2. Protein Tyrosine Kinase/RTK Cell Cycle/DNA Damage Stem Cell/Wnt PI3K/Akt/mTOR
  3. DYRK CDK GSK-3
  4. EHT 5372

EHT 5372 is a highly potent and selective inhibitor of DYRK's family kinases with IC50s of 0.22, 0.28, 10.8, 93.2, 22.8, 88.8, 59.0, 7.44, and 221 nM for DYRK1A, DYRK1B, DYRK2, DYRK3, CLK1, CLK2, CLK4, GSK-3α, and GSK-3β, respectively.

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EHT 5372

EHT 5372 構造式

CAS 番号 : 1425945-63-6

容量 価格（税別） 在庫状況 数量
5 mg $450 在庫あり
10 mg $800 在庫あり
25 mg $1650 在庫あり
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100 mg   お問い合わせ  

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Based on 1 publication(s) in Google Scholar

EHT 5372 関連抗体

Top Publications Citing Use of Products

DYRK アイソフォーム固有の製品をすべて表示:

すべてのアイソフォームを表示
DYRK1 DYRK2 DYRK3 DYRK4 HIPK PRP4

CDK アイソフォーム固有の製品をすべて表示:

すべてのアイソフォームを表示
CDK1 CDK2 CDK3 CDK4 CDK5 CDK6 CDK7 CDK8 CDK9 CDK11 CDK12 CDK13 CDK14 CDK16 CDK19 CDC CLK Pho85 CDK10 CDK15 CDK17 CDK18 CDK20 PITSLRE

GSK-3 アイソフォーム固有の製品をすべて表示:

すべてのアイソフォームを表示
GSK-3 GSK-3α GSK-3β

  • 生物活性

  • 純度とドキュメンテーション

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製品説明

EHT 5372 is a highly potent and selective inhibitor of DYRK's family kinases with IC50s of 0.22, 0.28, 10.8, 93.2, 22.8, 88.8, 59.0, 7.44, and 221 nM for DYRK1A, DYRK1B, DYRK2, DYRK3, CLK1, CLK2, CLK4, GSK-3α, and GSK-3β, respectively[1][2].

IC50 & Target[1][2]

DYRK1A

0.22 nM (IC50)

DYRK1B

0.28 nM (IC50)

DYRK2

10.8 nM (IC50)

DYRK4

93.2 nM (IC50)

CLK1

22.8 nM (IC50)

CLK2

88.8 nM (IC50)

CLK4

59.0 nM (IC50)

GSK-3α

7.44 nM (IC50)

GSK-3β

221 nM (IC50)

体外実験

EHT 5372 (0.1-10 μM; 24 hours) dose-dependently reduces pS396-Tau levels with an IC50 of 1.7 μM whereas cell viability remains over 87% in all conditions[1].
EHT 5372 (0.01-1 μM) inhibits the direct phosphorylation of Tau by DYRK1A[1]
EHT 5372 reduces Aβ production in a dose-dependent reduction with an IC50 of 1.06 μM[1].

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

EHT 5372 関連抗体

Cell Viability Assay[1]

Cell Line: HEK293 cells
Concentration: 0.1, 0.5, 1, 5, 10 μM
Incubation Time: 24 hours
Result: Cell viability remained over 87% in all conditions.

Western Blot Analysis[1]

Cell Line: HEK293 cells
Concentration: 0.01, 0.03, 0.1, 0.3 , 1 μM
Incubation Time:
Result: Potently and dose-dependently inhibited Tau phosphorylation at pS396.
分子量

404.27

分子式

C17H11Cl2N5OS
CAS 番号
Appearance

Solid

Color

Off-white to yellow

SMILES

N=C(C(S1)=NC2=C1C3=C(NC4=CC=C(Cl)C=C4Cl)N=CN=C3C=C2)OC
輸送条件

Room temperature in continental US; may vary elsewhere.
保管条件
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
溶剤 & 溶解度
体外: 

DMSO : 6.25 mg/mL (15.46 mM; ultrasonic and warming and heat to 60°C; 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 2.4736 mL 12.3680 mL 24.7359 mL
5 mM 0.4947 mL 2.4736 mL 4.9472 mL
10 mM 0.2474 mL 1.2368 mL 2.4736 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, 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

  • Dilution Calculator

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

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Molecular Weight *

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

一般には略語で表示されます：C1V1 = C2V2

濃度 （開始）

C1

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体積 （開始）

V1

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In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
純度とドキュメンテーション

純度: 98.12%

COA (253 KB) HNMR (138 KB) RP-HPLC (169 KB) LCMS (385 KB)

取扱説明書 (2659 KB)
参考文献

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, 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 2.4736 mL 12.3680 mL 24.7359 mL 61.8399 mL
5 mM 0.4947 mL 2.4736 mL 4.9472 mL 12.3680 mL
10 mM 0.2474 mL 1.2368 mL 2.4736 mL 6.1840 mL
15 mM 0.1649 mL 0.8245 mL 1.6491 mL 4.1227 mL
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EHT 5372 Related Classifications

  • Molarity Calculator

  • Dilution Calculator

The molarity calculator equation

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

質量   濃度   体積   分子量 *
= × ×

The dilution calculator equation

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

一般には略語で表示されます：C1V1 = C2V2

濃度 （開始） × 体積 （開始） = 濃度 （終了） × 体積 （終了）
× = ×
C1   V1   C2   V2
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:

EHT 53721425945-63-6EHT5372EHT-5372DYRKCDKGSK-3Dual specificity tyrosine phosphorylation regulated kinaseDual specificity tyrosine regulated kinaseCyclin dependent kinaseGlycogen synthase kinase-3Glycogen synthase kinase 3neurodegenerativediseasescancerdiabetesAlzheimerDYRK1ATauamyloidprecursorInhibitorinhibitorinhibit

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製品名:
EHT 5372
製品番号:
HY-111379
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