PAC-1 did not induce cell death in Apaf-1 knockout cells. Apaf-1 knockout cells induced cell death and cystatinase-3 activation, suggesting that apoptosome formation is required for cystatinase-3 activation via PAC-1-mediated cell death.PAC-1 induced apoptosis in primary carcinoma cells with IC50 values ranging from 3 nM to 1.41 μM, and was more potent than that in neighboring noncancerous cells with IC50 values ranging from 5.02 μM to 9.98 μM, which is also consistent with procaspase-1-induced apoptosis in primary cancer cells with IC50 values ranging from 3 nM to 1.41 μM. This was also directly related to the concentration of procaspase-3. PAC-1 activated procaspase-3, producing caspase-3 with an EC50 of 0.22 μM, and activated procaspase-7 with an EC50 of 4.5 μM. Increased levels of caspase 3 in the cancer cell lines caused PAC-1 to selectively induce apoptosis according to the ratio of the concentration of procaspase-3 to the concentration of procaspase-3. PAC-1 selectively induces apoptosis in a manner proportional to procaspase-3 concentration, with an IC50 of 0.35 μM in NCI-H226 cells and approximately 3.5 μM in UACC-62 cells.PAC-1 activates cystatinase-3 by chelating zinc ions, which attenuates zinc-mediated inhibition and permits the self-activation of cystatinogen-3 to cystatinase-3.PAC-1 is also known to activate cystatinogen-3 by chelating zinc ions, which is a zinc-mediated inhibition.
• Cell Research:
  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)

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

Procaspase activating compound 1, Procaspase activating compound1, Procaspase activating compound-1, Procaspase-3, Apoptosis, Autophagy, Caspase, Inhibitor, PAC 1, PAC1, PAC-1, inhibit

Compound Identifiers

PubChem CID

135421197