2. Immunology/Inflammation
  3. Interleukin Related
  4. iST2-1

iST2-1 is an Stimulation-2 (ST2) inhibitor with an IC50 value of 46.65 μM, blocks interaction between ST2 and IL-33, inhibits downstream signaling. iST2-1 functions as an immunomodulator, reduces proliferation of CD4+ and CD8+ T cells, increases regulatory T cell populations, reduces IFN-γ+CD4+ T cell populations, increases Foxp3+CD4+ regulatory T cell populations in the gastrointestinal tract. iST2-1 reduces plasma soluble ST2 and IFN-γ levels, reduces graft-versus-host disease scores, improves survival in graft-versus-host disease animal models, preserves graft-versus-tumor effect. iST2-1 can be used for the research of graft-versus-host disease.

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iST2-1

iST2-1 Chemical Structure

CAS No. : 1019158-02-1

Size Price Stock Quantity
Liquid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
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Solution
10 mM * 1 mL in DMSO In-stock
Liquid
25 mg In-stock
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100 mg   Get quote  

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Customer Review

Based on 1 publication(s) in Google Scholar

iST2-1 Related Antibodies

Top Publications Citing Use of Products

View All Interleukin Related Isoform Specific Products:

View All Isoforms
IL-1 IL-2 IL-3 IL-4 IL-5 IL-6 IL-8 IL-10 IL-12 IL-13 IL-15 IL-17 IL-23 IL-7 IL-33 IL-22 IL-18

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

iST2-1 is an Stimulation-2 (ST2) inhibitor with an IC50 value of 46.65 μM, blocks interaction between ST2 and IL-33, inhibits downstream signaling. iST2-1 functions as an immunomodulator, reduces proliferation of CD4+ and CD8+ T cells, increases regulatory T cell populations, reduces IFN-γ+CD4+ T cell populations, increases Foxp3+CD4+ regulatory T cell populations in the gastrointestinal tract. iST2-1 reduces plasma soluble ST2 and IFN-γ levels, reduces graft-versus-host disease scores, improves survival in graft-versus-host disease animal models, preserves graft-versus-tumor effect. iST2-1 can be used for the research of graft-versus-host disease[1][2].

IC50 & Target

ST2

46.65 μM (IC50)

In Vitro

iST2-1 inhibits ST2/IL-33 binding in the AlphaLISA assay with an IC50 of 46.65 μM[1].
iST2-1 inhibits ST2/IL-33 signaling in HEK-BlueTM IL-33 cells with an IC50 range of 56.42-65.87 μM[1].
iST2-1 (1 μM) exhibits short metabolic stability in both mouse and human liver microsomes with T1/2 values of 0.73 min and 1.10 min, respectively[1].

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

iST2-1 Related Antibodies
Parmacokinetics
Species Dose Route T1/2
Mice[1] 40 mg/kg i.p. 1.43 h
In Vivo

iST2-1 (41.4 mg/kg; i.p.; daily; 21 days) reduces GVHD score to 3, maintains plasma hsST2 below 30 pg/mL through Day 28, and improves survival rate to 45% on Day 35 in NSG mouse GVHD models[2].
iST2-1 reduces plasma sST2 concentration, decreases gastrointestinal IFNγ+CD4+ T cells, and increases gastrointestinal Foxp3+CD4+ Tregs in C3H.SW mouse GVHD models[2].

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

Animal Model: NSG (irradiated with 300 cGy total body irradiation, transplanted with human PBMC)[2]
Dosage: 41.4 mg/kg
Administration: i.p.; daily; 21 days
Result: Reduced IFNγ+CD4+ T cells and increased Foxp3+CD4+ Tregs in gastrointestinal CD45+CD4+ cells at Day 14; Lowered plasma human IFNγ by at least 50% compared to DMSO control at Day 14; Produced more profound effects on T cell populations at Day 21; Maintained plasma hsST2 below 30 pg/mL through Day 28; Decreased GVHD score to 3; Improved survival rate to 45% on Day 35.
Molecular Weight

378.42

Formula

C22H22N2O4
CAS No.
Appearance

Liquid (Density: 1.235±0.06 g/cm3)

Color

Yellow to brown

SMILES

COC1=CC=C(C=C1)C1CCCN1CC1=CC=C(O1)C1=CC=CC=C1[N+]([O-])=O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Pure form -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (264.26 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 2.6426 mL 13.2128 mL 26.4257 mL
5 mM 0.5285 mL 2.6426 mL 5.2851 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. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
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Concentration
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Volume
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Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

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Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 5 mg/mL (13.21 mM); Clear solution

    This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation

Purity: 99.58%

SDS (394 KB)

COA (254 KB) HNMR (146 KB) RP-HPLC (165 KB) LCMS (235 KB)

Handling Instructions (2659 KB)
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. 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 2.6426 mL 13.2128 mL 26.4257 mL 66.0642 mL
5 mM 0.5285 mL 2.6426 mL 5.2851 mL 13.2128 mL
10 mM 0.2643 mL 1.3213 mL 2.6426 mL 6.6064 mL
15 mM 0.1762 mL 0.8809 mL 1.7617 mL 4.4043 mL
20 mM 0.1321 mL 0.6606 mL 1.3213 mL 3.3032 mL
25 mM 0.1057 mL 0.5285 mL 1.0570 mL 2.6426 mL
30 mM 0.0881 mL 0.4404 mL 0.8809 mL 2.2021 mL
40 mM 0.0661 mL 0.3303 mL 0.6606 mL 1.6516 mL
50 mM 0.0529 mL 0.2643 mL 0.5285 mL 1.3213 mL
60 mM 0.0440 mL 0.2202 mL 0.4404 mL 1.1011 mL
80 mM 0.0330 mL 0.1652 mL 0.3303 mL 0.8258 mL
100 mM 0.0264 mL 0.1321 mL 0.2643 mL 0.6606 mL
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iST2-1 Related Classifications

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:

iST2-11019158-02-1Interleukin RelatedILCD8+ T cellsHEK-Blue? IL-33 cellsgastrointestinal tractregulatory T cellsIL-33graft-versus-host diseaseFoxp3+CD4+ regulatory T cellsCD4+ T cellsinterferon-gammaST2Inhibitorinhibitorinhibit

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