2. Immunology/Inflammation Apoptosis NF-κB
  3. STING Apoptosis IKK IFNAR NF-κB
  4. MSA-2-Pt

MSA-2-Pt, platinum salt-modified MSA-2 (HY-136927), is a STING agonist. MSA-2-Pt inducing cell
death by platinum and activating the STING pathway by MSA-2. MSA-2-Pt direct activates STING pathway, induces phosphorylation of TBK1, IRF3, and NF-κB p65. MSA-2-Pt enhances tumor infiltration of CD4+ and CD8+ T cells, and induces tumor cell death and apoptosis in mouse colon carcinoma and melanoma models.

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MSA-2-Pt

MSA-2-Pt Chemical Structure

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MSA-2-Pt Related Antibodies

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Description

MSA-2-Pt, platinum salt-modified MSA-2 (HY-136927), is a STING agonist. MSA-2-Pt inducing cell
death by platinum and activating the STING pathway by MSA-2. MSA-2-Pt direct activates STING pathway, induces phosphorylation of TBK1, IRF3, and NF-κB p65. MSA-2-Pt enhances tumor infiltration of CD4+ and CD8+ T cells, and induces tumor cell death and apoptosis in mouse colon carcinoma and melanoma models[1].

IC50 & Target[1]

TBK1

 

IRF3

 

In Vitro

MSA-2-Pt (25-300 μM; 12-24 h) induces dose-dependent cell death in mouse colon adenocarcinoma MC38 cells, with significant cytotoxicity observed at concentrations ≥75 μM after 24 h[1].
MSA-2-Pt (10-50 μM; 24 h) activates IFN-β secretion in mouse macrophage RAW264.7 cells[1].
MSA-2-Pt (10-50 μM; 3 h) activates the STING signaling pathway in mouse macrophage RAW264.7 cells, inducing phosphorylation of STING, TBK1, IRF3, and NF-κB p65 at concentrations of 10, 25, and 50 μM after 3 h[1].

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

MSA-2-Pt Related Antibodies

Cell Viability Assay[1]

Cell Line: mouse colon adenocarcinoma MC38 cells
Concentration: 25 μM, 50 μM, 75 μM, 100 μM, 200 μM, 300 μM
Incubation Time: 12; 24 h;
Result: Induced significant MC38 cell death starting at 75 μM, with a dose-dependent reduction in cell viability.
Reduced cell viability to ~20% or lower at 100 μM and above.
Confirmed significant pyroptotic cell death in MC38 cells treated with 75 μM for 12 h and 24 h via microscopic imaging.

Western Blot Analysis[1]

Cell Line: mouse macrophage RAW264.7 cells
Concentration: 10 μM, 25 μM, 50 μM
Incubation Time: 3 h
Result: Increased levels of phosphorylated P65 (p-P65) compared to control.
Induced phosphorylation of STING, TBK1, and IRF3 in a concentration-dependent manner.
In Vivo

MSA-2-Pt (150 μg; i.t.; three doses on day 13, 15, 19) delivers robust antitumor efficacy in MC38 colon carcinoma-bearing mice, with 78% of treated mice achieving tumor-free status and significantly extended survival[1].
MSA-2-Pt (150 μg; i.t.; three doses on day 9, 11, 15) exhibits significant antitumor efficacy in poorly immunogenic B16F10 melanoma-bearing mice, with 22% of treated mice achieving tumor-free status and significantly extended survival[1].
MSA-2-Pt (150 μg; i.t.; single dose) activates the STING pathway (via elevated serum IFN-β), enhances tumor infiltration of CD4+ and CD8+ T cells, and induces tumor cell death and apoptosis in MC38 colon carcinoma-bearing mice[1].

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

Animal Model: Colon carcinoma C57BL/6 mice (female, 6 weeks old, subcutaneous injection of 2×105 MC38 cells)[1]
Dosage: 150 μg
Administration: intratumorly injection; three doses on day 13, 15, 19
Result: Significantly reduced tumor growth relative to the control group.
Achieved tumor-free status in 7 out of 9 treated mice.
Significantly increased survival compared to the control group.
Animal Model: Melanoma C57BL/6 mice (female, 6 weeks old, subcutaneous injection of 2×105 B16F10 cells)[1]
Dosage: 150 μg
Administration: intratumorly injection; three doses
Result: Significantly reduced tumor growth relative to the control group.
Achieved tumor-free status in 2 out of 9 treated mice.
Significantly increased survival compared to the control group.
Animal Model: Colon carcinoma C57BL/6 mice (female, 6 weeks old, subcutaneous injection of 2×105 MC38 cells)[1]
Dosage: 150 μg
Administration: intratumorly injection; single dose
Result: Increased serum IFN-β levels significantly relative to the control group.
Increased the ratio of CD4+ T cells of total cells and CD8+ T cells of total cells in tumor tissue relative to the control group.
Induced significant tumor cell death observed via H&E staining.
Induced a significantly higher proportion of tumor cell apoptosis observed via TUNEL staining.
Molecular Weight

815.78

Formula

C28H32N2O10PtS2
SMILES

O=C(CCC(O[Pt]([NH3])(OC(CCC(C1=CC2=CC(OC)=C(OC)C=C2S1)=O)=O)[NH3])=O)C3=CC4=CC(OC)=C(OC)C=C4S3
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
References
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MSA-2-Pt Related Classifications

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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:

MSA-2-PtSTINGApoptosisIKKIFNARNF-κBStimulator of Interferon GenesTMEM173MITAERISMPYSIκB kinaseI kappa B kinase Interferon-α/β receptorInterferon-alpha/beta receptor Nuclear factor-κBNuclear factor-kappaBmouse colon carcinomaMC38 cellsSTING pathwaymelanomatumor cell deathRAW264.7 cellsCD8+ T cellcGAS-STING pathwayB16F10 melanomaCD4+ T cellInhibitorinhibitorinhibit

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HY-162133
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