CLK8 |
Katalog-Nr.GB40148
One-Click Copy Product Info
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CLK8 is a potent and specific CLOCK inhibitor which can disrupt the interaction between CLOCK and BMAL1.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 898920-65-5
Sample solution is provided at 25 µL, 10mM.
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CLK8 is a potent and specific CLOCK inhibitor which can disrupt the interaction between CLOCK and BMAL1 [1]. CLK8 inhibits the translocation of CLOCK into the nucleus, leading to the stabilization of the negative arm of the transcription/translation feedback loop (TTFL) and enhancing the amplitude of the circadian rhythm [2]. CLK8 has been widely used to increase leukocyte-endothelium interactions [3].
In vitro, CLK8 treatment (20μM) for 12 hours significantly inhibited the entry of herpes simplex virus type 1 (HSV-1) into SH-SY5Y cells, and reduced the expression of NECTIN-1 protein as well as the protein levels of early HSV-1 protein ICP0 and late protein ICP5 [4].
In vivo, CLK8 treatment via intraperitoneal injection at a dose of 20mg/kg every other day for 10 days significantly inhibited tumor progression in AB1-HA tumor-bearing mice and reduced the number of αSMA-positive cancer-associated fibroblasts in the tumor tissue [5].
References:
[1] Doruk Y U, Yarparvar D, Akyel Y K, et al. A CLOCK-binding small molecule disrupts the interaction between CLOCK and BMAL1 and enhances circadian rhythm amplitude[J]. Journal of Biological Chemistry, 2020, 295(11): 3518-3531.
[2] Kavakli I H, Gul S, Turkay M. Identification of novel small molecules targeting core clock proteins to regulate circadian rhythm[J]. Current Opinion in Chemical Engineering, 2022, 35: 100730.
[3] Luna-Marco C, Devos D, Cacace J, et al. Molecular circadian clock disruption in the leukocytes of individuals with type 2 diabetes and overweight, and its relationship with leukocyte–endothelial interactions[J]. Diabetologia, 2024, 67(10): 2316-2328.
[4] Tang J J, Pan M, Liu J, et al. Circadian clock proteins BMAL1 and CLOCK regulate HSV-1 entry into nerve cells through NECTIN-1[J]. Virology Journal, 2025, 22(1): 333.
[5] Mitsuhashi A, Koyama K, Ogino H, et al. Clock pathway inhibitor overcomes tumor immune-exclusion via regulation of fibrocyte differentiation[J]. NPJ Precision Oncology, 2025, 9(1): 274.
| Cell experiment [1]: | |
Cell lines | SH-SY5Y cells |
Preparation Method | SH-SY5Y cells were grown in DMEM media supplemented with 10% fetal bovine serum in 5% CO2 at 37°C. SH-SY5Y were seeded in 12-well plates and cultured until reaching 70-80% confluence. Cells were subsequently incubated in fresh serum-free medium for 24h. A serum shock was induced by exposing the cells to medium containing 50% fetal bovine serum for 2h. Following the serum shock, the medium was replaced with serum-free medium. For HSV-1 infection experiments, cells were challenged with the virus at 2h post serum shock. SH-SY5Y cells were treated with different concentrations of CLK8 (0, 1, 5, 10, and 20μM) and infected with HSV-1 for 12h. Viral DNA copy numbers were quantified by qPCR and NECTIN-1 protein levels were analyzed by western blotting. |
Reaction Conditions | 0, 1, 5, 10, and 20μM; 12h |
Applications | CLK8 treatment significantly reduced the DNA copy numbers of HSV-1 genes and NECTIN-1 protein levels in SH-SY5Y cells in a dose-dependent manner. |
| Animal experiment [2]: | |
Animal models | BALB/c mice |
Preparation Method | BALB/c mice (six-week-old; 22-25g) were housed in cages and maintained in air-conditioned animal quarters with a 12h light-dark cycle and free access to autoclaved tap water and a standard chow diet. AB1-HA cells (1×106 cells per mouse) suspended in 0.1ml PBS were subcutaneously inoculated into the right flank of BALB/c mice. Tumor-bearing mice were treated every other day with CLK8 (20mg/kg per mouse) by intraperitoneal injection 5 days after tumor inoculation for 10 days. Tumor size was measured twice a week using Vernier calipers, where volume=ab2/2 (a, long diameter; b, short diameter). |
Dosage form | 20mg/kg; every other day for 10 days; p.o. |
Applications | CLK8 treatment inhibited tumor volume in AB1-HA tumor-bearing mice. |
References: | |
| Cas No. | 898920-65-5 | SDF | |
| Formula | C29H26N2O6 | M.Wt | 498.53 |
| Löslichkeit | DMSO : 50 mg/mL (100.29 mM; Need ultrasonic) | Storage | Store at -20°C,protect from light |
| 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. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.0059 mL | 10.0295 mL | 20.059 mL |
| 5 mM | 401.2 μL | 2.0059 mL | 4.0118 mL |
| 10 mM | 200.6 μL | 1.0029 mL | 2.0059 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
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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 saline, 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.
Quality Control & SDS
- View current batch:
- Purity: >98.00% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 30 reference(s) in Google Scholar.)