1. Metabolic Enzyme/Protease
  2. Cryptochrome
  3. CLK8

CLK8 is a potent and specific CLOCK inhibitor that can disrupt the interaction between CLOCK and BMAL1 and interfere with nuclear translocation of CLOCK. CLK8 can be used for the research of disorders associated with dampened circadian rhythms.

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

CLK8 Chemical Structure

CLK8 Chemical Structure

CAS No. : 898920-65-5

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Based on 1 publication(s) in Google Scholar

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Description

CLK8 is a potent and specific CLOCK inhibitor that can disrupt the interaction between CLOCK and BMAL1 and interfere with nuclear translocation of CLOCK. CLK8 can be used for the research of disorders associated with dampened circadian rhythms[1].

IC50 & Target

CLOCK[1]

In Vitro

CLK8 (10-40 μM; 4-6 d) enhances the amplitude of the Bmal1-dLuc signal in U2OS and NIH 3T3 cells in a dose-dependent manner with no period change[1].
CLK8 (10-40 μM) reduces BMAL1-CLOCK interaction, whereas the interaction between CLOCK-F80A, K220A and BMAL1 is not affected in HEK293T cells[1].
CLK8 (20 μM; 2 d) reduces nuclear localization of CLOCK in U2OS cells[1].

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

In Vivo

CLK8 (25 mg/kg; a single i.p.) decreases CLOCK levels in whole cell lysates of the mouse livers, whereas the levels of BMAL1 and CRY1 are unaltered[1].
CLK8 (5-1000 mg/kg; i.p.) exhibits no mortality or clinical signs (dyspnea, hyporeflexia, reduced locomotor activity, piloerection, hunched posture, and corneal opacity) at the doses of 5 and 25 mg/kg[1].

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

Animal Model: Male C57BL/6J mice (8 weeks, 18-24 g)[1]
Dosage: 25 mg/kg
Administration: A single i.p.
Result: A decrease in CLOCK levels was detected in whole cell lysates of the mouse livers, whereas the levels of BMAL1 and CRY1 were unaltered.
Decreased the abundance of CLOCK in the nucleus.
The abundances of cytosolic and nuclear BMAL1 and CRY1 were unaltered.
Decreased Cry1 transcriptional level.
Molecular Weight

498.53

Formula

C29H26N2O6

CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C(COC1=C(C(C2=CC=CC=C2)=CC(O3)=O)C3=C(CCC(C)(C)O4)C4=C1)NC5=C(C(N)=O)C=CC=C5

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, sealed storage, away from moisture and light

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

Solvent & Solubility
In Vitro: 

DMSO : 50 mg/mL (100.29 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 2.0059 mL 10.0295 mL 20.0590 mL
5 mM 0.4012 mL 2.0059 mL 4.0118 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 and light). 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)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

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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 (5.01 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    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 (5.01 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 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 (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

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.
Please enter your animal formula composition:
%
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+
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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 and light)

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 and light). 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 2.0059 mL 10.0295 mL 20.0590 mL 50.1474 mL
5 mM 0.4012 mL 2.0059 mL 4.0118 mL 10.0295 mL
10 mM 0.2006 mL 1.0029 mL 2.0059 mL 5.0147 mL
15 mM 0.1337 mL 0.6686 mL 1.3373 mL 3.3432 mL
20 mM 0.1003 mL 0.5015 mL 1.0029 mL 2.5074 mL
25 mM 0.0802 mL 0.4012 mL 0.8024 mL 2.0059 mL
30 mM 0.0669 mL 0.3343 mL 0.6686 mL 1.6716 mL
40 mM 0.0501 mL 0.2507 mL 0.5015 mL 1.2537 mL
50 mM 0.0401 mL 0.2006 mL 0.4012 mL 1.0029 mL
60 mM 0.0334 mL 0.1672 mL 0.3343 mL 0.8358 mL
80 mM 0.0251 mL 0.1254 mL 0.2507 mL 0.6268 mL
100 mM 0.0201 mL 0.1003 mL 0.2006 mL 0.5015 mL
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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.

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Product Name:
CLK8
Cat. No.:
HY-148765
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