2. MAPK/ERK Pathway
  3. MAP4K
  4. DMX-5804

DMX-5804 is a potent, orally active and selective MAP4K4 inhibitor, with an IC50 of 3 nM, a pIC50 of 8.55 for human MAP4K4, less potent on MINK1/MAP4K6 (pIC50, 8.18), and TNIK/MAP4K7 (pIC50, 7.96). DMX-5804 enhances cardiomyocyte survival, and reduces ischemia-reperfusion injury in mice.

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

DMX-5804 Chemical Structure

DMX-5804 Chemical Structure

CAS No. : 2306178-56-1

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 330 In-stock
Solution
10 mM * 1 mL in DMSO USD 330 In-stock
Solid
1 mg USD 142 In-stock
5 mg USD 300 In-stock
10 mg USD 480 In-stock
25 mg USD 860 In-stock
50 mg USD 1450 In-stock
100 mg USD 2200 In-stock
200 mg   Get quote  
500 mg   Get quote  

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Customer Review

Based on 3 publication(s) in Google Scholar

DMX-5804 Related Antibodies

Top Publications Citing Use of Products

View All MAP4K Isoform Specific Products:

View All Isoforms
MAP4K2/GCK MAP4K3/GLK MAP4K4/HGK MAP4K5/KHS1 MAP4K6/MINK1 MAP4K7/TNIK MAP4K1/HPK1

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

DMX-5804 is a potent, orally active and selective MAP4K4 inhibitor, with an IC50 of 3 nM, a pIC50 of 8.55 for human MAP4K4, less potent on MINK1/MAP4K6 (pIC50, 8.18), and TNIK/MAP4K7 (pIC50, 7.96). DMX-5804 enhances cardiomyocyte survival, and reduces ischemia-reperfusion injury in mice[1].

IC50 & Target[1]

MAP4K4

3 nM (IC50)

MAP4K4

8.55 (pIC50)

MINK1/MAP4K6

8.18 (pIC50)

TNIK/MAP4K7

7.96 (pIC50)

GCK/MAP4K2

6.50 (pIC50)

KHS/MAP4K5

6.36 (pIC50)

GLK/MAP4K3

4.95 (pIC50)

MLK1/MAP3K9

7.19 (pIC50)

MLK3/MAP3K11

6.99 (pIC50)

NUAK

6.88 (pIC50)

VEGFR

5.72 (pIC50)

ABL1

5.80 (pIC50)

Aurora B

5.49 (pIC50)

FLT3

5.31 (pIC50)

GSK3β

4.66 (pIC50)

In Vitro

DMX-5804 exhibits great selectivity at MAP4K4 over other kinases, such as GCK/MAP4K2 (pIC50, 6.50), GLK/MAP4K3 (pIC50, 4.95), KHS/MAP4K5 (pIC50, 6.36), ABL1 (pIC50, 5.80), Aurora B (pIC50, 5.49), FLT3 (pIC50, 5.31), GSK3β (pIC50, 4.66), MLK1/MAP3K9 (pIC50, 7.19), MLK3/MAP3K11 (pIC50, 6.99), NUAK (pIC50, 6.88) and VEGFR (pIC50, 5.72)[1].

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

DMX-5804 Related Antibodies
Molecular Weight

361.39

Formula

C21H19N3O3
CAS No.
Appearance

Solid

Color

Off-white to yellow

SMILES

O=C1NC=NC2=C1C(C3=CC=C(OCCOC)C=C3)=CN2C4=CC=CC=C4
Shipping

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

DMSO : 100 mg/mL (276.71 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 2.7671 mL 13.8355 mL 27.6709 mL
5 mM 0.5534 mL 2.7671 mL 5.5342 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

  • Molarity Calculator

  • Dilution Calculator

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

Mass
=
Concentration
×
Volume
×
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

×
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: ≥ 2.5 mg/mL (6.92 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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.
  • Protocol 2

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

    Solubility: ≥ 2.5 mg/mL (6.92 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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.
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: 99.83%

SDS (251 KB)

COA (255 KB) LCMS (94 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.7671 mL 13.8355 mL 27.6709 mL 69.1773 mL
5 mM 0.5534 mL 2.7671 mL 5.5342 mL 13.8355 mL
10 mM 0.2767 mL 1.3835 mL 2.7671 mL 6.9177 mL
15 mM 0.1845 mL 0.9224 mL 1.8447 mL 4.6118 mL
20 mM 0.1384 mL 0.6918 mL 1.3835 mL 3.4589 mL
25 mM 0.1107 mL 0.5534 mL 1.1068 mL 2.7671 mL
30 mM 0.0922 mL 0.4612 mL 0.9224 mL 2.3059 mL
40 mM 0.0692 mL 0.3459 mL 0.6918 mL 1.7294 mL
50 mM 0.0553 mL 0.2767 mL 0.5534 mL 1.3835 mL
60 mM 0.0461 mL 0.2306 mL 0.4612 mL 1.1530 mL
80 mM 0.0346 mL 0.1729 mL 0.3459 mL 0.8647 mL
100 mM 0.0277 mL 0.1384 mL 0.2767 mL 0.6918 mL
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DMX-5804 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:

DMX-58042306178-56-1DMX5804DMX 5804MAP4KMAPK Kinase Kinase KinaseInhibitorinhibitorinhibit

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