1. Immunology/Inflammation Protein Tyrosine Kinase/RTK Apoptosis
  2. Interleukin Related VEGFR Apoptosis
  3. S7

S7 is an inhibitory polypeptide targeting IL-6R, which specifically binds to IL-6R and its A chain (gp80/IL-6RA) to block its signal transduction. S7 inhibits IL-6-mediated anti-apoptosis (apoptosis), angiogenesis and the expression of VEGF-A, blocks related survival signaling pathways, and enhances the sensitivity of cancer cells to chemotherapeutic drugs. S7 can be applied to the research of related diseases such as cervical cancer, multiple myeloma, Kaposi's sarcoma, prostate cancer and basal cell carcinoma.

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S7

S7 Chemical Structure

CAS No. : 853248-13-2

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Description

S7 is an inhibitory polypeptide targeting IL-6R, which specifically binds to IL-6R and its A chain (gp80/IL-6RA) to block its signal transduction. S7 inhibits IL-6-mediated anti-apoptosis (apoptosis), angiogenesis and the expression of VEGF-A, blocks related survival signaling pathways, and enhances the sensitivity of cancer cells to chemotherapeutic drugs. S7 can be applied to the research of related diseases such as cervical cancer, multiple myeloma, Kaposi's sarcoma, prostate cancer and basal cell carcinoma[1][2].

IC50 & Target[1]

IL-6Ra

 

VEGFR1

 

In Vitro

S7 (1012 pfu/mL; 1 h) potently inhibits the binding of IL-6 to purified IL-6Rα in a cell-free competitive binding ELISA assay[1].
S7 (5×106 pfu/mL; 2 h) specifically binds to membrane-bound IL-6Rα on C33A, HeLa, Siha, BCC and HEK293 cell lines, but does not bind to IL-6Rα-negative HUVEC cells[1].
S7 inhibits the binding of IL-6 to membrane-bound IL-6Rα on C33A, HeLa, Siha, BCC and HEK293 cell lines[1].
S7 (50 μM; 24 h) blocks IL-6-mediated activation of the PI3-K/Akt and Ras/MAPK signaling pathways, and inhibits IL-6-induced upregulation of the anti-apoptotic protein Mcl-1 in C33A cervical cancer cells[1].
S7 inhibits IL-6-induced VEGF-A secretion in C33A cervical cancer cells, BCC cells, and RPMI 8226 multiple myeloma cells[1].
S7 inhibits the secretion of VEGF-A by C33A, BCC and RPMI 8226 cells, and blocks IL-6-induced HUVEC proliferation[1].
S7 almost completely inhibits IL-6-induced capillary-like tube formation in human umbilical vein endothelial cells (HUVECs) in vitro[1].
S7 (25-250 μM; 1 h) dose-dependently blocks the interaction between IL-6 and recombinant soluble human IL-6Rα, with significant inhibitory activity observed at concentrations of 25 μM and above[2].
S7 (50 μM; 2 h) significantly blocks the binding of IL-6 to IL-6Rα on C33A, HeLa, Siha, BCC and HEK293 cells[2].
S7 (50 μM; 24 h) sensitizes C33A cervical cancer cells to cisplatin-induced apoptosis by blocking the IL-6-mediated anti-apoptotic signaling pathway[2].
S7 (50 μM; 16 h) inhibits IL-6-induced VEGF-A protein and VEGF-A mRNA expression in C33A, RPMI 8226 and BCC cancer cells, and reduces constitutive VEGF-A expression in IL-6-overexpressing C33A/IL-6 cells[2].
S7 (50 μM; 24 h) reduces IL-6-induced VEGF-A secretion in C33A, BCC and RPMI 8226 cancer cells[2].
S7 (50 μM) inhibits IL-6-induced HUVEC proliferation by reducing pro-angiogenic factors in the conditioned media of C33A, BCC and RPMI 8226 cancer cells[2].

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

ELISA Assay[1]

Cell Line: C33A, HeLa, Siha, BCC, HEK293, HUVEC
Concentration: 5×1012 pfu/mL
Incubation Time: 2 h
Result: Showed high binding affinity to all membrane-type IL-6Rα-expressing cell lines (C33A, HeLa, Siha, BCC, HEK293) but did not bind to IL-6Rα-negative HUVEC cells, with significantly higher absorbance values than the control phage S1 in IL-6Rα-positive lines.

Western Blot Analysis[1]

Cell Line: C33A cervical cancer cell line
Concentration: 50 μmol/L
Incubation Time: 24 h
Result: Significantly inhibited IL-6-induced phosphorylation of Akt and ERK1/2, blocking activation of the PI3-K/Akt and Ras/MAPK signaling pathways.
Suppressed IL-6-induced up-regulation of the antiapoptotic Mcl-1 protein.

ELISA Assay[2]

Cell Line: C33A, HeLa, Siha, BCC, HEK293
Concentration: 50 μM
Incubation Time: 2 h
Result: Significantly reduced the binding of IL-6 to IL-6Rα in all five tested cell lines compared to the S1 control peptide.

Apoptosis Analysis[2]

Cell Line: C33A cervical carcinoma cells
Concentration: 50 μM
Incubation Time: 24 h
Result: Interfered with IL-6's protective effect against cisplatin-induced apoptosis.
Significantly increased the percentage of apoptotic cells compared to IL-6 plus cisplatin treatment without S7.

ELISA Assay[2]

Cell Line: C33A, BCC, RPMI 8226
Concentration: 50 μM
Incubation Time: 24 h
Result: Notably decreased IL-6-mediated VEGF-A secretion in all three tested cell lines compared to IL-6-treated cells without S7.
In Vivo

S7 (50 mg/kg; i.p.; once every 2 days) inhibits IL-6-induced cervical cancer tumor growth in SCID mice by 76%[1].
S7 (50 mg/kg; i.p.; once every 2 days; for a total of 39 days) inhibits IL-6-induced cervical tumor growth by 76% in SCID mice through suppressing the IL-6-mediated signaling pathway, VEGF-A expression, and inducing tumor cell apoptosis[2].
S7 abrogates IL-6-induced angiogenesis in C57BL/6J mice, which is verified by the decreased hemoglobin content in Matrigel plugs[2].

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

Animal Model: SCID mice (6- to 8-week-old female; inoculated s.c. with 1 × 106 IL-6-overexpressing C33A cervical carcinoma cells)[2]
Dosage: 50 mg/kg
Administration: i.p.; every 2 days; 39 days
Result: Reduced IL-6-induced tumor growth by 76%.
Significantly inhibited IL-6-mediated VEGF-A expression and phosphorylation of Akt and ERK in tumor tissue.
Increased the number of apoptotic tumor cells as measured by TUNEL assay.
Clinical Trial
Molecular Weight

815.01

Formula

C37H70N10O10

CAS No.
Appearance

Solid

Color

White to off-white

Sequence

Leu-Ser-Leu-Ile-Thr-Arg-Leu

Sequence Shortening

LSLITRL

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Sealed storage, away from moisture

Powder -80°C 2 years
-20°C 1 year

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility
In Vitro: 

DMSO : 50 mg/mL (61.35 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.2270 mL 6.1349 mL 12.2698 mL
5 mM 0.2454 mL 1.2270 mL 2.4540 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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Working solution concentration: mg/mL
Purity & Documentation

Purity: 98.25%

References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.2270 mL 6.1349 mL 12.2698 mL 30.6745 mL
5 mM 0.2454 mL 1.2270 mL 2.4540 mL 6.1349 mL
10 mM 0.1227 mL 0.6135 mL 1.2270 mL 3.0674 mL
15 mM 0.0818 mL 0.4090 mL 0.8180 mL 2.0450 mL
20 mM 0.0613 mL 0.3067 mL 0.6135 mL 1.5337 mL
25 mM 0.0491 mL 0.2454 mL 0.4908 mL 1.2270 mL
30 mM 0.0409 mL 0.2045 mL 0.4090 mL 1.0225 mL
40 mM 0.0307 mL 0.1534 mL 0.3067 mL 0.7669 mL
50 mM 0.0245 mL 0.1227 mL 0.2454 mL 0.6135 mL
60 mM 0.0204 mL 0.1022 mL 0.2045 mL 0.5112 mL
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  • 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.

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S7
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