DMX-5804 |
| Catalog No.GC65298 |
Le DMX-5804 est un inhibiteur de MAP4K4 puissant, actif par voie orale et sélectif, avec une IC50 de 3 nM, une pIC50 de 8,55 pour la MAP4K4 humaine, moins puissante sur MINK1/MAP4K6 (pIC50, 8,18) et TNIK/MAP4K7 (pIC50, 7,96) .
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 2306178-56-1
Sample solution is provided at 25 µL, 10mM.
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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].
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].
[1]. Fiedler LR, et al. MAP4K4 Inhibition Promotes Survival of Human Stem Cell-Derived Cardiomyocytes and Reduces Infarct Size In Vivo. Cell Stem Cell. 2019 Mar 1. pii: S1934-5909(19)30013-X.
MAP4K4 3nM(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) | AuroraB 5.49(pIC50) | FLT3 5.31(pIC50) | GSK3β 4.66(pIC50) |
| Cas No. | 2306178-56-1 | SDF | |
| Formula | C21H19N3O3 | M.Wt | 361.39 |
| Solubility | DMSO : 125 mg/mL (345.89 mM; Need ultrasonic) | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
||
| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 2.7671 mL | 13.8355 mL | 27.6709 mL |
| 5 mM | 553.4 μL | 2.7671 mL | 5.5342 mL |
| 10 mM | 276.7 μL | 1.3835 mL | 2.7671 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >99.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 30 reference(s) in Google Scholar.)
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