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.

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CLK1-IN-3 Chemical Structure

CLK1-IN-3 Chemical Structure

CAS No. : 2922550-28-3

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5 mg USD 320 In-stock
10 mg USD 520 In-stock
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Based on 1 publication(s) in Google Scholar

CLK1-IN-3 Related Antibodies

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Description

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)

In Vitro

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 Related Antibodies

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.
In Vivo

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%
Molecular Weight

430.48

Formula

C24H23FN6O
CAS No.
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
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, sealed storage, away from moisture

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

Solvent & Solubility
In Vitro: 

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
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
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Volume
×
Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

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.
Purity & Documentation
References

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
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CLK1-IN-3 Related Classifications

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

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