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.
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- CAS 番号: 3081319-75-4
- 分子式: C54H46ClF8N8O2PRu
- 分子量:1158.48
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
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製品説明
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[1].
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| MCF7 | IC50 |
1.43 μM
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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.
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42570373 |
| 143B | IC50 |
1.36 μM
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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
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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
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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
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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.
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42570373 |
| MCF-10A | IC50 |
4.72 μM
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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.
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42570373 |
体外実験
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].
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].
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]
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Cell Line:MCF-7
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Concentration:2 μM
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Incubation Time:30 min; 4 h; 1 h
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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]
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Cell Line:MCF-7
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Concentration:2 μM; 4 μM; 6 μM
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Incubation Time:24 h
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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]
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Cell Line:MCF-7
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Concentration:2 μM; 4 μM; 6 μM
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Incubation Time:8 h; 24 h
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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]
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Cell Line:MCF-7
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Concentration:2 μM; 4 μM; 6 μM
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Incubation Time:6 h
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Result:Increased the fluorescence intensity of Fluo-3 (HY-126821) in a concentration-dependent manner.
体内実験
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.
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Animal Model:BALB/c (female)[1]
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Dosage:6 μM
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Administration:s.c.; single dose
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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 :
- Western Blot
- Mitochondrial membrane-potential fluorescent assay
- Mammalian live/dead viability and cytotoxicity staining
- ROS/oxidative-stress fluorescent staining
- BrdU Incorporation Assay
- Protocol for Cell Cycle
- Research Protocol for Inflammation-related Diseases
- Breast Cancer Modeling
- Kinase activity and phosphorylation assays
- EdU Incorporation Assay (Click Chemistry-Based DNA Synthesis Measurement)
- Flow cytometric DNA-content cell-cycle staining
- Cell Cytotoxicity Assay
- Fluorescent plasma-membrane potential dye assay
- Mitochondrial membrane-potential and mitochondrial mass staining
- Apoptosis Solutions
- Calcium Spark Assay
- Protocol for Kinase activity and phosphorylation assays
- Monocyte-derived dendritic cell differentiation
- Pyroptosis Solutions
化学情報
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CAS 番号 3081319-75-4
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分子量 1158.48
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分子式 C54H46ClF8N8O2PRu
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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-]
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
純度とドキュメンテーション
バッチを選択:
純度:
99.98%
Assay:
99.98%
ee.:
99.98%
参考文献
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Pyroptosis inducer-1 関連分類
HY-189386 関連分類
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Keywords
- Pyroptosis inducer-1
- 3081319-75-4
- Pyroptosis inducer1
- Pyroptosis inducer 1
- Pyroptosis
- STING
- NF-κB
- Caspase
- Reactive Oxygen Species (ROS)
- Stimulator of Interferon Genes
- TMEM173
- MITA
- ERIS
- MPYS
- Nuclear factor-κB
- Nuclear factor-kappaB
- GSDMD cleavage
- mitochondrial membrane potential disruption
- S-phase cell cycle arrest
- cGAS-STING pathway
- STING phosphorylation
- pyroptosis
- ER stress
- caspase-1-dependent pyroptosis
- ROS generation
- NF-κB activation
- Inhibitor
- inhibitor
- inhibit