2. Cell Cycle/DNA Damage Protein Tyrosine Kinase/RTK Autophagy
  3. CDK DYRK Autophagy
  4. CLK1-IN-3

CLK1-IN-3 (compound 10ad) is a potent and selective Clk1 inhibitor, with an IC50 of 5 nM and over 300-fold selectivity for Dyrk1A. CLK1-IN-3 also shows a relatively potent inhibition against Clk2 and Clk4, with IC50 values of 42 and 108 nM, respectively. CLK1-IN-3 potently induces autophagy in vitro. CLK1-IN-3 can be used for acute liver injury (ALI) research.

商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。

CLK1-IN-3

CLK1-IN-3 構造式

CAS 番号 : 2922550-28-3

容量 価格（税別） 在庫状況 数量
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 352 在庫あり
Solution
10 mM * 1 mL in DMSO USD 352 在庫あり
Solid
5 mg $320 在庫あり
10 mg $520 在庫あり
25 mg $1050 在庫あり
50 mg $1750 在庫あり
100 mg $2800 在庫あり
200 mg   お問い合わせ  
500 mg   お問い合わせ  

* アイテムを追加する前、数量をご選択ください

This product is a controlled substance and not for sale in your territory.

カスタマーレビュー

Based on 0 publication(s) in Google Scholar

CLK1-IN-3 関連抗体

Top Publications Citing Use of Products

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

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

  • 生物活性

  • 純度とドキュメンテーション

  • 参考文献

  • カスタマーレビュー

製品説明

CLK1-IN-3 (compound 10ad) is a potent and selective Clk1 inhibitor, with an IC50 of 5 nM and over 300-fold selectivity for Dyrk1A. CLK1-IN-3 also shows a relatively potent inhibition against Clk2 and Clk4, with IC50 values of 42 and 108 nM, respectively. CLK1-IN-3 potently induces autophagy in vitro. CLK1-IN-3 can be used for acute liver injury (ALI) research[1].

IC50 & Target

CLK1

5 nM (IC50)

CLK2

42 nM (IC50)

CLK4

108 nM (IC50)

DYRK1A

1521 nM (IC50)

体外実験

CLK1-IN-3 (compound 10ad) shows potential in anti-tumor because of dual inhibition of Clk1 and Clk2[1].
CLK1-IN-3 (10 μM-1000 μM) can effectively bind to Clk1 protein and inhibit its degradation in a dose-dependent manner[1].
CLK1-IN-3 (0-10 μM, 24 h) induces autophagy in Hela, BNLCL.2 and HCT 116 cells[1].
CLK1-IN-3 stimulates the degradation of SQSTM1/p62 (a marker of autolysosomes)[1].

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

CLK1-IN-3 関連抗体

Western Blot Analysis[1]

Cell Line: Hela cells, BNLCL.2 and HCT 116 cells
Concentration: 0.2, 1, 5, and 10 μM
Incubation Time: 24 h
Result: Elevated the expression level of LC3II protein (a marker of autophagosomes) as well as the ratio of LC3II to LC3I (a sensitive index of autophagy) in a dose-dependent and time-dependent manner.
体内実験

CLK1-IN-3 (compound 10ad) (0-40 mg/kg, IP, once) significantly suppresses acute liver injury (ALI) without apparent liver cell death in the ALI model induced by acetaminophen (HY-66005, APAP)[1].
CLK1-IN-3 (10 mg/kg; IV, PO, IP, once) shows acceptable pharmacokinetic profile, has a relatively long T1/2 with 5.29 h and oral bioavailability of 19.5%[1].

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

Animal Model: Male C57BL/6 mice(8 weeks, injected acetaminophen (HY-66005) (500 mg/kg, ip))[1]
Dosage: 10, 20, and 40 mg/kg
Administration: IP, once
Result: Decreased serum alanine aminotransferase (ALT) and aspartate aminotransferase (AST) levels significantly in dose-dependent.
Animal Model: Male Balb/c mice (aged 8 weeks)[1]
Dosage: 10 mg/kg
Administration: IV, PO, IP, once (Pharmacokinetic Analysis)
Result: Pharmacokinetic Parameters of CLK1-IN-3 in male Balb/C mice[1].
IV (10 mg/kg) PO (10 mg/kg) IP (10 mg/kg)
Cmax (ng/mL) 13166.5±875.9 1457.4±177.3 4654.3±435.3
T1/2 (h) 2.96±1.2 5.29±2.1 3.27 ±1.1
AUC0-t (ng/mL∗h) 9520.5±1011.3 1860.2±411.0 5010.4±987.2
CL (L/h/kg) 1.05±0.10 5.51±1.00 3.58±0.82
F (%) 19.5%
分子量

430.48

分子式

C24H23FN6O
CAS 番号
Appearance

Solid

Color

Off-white to light yellow

SMILES

CN1CCN(CC1)C2=CC=C(C=C2)C(NC3=CN=C4NC=C(C4=C3)C5=CN=CC(F)=C5)=O
輸送条件

Room temperature in continental US; may vary elsewhere.
保管条件

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
溶剤 & 溶解度
体外: 

DMSO : 100 mg/mL (232.30 mM; Need ultrasonic; 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 2.3230 mL 11.6149 mL 23.2299 mL
5 mM 0.4646 mL 2.3230 mL 4.6460 mL
10 mM 0.2323 mL 1.1615 mL 2.3230 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 (sealed storage, away from moisture). 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)

Mass
=
Concentration
×
Volume
×
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

×
体積 （開始）

V1

=
濃度 （終了）

C2

×
体積 （終了）

V2

体内:

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

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    40% PEG300    5% Tween-80    45% Saline

    Solubility: 2.5 mg/mL (5.81 mM); Clear solution; Need ultrasonic

    This protocol yields a clear solution of 2.5 mg/mL.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

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

    Solubility: 2.5 mg/mL (5.81 mM); Clear solution; Need ultrasonic

    This protocol yields a clear solution of 2.5 mg/mL. 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 (25.0 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.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
純度とドキュメンテーション
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 (sealed storage, away from moisture). 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 2.3230 mL 11.6149 mL 23.2299 mL 58.0747 mL
5 mM 0.4646 mL 2.3230 mL 4.6460 mL 11.6149 mL
10 mM 0.2323 mL 1.1615 mL 2.3230 mL 5.8075 mL
15 mM 0.1549 mL 0.7743 mL 1.5487 mL 3.8716 mL
20 mM 0.1161 mL 0.5807 mL 1.1615 mL 2.9037 mL
25 mM 0.0929 mL 0.4646 mL 0.9292 mL 2.3230 mL
30 mM 0.0774 mL 0.3872 mL 0.7743 mL 1.9358 mL
40 mM 0.0581 mL 0.2904 mL 0.5807 mL 1.4519 mL
50 mM 0.0465 mL 0.2323 mL 0.4646 mL 1.1615 mL
60 mM 0.0387 mL 0.1936 mL 0.3872 mL 0.9679 mL
80 mM 0.0290 mL 0.1452 mL 0.2904 mL 0.7259 mL
100 mM 0.0232 mL 0.1161 mL 0.2323 mL 0.5807 mL
  • No file chosen (Maximum size is: 1024 Kb)
  • If you have published this work, please enter the PubMed ID.
  • Your name will appear on the site.

CLK1-IN-3 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:

CLK1-IN-32922550-28-3CDKDYRKAutophagyCyclin dependent kinaseDual specificity tyrosine phosphorylation regulated kinaseDual specificity tyrosine regulated kinaseHepatoprotectiveacute liver injuryHela cellsHCT116 cellsBNL CL.2 cellsautophagosomesInhibitorinhibitorinhibit

最近チェックした製品:

オンラインお問い合わせ

Your information is safe with us. * Required Fields.

製品名

  

カスタマ需要量 *

お名前 *

 

タイトル

メールアドレス *

 

電話番号 *

デパートメント

 

組纖名 *

市区町村

都道府県

国或いは地域 *

      

必ず会社名を記載ください。個人への返信は行いません。

備考

バルクお問い合わせ

Inquiry Information

製品名:
CLK1-IN-3
製品番号:
HY-149262
数量:
MCE 日本正規代理店:

カスタマーレビュー

Thank You for Your Feedback!

Request for HNMR Report

Please fill out this form to request the QC report. We will send it to your Email address shortly.

Your information is safe with us. * Required Fields.

製品名

  

Lot #

お名前 *

 

メールアドレス *

電話番号 *

 

部門 *

組纖名 *

 

国或いは地域 *

備考

Request for HNMR Report

We have received your request and will respond to you as soon as possible.