Cat. No.: HY-189386

Pyroptosis inducer-1

Pyroptosis inducer-1 is a pyroptosis inducer. Pyroptosis inducer-1 promotes STING phosphorylation, NF-κB activation, caspase-1-dependent pyroptosis, GSDMD cleavage, mitochondrial membrane potential disruption, ROS production, S phase cell cycle arrest, ER stress, calcium release, and immunogenic cell death accompanied by CRT exposure, HMGB1 release, and ATP secretion. Pyroptosis inducer-1 enters cancer cells via endocytosis and accumulates in mitochondria and endoplasmic reticulum. Pyroptosis inducer-1 increases dendritic cells and CD8⁺ T cells while decreasing regulatory T cells. Pyroptosis inducer-1 can be used for breast cancer research.

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

CAS No.: 3081319-75-4
Formula: C₅₄H₄₆ClF₈N₈O₂PRu
Molecular Weight:1158.48

Storage:

Please store the product under the recommended conditions in the Certificate of Analysis.

Pyroptosis inducer-1 Chemical Structure

CAS No.: 3081319-75-4

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Use of MCE Products

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Purity & Documentation
References
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Bioz

Biological Activity

Description

All NF-κB Isoforms :

All Caspase Isoforms :

Cellular Effect

Cell Line	Type	Value	Description	References
MCF7	IC50	1.43 μM	Antiproliferative activity against human breast cancer MCF-7 cells assessed as reduction in cell viability incubated for 48 hrs. Antiproliferative activity against human breast cancer MCF-7 cells assessed as reduction in cell viability incubated for 48 hrs.	42570373
143B	IC50	1.36 μM	Antiproliferative activity against human osteosarcoma 143B cells assessed as reduction in cell viability incubated for 48 hrs. Antiproliferative activity against human osteosarcoma 143B cells assessed as reduction in cell viability incubated for 48 hrs.	42570373
Caco-2	IC50	3.40 μM	Antiproliferative activity against human colorectal cancer Caco-2 cells assessed as reduction in cell viability incubated for 48 hrs. Antiproliferative activity against human colorectal cancer Caco-2 cells assessed as reduction in cell viability incubated for 48 hrs.	42570373
HeLa	IC50	1.27 μM	Antiproliferative activity against human cervical cancer HeLa cells assessed as reduction in cell viability incubated for 48 hrs. Antiproliferative activity against human cervical cancer HeLa cells assessed as reduction in cell viability incubated for 48 hrs.	42570373
HepG2	IC50	1.75 μM	Antiproliferative activity against human hepatocellular carcinoma HepG2 cells assessed as reduction in cell viability incubated for 48 hrs. Antiproliferative activity against human hepatocellular carcinoma HepG2 cells assessed as reduction in cell viability incubated for 48 hrs.	42570373
MCF-10A	IC50	4.72 μM	Antiproliferative activity against non-tumorigenic human mammary epithelial MCF-10A cells assessed as reduction in cell viability incubated for 48 hrs. Antiproliferative activity against non-tumorigenic human mammary epithelial MCF-10A cells assessed as reduction in cell viability incubated for 48 hrs.	42570373

In Vitro

Anti-cancerMitochondrial FunctionOxidative StressCell Cycle RegulationPyroptosisEndoplasmic Reticulum Stress

Anti-cancer

Pyroptosis inducer-1 (Ru3) (48 h) exhibits potent broad-spectrum antiproliferative activity against human cancer cell lines, including MCF-7, with IC₅₀ values ranging from 1.27 to 3.40 μM^[1].
Pyroptosis inducer-1 (2 μM; 30 min-4 h) rapidly enters MCF-7 cells via an endocytosis-associated pathway and preferentially accumulates in the mitochondria and endoplasmic reticulum^[1].

Mitochondrial Function

Anti-cancer

Pyroptosis inducer-1 (2-6 μM; 8 h) induces significant mitochondrial membrane depolarization and dysfunction in MCF-7 cells^[1].
Pyroptosis inducer-1 (2-6 μM) effectively induces the release of multiple DAMPs (CRT exposure, HMGB1 release, ATP secretion) in MCF-7 cells, thereby triggering ICD-related responses^[1].
Pyroptosis inducer-1 (2-6 μM) effectively activates the cGAS-STING signaling pathway in MCF-7 cells, potentially exerting antitumor immunomodulatory effects^[1].

Oxidative Stress

Anti-cancer

Pyroptosis inducer-1 (2-6 μM) induces pronounced intracellular oxidative stress through massive ROS accumulation in MCF-7 cells^[1].

Anti-cancer

Cell Cycle Regulation

Pyroptosis inducer-1 (2-6 μM; 24 h) disrupts normal cell cycle progression and inhibits the proliferative capacity of MCF-7 cells through induction of S-phase arrest^[1].

Anti-cancer

Pyroptosis

Pyroptosis inducer-1 (2-6 μM; 8-24 h) triggers caspase-1-dependent pyroptosis in MCF-7 cells, characterized by morphological changes and release of pro-inflammatory cytokines^[1].

Endoplasmic Reticulum Stress

Anti-cancer

Pyroptosis inducer-1 (2-6 μM; 6 h) effectively induces ER stress in MCF-7 cells, characterized by calcium release and activation of the eIF2α-ATF4-Chop signaling axis^[1].

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

Immunofluorescence^[1]

Cell Line:

MCF-7
Concentration:

2 μM
Incubation Time:

30 min; 4 h; 1 h
Result:

Intracellular red fluorescence was detectable after 30 min, with intense distribution in the cytoplasm after 4 h.
Colocalized significantly with mitochondrial (PCC = 0.68) and ER (PCC = 0.73) probes, but showed limited overlap with lysosomal probe (PCC = 0.49).

Cell Cycle Analysis^[1]

Cell Line:

MCF-7
Concentration:

2 μM; 4 μM; 6 μM
Incubation Time:

24 h
Result:

Markedly induced S-phase arrest.
The proportion of cells in the S phase increased from 25.8% in the control group to 41.1% following treatment with 6 μM Ru3.
The percentage of cells in the G2/M phase decreased from 26.3% to 16.2%.

ELISA Assay^[1]

Cell Line:

MCF-7
Concentration:

2 μM; 4 μM; 6 μM
Incubation Time:

8 h; 24 h
Result:

Treated cells exhibited typical pyroptotic morphological features including cellular swelling, membrane disruption, and bubble-like protrusions.
ELISA showed significantly elevated extracellular levels of IL-6, TNF-α, and IFN-β.
NSA pretreatment attenuated Ru3-induced cytotoxicity.
Western blot demonstrated concentration-dependent upregulation of Cleaved-Caspase-1 and increased GSDMD-N expression.

Immunofluorescence^[1]

Cell Line:

MCF-7
Concentration:

2 μM; 4 μM; 6 μM
Incubation Time:

6 h
Result:

Increased the fluorescence intensity of Fluo-3 (HY-126821) in a concentration-dependent manner.

In Vivo

Anti-cancerAdaptive ImmunityImmune Tolerance & Immunosuppression

Anti-cancer

Adaptive Immunity

Immune Tolerance & Immunosuppression

Pyroptosis inducer-1 (Ru3) (6 μM; s.c.; single dose) vaccination induces potent antitumor immunity in vivo, achieving a tumor growth inhibition rate of 86.69% on day 30 and significantly enhancing infiltration of DCs and CD8⁺ T cells while reducing immunosuppressive Tregs^[1].

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

Animal Model:

BALB/c (female)^[1]
Dosage:

6 μM
Administration:

s.c.; single dose
Result:

Inhibited tumor growth with a tumor growth inhibition rate of 80.21% on day 16 and 86.69% on day 30.
Increased the proportion of CD11c+ dendritic cells in the spleen by approximately 2.5-fold.
Increased the number of CD4+ T cells in the spleen and tumors by approximately 5.9-fold and 3.6-fold, respectively.
Increased the proportion of CD8+ T cells in the spleen and tumors by approximately 5.9-fold and 3.2-fold, respectively.
Reduced the proportion of regulatory T cells (Tregs) in the spleen and tumors, which were approximately 3.4-fold and 6.2-fold higher in control mice, respectively.

Related Protocols :

Chemical Information

CAS No. 3081319-75-4
Molecular Weight 1158.48
Formula C₅₄H₄₆ClF₈N₈O₂PRu
SMILES

O=C(COCCN1CCN(C(C2=CC=C(C=C2)Cl)C3=CC=CC=C3)CC1)NC4=CC5=CC=C[N]6=C5C7=[N]([Ru+2]689([N]%10=C(C%11=[N]9C=CC=C%11)C=CC=C%10)[C-]%12=C(C%13=[N]8C=CC=C%13)C(F)=CC(F)=C%12)C=CC=C74.[F-][P+5]([F-])([F-])([F-])([F-])[F-]
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation

Handling Instructions (2659 KB)

References

[1]. Zhang Y, et al. Ruthenium(II) complex enhances anti-breast cancer immune responses by inducing pyroptosis and immunogenic cell death while activating the cGAS-STING pathway. Bioorganic chemistry. 2026 Oct 05;181:110347. [Content Brief]

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Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

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Pyroptosis inducer-1

All NF-κB Isoforms

All Caspase Isoforms