TC6-D3
TC6-D3 is a proteolysis-resistant peptide and also a CC chemokine receptor 7 (CCR7) inhibitor, with a Kd value of 403 nM against mouse targets. TC6-D3 blocks the interaction between CCR7 and its ligands CCL19 and CCL21, and inhibits the activation of the ERK1/2 pathway. TC6-D3 reduces the migratory capacity of tumor cells in vitro. TC6-D3 inhibits tumor growth and lymph node metastasis in vivo. TC6-D3 restores T cell cytotoxicity, promotes CD8+ T cell infiltration, and enhances anti-tumor immune responses. TC6-D3 can be used in studies related to lymph node metastasis.
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- No. CAS: 3121532-43-9
- Fòrmula: C61H98N12O19
- Peso molecular:1303.50
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Almacenamiento:
Please store the product under the recommended conditions in the Certificate of Analysis.
Actividad biológica
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CCR7 403 nM (Kd) |
ERK1 |
ERK2 |
TC6-D3 peptide (0.2 mM; 0.2548 h) exhibits significantly enhanced proteolysis resistance compared to TC6, retaining ~70% of its initial concentration after 48 h incubation in 10% mouse serum at 37°C[1].
TC6-D3 peptide (5 min) binds specifically to mouse CCR7 with a dissociation constant of 403 nM, as measured via MST with CHOK1-mCCR7-EGFP cell membrane proteins[1].
TC6-D3 peptide (12.5-200 μM; 24-72 h) does not inhibit the proliferation of MC38-CCR7 (GFP) cells at concentrations ranging from 12.5 μM to 200 μM over 24 h, 48 h, or 72 h incubations[1].
TC6-D3 peptide (200 μM; 48 h) significantly inhibits CCL19-induced chemotaxis of MC38-CCR7 (GFP) cells in a 48 h transwell assay[1].
TC6-D3 peptide (200 μM) significantly attenuates CCL19- and CCL21-induced ERK1/2 phosphorylation in MC38-CCR7 (GFP) and B16-CCR7 cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:MC38-CCR7 (GFP) cells
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Concentration:12.5 μM; 25 μM; 50 μM; 100 μM; 200 μM
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Incubation Time:24 h, 48 h, 72 h
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Result:Showed no significant inhibitory effect on the proliferation of MC38-CCR7 (GFP) cells across all tested concentrations and incubation times.
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Cell Line:MC38-CCR7 (GFP) and MC38-V (GFP) cells
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Concentration:200 μM
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Incubation Time:48 h
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Result:Significantly inhibited CCL19-induced migration of MC38-CCR7 (GFP) cells, while CCL19 had only a weak effect on MC38-V (GFP) cell migration.
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Cell Line:MC38-CCR7 (GFP) and B16-CCR7 cells
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Concentration:200 μM
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Incubation Time:5 min; 10 min; 20 min
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Result:Significantly inhibited CCL19- or CCL21-induced increase in phospho-ERK1/2 levels in both MC38-CCR7 (GFP) and B16-CCR7 cells.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:C57BL/6 (female, 6 to 8 weeks old, MC38-CCR7 (GFP) cell footpad injection-induced popliteal lymph node metastasis model)[1]
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Dosage:2 mg/kg; 6 mg/kg
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Administration:i.p.; daily; 14 days
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Result:Slowed primary tumor growth at 2 mg/kg, with more prominent anti-tumor activity observed at 6 mg/kg; tumor weight followed the same trend.
Significantly inhibited popliteal lymph node metastasis at 6 mg/kg, as measured by IVIS imaging and reduced frequencies of CCR7+GFP+ tumor cells in popliteal lymph nodes via flow cytometry; no significant effect on inguinal lymph node metastasis was observed at either dose.
Showed no significant change in body weight compared to controls.
Significantly increased the frequency of intratumoral CD8+ T cells to 35.3% of CD45+ cells (vs. 12.1% in controls) and intratumoral IFN-γ-secreting CD8+ T cells to 9.66% (vs. 4.73% in controls) at 6 mg/kg; caused a smaller increase in these populations at 2 mg/kg.
Increased the frequency of IFN-γ-secreting CD8+ T cells in popliteal lymph nodes to 2.37% (vs. 0.92% in controls) and inguinal lymph nodes to 3.94% (vs. 2.26% in controls) at 6 mg/kg; both doses showed this effect.
Caused no significant changes in the frequency of total DCs or CCR7+ DCs in primary tumors, popliteal lymph nodes, or inguinal lymph nodes.
Maintained serum ALT, AST, BUN, and CREA levels within normal ranges, and showed no abnormalities in histopathology of major organs.
Chemical Information
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No. CAS 3121532-43-9
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Peso molecular 1303.50
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Fòrmula C61H98N12O19
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Sequence
d{Leu-Ser-Pro}-Leu-Ile-Phe-Val-Thr-Thr-Pro-Asp-{d-Thr}
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Sequence Shortening
d{Leu-Ser-Pro}-LIFVTTPD-{d-Thr}
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureza y Documentación
Referencias
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)