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DMX-5804

Catalog No. T5483 CAS 2306178-56-1

Synonyms: DMX-5084

DMX-5804 is a potent, selective MAP4K4 inhibitor, with an IC50 of 3 nM.DMX-5804 enhances cardiomyocyte survival, and reduces ischemia-reperfusion injury in mice.

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DMX-5804, CAS 2306178-56-1

Pack Size	Availability	Price/USD
1 mg	In stock	$ 108.00
2 mg	In stock	$ 157.00
5 mg	In stock	$ 247.00
10 mg	In stock	$ 397.00
25 mg	In stock	$ 663.00
50 mg	In stock	$ 945.00
100 mg	In stock	$ 1,280.00
1 mL * 10 mM (in DMSO)	In stock	$ 272.00

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Purity: 99.63%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	DMX-5804 is a potent, selective MAP4K4 inhibitor, with an IC50 of 3 nM.DMX-5804 enhances cardiomyocyte survival, and reduces ischemia-reperfusion injury in mice.
Targets&IC50	MAP4K4:3 nM
In vitro	DMX-5804, that rescues cell survival, mitochondrial function.
In vivo	DMX-5804 reduces ischemia-reperfusion injury in mice by more than 50%.
Cell Research	Mitochondrial function in hiPSC-CMs was determined using a Seahorse XFe24 Analyzer.?vCor.4U cells (60,000/well) were transferred to 0.1% gelatin-coated XF24 plates and maintained for 5 d. On day 6, DMX-5804 was added 45 min prior to challenge with menadione for 2 h. The medium was replaced 1 hr before the assay, using bicarbonate-free Seahorse assay medium (8.3 g L-1 DMEM Base , 10 mM glucose, 2 mM L-alanyl-L-glutamine dipeptide, 1 mM sodium pyruvate , pH 7.4).?Cells were maintained at 37 C without supplemental CO2 starting 1 hr before the assay.?For each state measured, three assay cycles were performed (4 min mixing, 2 min wait, and 2 min measurement periods, with readings every 15 s). The basal oxygen consumption rate (OCR) and extracellular acidification rate were determined, followed by sequential injection of 1 μM oligomycin A to inhibit ATP synthase, 0.5 μM carbonyl cyanide-4-phenylhydrazone to uncouple oxidative phosphorylation, and 1 μM antimycin A/rotenone to inhibit mitochondrial complex III and I. For each condition, 12 wells were tested, comprising 4 independent experiments.
Animal Research	n vivo pharmacokinetic profiling was performed in female CD-1 mice, using 3 animals per time point.?First, 30% w/v Kleptose as excipient was dissolved in water and vortexed gently for several min. Next, 30 mg of DMX-5084?was dissolved into 0.6 mL of DMSO, for a concentration of 50 mg ml-1, and 4.5 mL of the Kleptose solution was added to 0.5 mL of the test compound solution.?A precipitate forms, which re-dissolves over 2-5 min, leaving a clear or slightly hazy solution with a final concentration of 5 mg/ml.?The dosing solution is used as soon as practicable, vortexing immediately prior to use.?This amount was sufficient formulation for 25 doses of 200 μL (20 g mouse).?Compounds were administered orally at 50 mg/kg, with terminal blood (plasma) sampling at 10 min, 30 min, 1 h, 2.5 h, 5 h, 10 h, and 20 h[1].

Synonyms	DMX-5084
Molecular Weight	361.39
Formula	C21H19N3O3
CAS No.	2306178-56-1

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 125 mg/mL (345.89 mM)

References and Literature

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.

Citations

1. Zhang Z, Zhou H, Gu W, et al.CGI1746 targets σ1R to modulate ferroptosis through mitochondria-associated membranes.Nature Chemical Biology.2024: 1-11.

Related compound libraries

This product is contained In the following compound libraries：

Kinase Inhibitor Library Inhibitor Library Neural Regeneration Compound Library Stem Cell Differentiation Compound Library Reprogramming Compound Library MAPK Inhibitor Library Anti-Aging Compound Library Orally Active Compound Library Bioactive Compound Library NO PAINS Compound Library

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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 add μL PEG300， mix and clarify, next add μL Tween 80，mix and clarify, next add μL ddH₂O, mix and clarify.

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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

DMX-5804 2306178-56-1 MAPK inhibit Inhibitor MAP4K DMX5084 DMX-5084 DMX5804 DMX 5084 DMX 5804 MAPK Kinase Kinase Kinase inhibitor

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