ホーム>>Signaling Pathways>> Stem Cell>> GSK-3>>EHT 5372

EHT 5372

カタログ番号GC38330

Products are for research use only. Not for human use. We do not sell to patients.

EHT 5372 化学構造

Cas No.: 1425945-60-3

サイズ 価格 在庫数 個数
10mM (in 1mL DMSO)
$506.00
在庫あり
5mg
$459.00
在庫あり

Tel:(909) 407-4943 Email: sales@glpbio.com

顧客レビュー

カスタマーレビューに基づきます。

  • GlpBio Citations

    GlpBio Citations
  • Bioactive Compounds Premium Provider

    Bioactive Compounds Premium Provider

Sample solution is provided at 25 µL, 10mM.

Product Documents

Quality Control & SDS

View current batch:

Background

EHT 5372 is a strong inhibitor of DYRK's family kinases, with IC50s of 0.22, 0.28 nM for DYRK1A and DYRK1B, respectively.

EHT 5372 is a strong inhibitor of DYRK's family kinases, with IC50s of 0.22, 0.28 nM for DYRK1A and DYRK1B, respectively[1][2]. IC50 for DYRK2 and DYRK3 were higher (10.8 and 93.2 nM, respectively) and there was no inhibition on DYRK4. EHT 5372 displayed minimal impact on the CDC2-like kinase (CLK) family, with more than 100x selectivity over CLK1 (CLK1: IC50=22.8 nM; CLK2: IC50=88.8 nM; CLK3: IC50>10 lM; CLK4: no inhibition) and on the glycogen synthase kinase 3 (GSK3) family (GSK3α: IC50=7.44 nM; GSK3β: IC50=221 nM). EHT 5372 inhibits the direct phosphorylation of Tau by DYRK1A. EHT 5372 also normalizes both Aβ-induced Tau phosphorylation and DYRK1A-stimulated Aβ production[2].

[1]. Chaikuad A, et al. An Unusual Binding Model of the Methyl 9-Anilinothiazolo[5,4-f] quinazoline-2-carbimidates (EHT 1610 and EHT 5372) Confers High Selectivity for Dual-Specificity Tyrosine Phosphorylation-Regulated Kinases. J Med Chem. 2016 Nov 23;59(22):10315-10321. [2]. Coutadeur S, et al. A novel DYRK1A (dual specificity tyrosine phosphorylation-regulated kinase 1A) inhibitor for the treatment of Alzheimer's disease: effect on Tau and amyloid pathologies in vitro. J Neurochem. 2015 May;133(3):440-51.

Chemical Properties

Cas No. 1425945-60-3 SDF
Canonical SMILES N=C(C(S1)=NC2=C1C3=C(NC4=CC=C(OC)C=C4F)N=CN=C3C=C2)OC
Formula C18H14FN5O2S M.Wt 383.4
溶解度 DMSO: 25 mg/mL (65.21 mM); Water: < 0.1 mg/mL (insoluble) Storage Store at -20°C,unstable in solution, ready to use.
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.

Complete Stock Solution Preparation Table

Prepare stock solution
1 mg 5 mg 10 mg
1 mM 2.6082 mL 13.0412 mL 26.0824 mL
5 mM 0.5216 mL 2.6082 mL 5.2165 mL
10 mM 0.2608 mL 1.3041 mL 2.6082 mL
  • モルアリティ計算機

  • 希釈計算機

質量
=
濃度
x
容積
x
MW*
 
 
 
**ストックソリューションを準備する際には、常にバイアルラベルおよび MSDS/CoA(オンラインで利用可能)で掲載された製品のロット固有分子量を使用してください。

計算

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

mg/kg 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.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

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.

レビュー

Review for EHT 5372

Average Rating: 5 ★★★★★ (Based on Reviews and 1 reference(s) in Google Scholar.)

5 Star
100%
4 Star
0%
3 Star
0%
2 Star
0%
1 Star
0%
Review for EHT 5372

GLPBIO products are for RESEARCH USE ONLY. Please make sure your review or question is research based.

Required fields are marked with *

You may receive emails regarding this submission. Any emails will include the ability to opt-out of future communications.