PAC-1 - Moligand™, 10mM in DMSO , Activator of Caspase 3, CAS No.315183-21-2, Activator of Caspase 3

CAS: 315183-21-2 Cat. No.: P408074 Formula: C₂₃H₂₈N₄O₂ Peso molecolare: 392.49 Numero EC: 636-533-6

GRADE & PURITY Moligand™, 10mM in DMSO

Synonyms

(E)-N'-(3-allyl-2-hydroxybenzylidene)-2-(4-benzylpiperazin-1-yl)acetohydrazide

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

Panoramica

Information

PAC-1 is a potentprocaspase-3activator withEC50of 0.22 μM and the first small molecule known to directly activate procaspase-3 to caspase-3.
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. 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. 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.

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.
Cell Data

cell lines：

Concentrations：Dissolved in DMSO, final concentrations ~100 μM

Incubation Time：72 hours

Powder Purity:≥99%

Specifications

Sinonimi

(E)-N'-(3-allyl-2-hydroxybenzylidene)-2-(4-benzylpiperazin-1-yl)acetohydrazide

Specifiche e purezza

Moligand™, 10mM in DMSO

Meccanismi biochimici e fisiologici

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.

Condizioni di conservazione di stoccaggio

Store at -80°C

Spedito in

Dry ice packs + Cold packs

Questo prodotto richiede spedizione a catena fredda. I servizi di terra e altri servizi economici non sono disponibili.

Grado

Moligand™

Tipo di azione

ACTIVATOR

Meccanismo d'azione

Activator of Caspase 3

Nomi e identificatori

• Isomeri SMILES: C=CCC1=C(C(=CC=C1)/C=N/NC(=O)CN2CCN(CC2)CC3=CC=CC=C3)O
• WGK Germania: 3
• Peso molecolare: 392.49
• Reaxy-Rn: 18691810
• Reaxys-RN_link_address: https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=18691810&ln=

Obiettivi associati (umani)

CASP3 Tchem Caspase-3 (0 Activities)

Discover Target: CASP3

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

Proprietà chimiche e fisiche

• Solubilità: Solubility (25°C) In vitro DMSO: 27 mg/mL (198.31 mM); Water: 27 mg/mL (198.31 mM); Ethanol: 27 mg/mL

Riferimenti

1. Zitong Zhao, Ge Ge, Menghan Gong, Yi Liu, Liying Ma, Dongdong Zhang, Li Sun, Yongmei Song.  (2026)  Redox-triggered USP18 confers cisplatin resistance in ovarian cancer by selectively activating a non-canonical FSP1-dependent ferroptosis escape pathway.  Redox Biology,      [PMID:42030646] [10.1016/j.redox.2026.104179]

Domande frequenti

What is Moligand??

Moligand? is one of Aladdin Scientific's premium product lines, formulated for high-purity applications across multiple workflows. Compared to standard grades in the same workflow, Moligand? products typically offer tighter specifications, more rigorous QC, and stronger lot-to-lot consistency.

How should this product be stored?

Store at ?80 °C. Ultra-low temperature storage is required to maintain the specified shelf life.

How is this product shipped?

This product ships frozen with dry ice and cold packs. Unpack on arrival and transfer it to the storage condition stated above; handle dry ice with insulated gloves in a ventilated area.

What are the CAS number, molecular formula and molecular weight?

The CAS Number is 315183-21-2, the molecular formula is C23H28N4O2, and the molecular weight is 392.49 g/mol.

What documentation is provided?

Available product documentation, including Certificates of Analysis (COA), Safety Data Sheets (SDS), and specification sheets, is shown in the product document area. Document availability and access follow the current site policy.