KH CB19 |
Catalog No.GC11774
One-Click Copy Product Info
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inhibitor of CLK1 and CLK4, potent and selective
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1354037-26-5
Sample solution is provided at 25 µL, 10mM.
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KH CB19 is a potent and selective inhibitor of CLK1 and CLK4 with IC50 values of 19.7 and 530 nM for CLK1 and CLK3, respectively [1] [2].
The cdc2-like kinases (CLKs) are dual specificity protein kinases that phosphorylate the serine- and arginine-rich (SR) proteins, which are involved in regulating the alternative pre-mRNA splicing process [1].
KH CB19 is a potent and selective inhibitor of CLK1 and CLK4. In endothelial cells, KH CB19 inhibited the phosphorylation of serine- and arginine-rich (SR) proteins stimulated by TNF-α and decreased the mRNA expression of tissue factor splice variants [1]. KH CB19 bound to the ATP binding site in CLK3 and CLK1. In enzyme kinetic assays, KH CB19 inhibited DYRK1A with IC50 value of 55.2 nM. In human microvascular endothelial cells (HMEC-1), KH-CB19 (10 µM) reduced the phosphorylation of SRp75, SRp55 and SRp20. However, in TNF-α stimulated HMEC-1, KH-CB19 (10 µM) inhibited the phosphorylation of SRp75, SRp55, SRp40, SC35, SF2/ASF and SRp20. In HMEC-1, KH CB19 (10 µM) significantly reduced the expression of the membrane bound full-length tissue factor (flTF) as well as the soluble asHTF in TNF-α-induced and TNF-α-non-induced cells [2].
References:
[1]. Grant SK, Lunney EA. Kinase inhibition that hinges on halogen bonds. Chem Biol, 2011, 18(1): 3-4.
[2]. Fedorov O, Huber K, Eisenreich A, et al. Specific CLK inhibitors from a novel chemotype for regulation of alternative splicing. Chem Biol, 2011, 18(1): 67-76.
| Cas No. | 1354037-26-5 | SDF | |
| Chemical Name | (E)-ethyl 3-(2-amino-1-cyanovinyl)-6,7-dichloro-1-methyl-1H-indole-2-carboxylate | ||
| Canonical SMILES | ClC1=C2N(C)C(C(OCC)=O)=C(/C(C#N)=C\N)C2=CC=C1Cl | ||
| Formula | C15H13Cl2N3O2 | M.Wt | 338.19 |
| Solubility | DMSO : ≥ 50 mg/mL (147.85 mM) | Storage | Store at -20°C |
| 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 | 2.9569 mL | 14.7846 mL | 29.5692 mL |
| 5 mM | 591.4 μL | 2.9569 mL | 5.9138 mL |
| 10 mM | 295.7 μL | 1.4785 mL | 2.9569 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
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 9 reference(s) in Google Scholar.)