Cat. No.: HY-114331

DLK-IN-1

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DLK-IN-1 (Compound 14) is an orally active, blood-brain barrier-penetrable and selective inhibitor of dual leucine zipper kinase (DLK, MAP3K12) with a K_i value of 3 nM. DLK-IN-1 inhibits Flt3, PAK4, STK33 and TrkA. DLK-IN-1 reduces p-c-Jun. DLK-IN-1 can be used in Alzheimer's disease research.

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

Purity: 98.27%
CAS No.: 1620574-24-4
Formula: C₂₀H₂₄F₃N₅O₂
Molecular Weight:423.43

Storage:

Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month

DLK-IN-1 Chemical Structure

CAS No.: 1620574-24-4

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Sample (0.1mg)

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(In Japan)

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Biological Activity
- Description
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Solvent & Solubility
- In Vitro
- In Vivo
Purity & Documentation
References
Help & FAQs
Bioz

Biological Activity

Description

IC₅₀ & Target

Ki: 3 nM (DLK)^[1].

All MAP3K Isoforms :

All PAK Isoforms :

All Trk Receptor Isoforms :

In Vitro

DLK-IN-1 can protect axons in a dose-dependent manner, with an EC₅₀ of 0.574 μM^[1].
DLK-IN-1 (1 μM) inhibits kinases such as Flt3, PAK4, STK33, and TrkA by ≥50%^[1].

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

In Vivo

DLK-IN-1 (15-50 mg/kg; p.o.) can significantly reduce the phosphorylation level of c-Jun in the PS2APP mouse model of Alzheimer's disease^[1].
DLK-IN-1 (25-75 mg/kg; 7 days) is well-tolerated in Sprague-Dawley rats^[1].

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

Chemical Information

CAS No. 1620574-24-4
Appearance Solid
Molecular Weight 423.43
Formula C₂₀H₂₄F₃N₅O₂
Color White to off-white
SMILES

CC(N1C([C@@H]2[C@]3([H])[C@@]2([H])CN(C4COC4)C3)=CC(C5=CN=C(N)C(OC(F)(F)F)=C5)=N1)C
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 : 62.5 mg/mL (147.60 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.3617 mL

11.8083 mL

23.6167 mL

5 mM

0.4723 mL

2.3617 mL

4.7233 mL

10 mM

0.2362 mL

1.1808 mL

2.3617 mL

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

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

Mass

Concentration

Volume

Molecular Weight

Dilution Calculator

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

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

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% (20% SBE-β-CD in Saline)

Solubility: ≥ 2.08 mg/mL (4.91 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.

Protocol 2

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.08 mg/mL (4.91 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 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 (20.8 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.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

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).

Working solution concentration: 0.22 mg/mL

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (273 KB)
SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Portuguese - PT (251 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[1]. Patel S, et al. Selective Inhibitors of Dual Leucine Zipper Kinase (DLK, MAP3K12) with Activity in a Model of Alzheimer's Disease. J Med Chem. 2017 Oct 12;60(19):8083-8102. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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	2.3617 mL	11.8083 mL	23.6167 mL	59.0416 mL
	5 mM	0.4723 mL	2.3617 mL	4.7233 mL	11.8083 mL
	10 mM	0.2362 mL	1.1808 mL	2.3617 mL	5.9042 mL
	15 mM	0.1574 mL	0.7872 mL	1.5744 mL	3.9361 mL
	20 mM	0.1181 mL	0.5904 mL	1.1808 mL	2.9521 mL
	25 mM	0.0945 mL	0.4723 mL	0.9447 mL	2.3617 mL
	30 mM	0.0787 mL	0.3936 mL	0.7872 mL	1.9681 mL
	40 mM	0.0590 mL	0.2952 mL	0.5904 mL	1.4760 mL
	50 mM	0.0472 mL	0.2362 mL	0.4723 mL	1.1808 mL
	60 mM	0.0394 mL	0.1968 mL	0.3936 mL	0.9840 mL
	80 mM	0.0295 mL	0.1476 mL	0.2952 mL	0.7380 mL
	100 mM	0.0236 mL	0.1181 mL	0.2362 mL	0.5904 mL

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DLK-IN-1

Cell Cycle/DNA Damage Compound Library

Immunology/Inflammation Compound Library

Kinase Inhibitor Library

MAPK Compound Library

Neuronal Signaling Compound Library

Protein Tyrosine Kinase Compound Library

CNS-Penetrant Compound Library

Anti-Aging Compound Library

Oxygen Sensing Compound Library

Cytoskeleton Compound Library

Orally Active Compound Library

Anti-Alzheimer's Disease Compound Library

Anti-Blood Cancer Compound Library

Neurodegenerative Disease-related Compound Library

Anti-Obesity Compound Library

Targeted Diversity Library

Heterocyclic Compound Library

Pain-Related Compound Library

Membrane Protein-targeted Compound Library

Membrane Receptor-targeted Compound Library

Highly Selective Inhibitors Library

Cytokine Inhibitors Library

Serine/Threonine Kinase Inhibitor Library

Anti-Hematopathy Compound Library

Multi-Target Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

Anti-Brain Cancer Compound Library

Protein Kinase Compound Library

High-Throughput Bioactive Compound Library

Posttranslational Modification Library

All MAP3K Isoforms

All PAK Isoforms

All Trk Receptor Isoforms

Biological Activity

Chemical Information

Solvent & Solubility

Purity & Documentation

References

Help & FAQs

Complete Stock Solution Preparation Table

DLK-IN-1 Related Classifications

Cat. No.: HY-114331