2. MAPK/ERK Pathway
  3. p38 MAPK
  4. (R)-STU104

(R)-STU104 is a potent and orally active TAK1-MKK3 interaction inhibitor with IC50s of 0.58 μM and 4.0 μM for TNF-α and MKK3 phosphorylation. (R)-STU104 suppresses the TAK1/MKK3/p38/MnK1/MK2/elF4E signal pathways through binding with MKK3 and disrupting the TAK1 phosphorylating MKK3. (R)-STU104 can be used for researching ulcerative colitis.

For research use only. We do not sell to patients.

(R)-STU104 Chemical Structure

(R)-STU104 Chemical Structure

CAS No. : 2767124-77-4

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Based on 1 publication(s) in Google Scholar

(R)-STU104 Related Antibodies

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Description

(R)-STU104 is a potent and orally active TAK1-MKK3 interaction inhibitor with IC50s of 0.58 μM and 4.0 μM for TNF-α and MKK3 phosphorylation. (R)-STU104 suppresses the TAK1/MKK3/p38/MnK1/MK2/elF4E signal pathways through binding with MKK3 and disrupting the TAK1 phosphorylating MKK3. (R)-STU104 can be used for researching ulcerative colitis[1].

IC50 & Target

IC50: 0.58 μM (TNF-α), 4.0 μM (MKK3 phosphorylation)[1]
Cellular Effect
Cell Line Type Value Description References
RAW264.7 IC50
0.58 μM
Compound: (R)-STU104
Inhibition of LPS-induced TNFalpha production in mouse RAW264.7 cells preincubated for 2 hrs followed by LPS treatment for 24 hrs by RT-qPCR analysis
Inhibition of LPS-induced TNFalpha production in mouse RAW264.7 cells preincubated for 2 hrs followed by LPS treatment for 24 hrs by RT-qPCR analysis
[PMID: 35442672]
In Vitro

(R)-STU104 attenuates phosphorylation levels of Mnk1, MK2, and elF4E, leading to the downregulation of TNF-α expression and production[1].

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

(R)-STU104 Related Antibodies
In Vivo

(R)-STU104 (1, 3 and 10 mg/kg; IG for 7 days) ameliorates the symptoms of DSS-induced experimental colitis in mice, and significantly inhibits inflammatory cytokine protein[1].
Pharmacokinetic Parameters of (R)-STU104 in male C57 mice[1].

IV (5 mg/kg) PO (30 mg/kg)
Tmax (h) 0.083
AUC0-t (μg/L·h) 7249 9895
AUC0-∞ (μg/L·h) 8635 16991
MRT0-∞ (h) 7.32 12.52
Cmax (ng/mL) 2920 2290
t1/2 (ng/mL) 9.29 8.67
VZ (L/kg) 7.76 3.68
CLZ (ng/mL) 0.58 0.29
F (%) 33%

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

Animal Model: C57BL/6 mice (dextran sodium sulfate (DSS)-induced acute ulcerative colitis)[1]
Dosage: 1, 3 and 10 mg/kg
Administration: IG, for 7 days
Result: Ameliorated the symptoms of DSS-induced experimental colitis, and significantly inhibited inflammatory cytokine protein TNF-α, IL-1β, IL-6, and IL-23.
Molecular Weight

298.33

Formula

C18H18O4
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C1C[C@H](C2=CC=C(OC)C=C2)C3=C1C=C(OC)C=C3OC
Shipping

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

DMSO : 50 mg/mL (167.60 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 3.3520 mL 16.7600 mL 33.5199 mL
5 mM 0.6704 mL 3.3520 mL 6.7040 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)

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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)

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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    90% Corn Oil

    Solubility: ≥ 5 mg/mL (16.76 mM); Clear solution

    This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 mg/mL) to 900 μL Corn oil, and mix evenly.

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
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 3.3520 mL 16.7600 mL 33.5199 mL 83.7998 mL
5 mM 0.6704 mL 3.3520 mL 6.7040 mL 16.7600 mL
10 mM 0.3352 mL 1.6760 mL 3.3520 mL 8.3800 mL
15 mM 0.2235 mL 1.1173 mL 2.2347 mL 5.5867 mL
20 mM 0.1676 mL 0.8380 mL 1.6760 mL 4.1900 mL
25 mM 0.1341 mL 0.6704 mL 1.3408 mL 3.3520 mL
30 mM 0.1117 mL 0.5587 mL 1.1173 mL 2.7933 mL
40 mM 0.0838 mL 0.4190 mL 0.8380 mL 2.0950 mL
50 mM 0.0670 mL 0.3352 mL 0.6704 mL 1.6760 mL
60 mM 0.0559 mL 0.2793 mL 0.5587 mL 1.3967 mL
80 mM 0.0419 mL 0.2095 mL 0.4190 mL 1.0475 mL
100 mM 0.0335 mL 0.1676 mL 0.3352 mL 0.8380 mL
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(R)-STU104 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:

(R)-STU1042767124-77-4p38 MAPKTAK1MKK3TAK1/MKK3/p38/MnK1/MK2/elF4E signal pathwaysulcerative colitisdextran sodium sulfateInhibitorinhibitorinhibit

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