1. Immunology/Inflammation
  2. Interleukin Related
  3. JTE-607

JTE-607, a highly selective inflammatory cytokine synthesis inhibitor, protects from endotoxin shock in mice. JTE-607 inhibits inflammatory cytokine production, including TNF-α, IL-1β, IL-6, IL-8 and IL-10, from LPS-stimulated human PBMCs, with IC50s of 11, 5.9, 8.8, 7.3 and 9.1 nM, respectively. Cleavage and Polyadenylation Specificity Factor 3 (CPSF3) is the target of JTE-607.

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JTE-607 Chemical Structure

JTE-607 Chemical Structure

CAS No. : 188791-09-5

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Solid + Solvent
10 mM * 1 mL in DMSO
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10 mg USD 198 In-stock
25 mg USD 418 In-stock
50 mg USD 715 In-stock
100 mg USD 1188 In-stock
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Based on 1 publication(s) in Google Scholar

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Description

JTE-607, a highly selective inflammatory cytokine synthesis inhibitor, protects from endotoxin shock in mice. JTE-607 inhibits inflammatory cytokine production, including TNF-α, IL-1β, IL-6, IL-8 and IL-10, from LPS-stimulated human PBMCs, with IC50s of 11, 5.9, 8.8, 7.3 and 9.1 nM, respectively[1]. Cleavage and Polyadenylation Specificity Factor 3 (CPSF3) is the target of JTE-607[2].

IC50 & Target

IL-10

 

IL-6

 

IL-8

 

In Vitro

JTE-607 inhibits inflammatory cytokine production, including TNF-α, IL-1β, IL-6, IL-8 and IL-10, from LPS-stimulated human PBMCs, with IC50s of 11, 5.9, 8.8, 7.3 and 9.1 nM, respectively. The inhibitory effects of JTE-607 are also seen in mRNA expression of those cytokines[1].
JTE-607 inhibits inflammatory cytokine production from LPS-stimulated human PBMCs with an IC50 of approximately 10 nM[1].
JTE607 inhibits LPS-stimulated IL-8 production from monkey and rabbit PBMCs, and TNF-α production from mouse and rat PBMCs with IC50s of 59, 780, 1600 and 19000 nM, respectively[1].
JTE607 also suppresses other cytokines, granulocyte-macrophage colony stimulating factor and IL-1RA with IC50s of 2.4±0.8 and 5.4±0.4 nM, respectively[1].
JTE-607 inhibits cytokine production in monkey, rabbit, mouse and rat with IC50s of 59±26, 780±120, 1600±650 and 19000±3200 nM, respectively[1].

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

RT-PCR[1]

Cell Line: human peripheral blood mononuclear cells (PBMCs)
Concentration: 100 nM
Incubation Time: 20 hours
Result: Reduced the increase in the level of mRNAs of TNF-α, IL-1b, IL-6 and IL-8.
In Vivo

JTE-607 (0.3-10 mg/kg, i.v.) shows dose dependent inhibition of mortality after LPS challenge in C. parvum sensitized mice in accordance with a decrease of plasma TNF-α[1].

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

Animal Model: Male C57BL/6 mice (5 to 6 weeks old) are sensitized by injecting Corynebacterium parvum[1]
Dosage: 0.3, 1, 3, 10 mg/kg
Administration: Administered intravenously 10 min before the LPS challenge.
Result: Showed dose dependent inhibition of the mortality at 0.3 to 10 mg/kg and significant effect at 3 and 10 mg/kg.
Molecular Weight

597.36

Formula

C25H33Cl4N3O5

CAS No.
Appearance

Solid

Color

White to off-white

SMILES

CCOC([C@H](CC1=CC=CC=C1)NC(C2=C(C(Cl)=C(C(Cl)=C2)OCCN3CCN(CC3)C)O)=O)=O.Cl.Cl

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, sealed storage, away from moisture

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

Solvent & Solubility
In Vitro: 

DMSO : 250 mg/mL (418.51 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H2O : 20 mg/mL (33.48 mM; ultrasonic and warming and heat to 60°C)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.6740 mL 8.3702 mL 16.7403 mL
5 mM 0.3348 mL 1.6740 mL 3.3481 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.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

  • Molarity Calculator

  • Dilution Calculator

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

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

This equation is commonly abbreviated as: C1V1 = C2V2

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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: ≥ 2.08 mg/mL (3.48 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.08 mg/mL (3.48 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.

For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
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:  PBS

    Solubility: 100 mg/mL (167.40 mM); Clear solution; Need ultrasonic

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.
Calculation results:
Working solution concentration: mg/mL
This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
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).
Purity & Documentation

Purity: 99.27%

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
H2O / DMSO 1 mM 1.6740 mL 8.3702 mL 16.7403 mL 41.8508 mL
5 mM 0.3348 mL 1.6740 mL 3.3481 mL 8.3702 mL
10 mM 0.1674 mL 0.8370 mL 1.6740 mL 4.1851 mL
15 mM 0.1116 mL 0.5580 mL 1.1160 mL 2.7901 mL
20 mM 0.0837 mL 0.4185 mL 0.8370 mL 2.0925 mL
25 mM 0.0670 mL 0.3348 mL 0.6696 mL 1.6740 mL
30 mM 0.0558 mL 0.2790 mL 0.5580 mL 1.3950 mL
DMSO 40 mM 0.0419 mL 0.2093 mL 0.4185 mL 1.0463 mL
50 mM 0.0335 mL 0.1674 mL 0.3348 mL 0.8370 mL
60 mM 0.0279 mL 0.1395 mL 0.2790 mL 0.6975 mL
80 mM 0.0209 mL 0.1046 mL 0.2093 mL 0.5231 mL
100 mM 0.0167 mL 0.0837 mL 0.1674 mL 0.4185 mL

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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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.

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JTE-607
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