| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 50mg |
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| 100mg |
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| Other Sizes |
| Targets |
SIK1, SIK2, and SIK3 (salt-inducible kinases). WH-4-025 is a small-molecule inhibitor that targets salt-inducible kinases, particularly SIK1, SIK2, and SIK3. These kinases are members of the AMPK-related kinase family and play important roles in metabolic regulation, immune responses, and inflammatory signaling. By inhibiting SIKs, WH-4-025 modulates downstream signaling pathways.
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| ln Vitro |
WH-4-025 is a potent and selective inhibitor of SIKs, with activity against SIK1, SIK2, and SIK3. By inhibiting SIK-mediated phosphorylation, it modulates transcriptional and inflammatory signaling pathways, including those affecting CRTCs. The compound exhibits high purity (≥95%) and good cell permeability, making it suitable for cellular studies. Its activity is characterized by its ability to inhibit SIK-mediated phosphorylation events and modulate downstream gene expression.
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| ln Vivo |
In vivo, WH-4-025 is used to study the role of SIKs in metabolic regulation, immune modulation, and inflammatory diseases. By inhibiting SIK activity, the compound can modulate inflammatory responses and metabolic pathways. It has potential applications in the study of depression and other conditions where SIK signaling is implicated. Its in vivo effects would be assessed in animal models of these diseases.
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| Enzyme Assay |
In vitro binding and enzyme activity assays are used to characterize WH-4-025 as a SIK inhibitor. Kinase activity assays are performed using recombinant SIK1, SIK2, or SIK3 enzymes incubated with substrates in the presence of increasing concentrations of the compound. The inhibition of kinase activity is measured to determine the compound's potency and selectivity for the SIK family members.
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| Cell Assay |
In vitro cellular assays for WH-4-025 involve treating cells with the compound and measuring downstream effects of SIK inhibition. Readouts include the phosphorylation status of SIK substrates (such as CRTCs) and changes in gene expression of SIK-regulated targets. The compound's good cell permeability ensures effective cellular activity. These assays confirm that WH-4-025 can inhibit SIK activity in a cellular context and modulate relevant signaling pathways.
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| Animal Protocol |
In vivo efficacy of WH-4-025 would be evaluated in animal models of inflammatory diseases, metabolic disorders, or depression. The compound is supplied as a solid and is soluble in DMSO, making it suitable for formulation for in vivo administration. Efficacy endpoints would include reduction of inflammatory markers, improvement in metabolic parameters, or behavioral changes depending on the disease model being studied.
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| ADME/Pharmacokinetics |
WH-4-025 has a molecular formula of C39H38F3N7O5 and a molecular weight of 741.76. It is supplied as a solid with ≥95% purity and is soluble in DMSO. As a small-molecule SIK inhibitor, its pharmacokinetic properties would be characteristic of this class, with potential for oral bioavailability. The compound's high purity and good cell permeability make it a valuable tool for cellular and in vivo studies.
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| Toxicity/Toxicokinetics |
No specific toxicity data is available for WH-4-025. As a SIK inhibitor, its safety profile would be an important consideration. Potential toxicities could be related to its effects on SIK-mediated signaling in various tissues. Standard preclinical safety studies would be required to evaluate its safety for potential therapeutic applications.
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| References | |
| Additional Infomation |
WH-4-025 (CAS#: 1876463-35-2) is a potent and selective small-molecule inhibitor of salt-inducible kinases (SIKs), particularly SIK1, SIK2, and SIK3. It has a molecular formula of C39H38F3N7O5 and a molecular weight of 741.76. The compound modulates transcriptional and inflammatory signaling pathways and is used as a research tool for studying metabolic regulation, immune modulation, and potential treatments for inflammatory diseases and depression. It is not approved for clinical use.
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| Molecular Formula |
C39H38F3N7O5
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|---|---|
| Molecular Weight |
741.758139133453
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| Exact Mass |
741.288
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| CAS # |
1876463-35-2
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| PubChem CID |
73707529
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| Appearance |
White to off-white solid powder
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| LogP |
7.3
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
13
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| Rotatable Bond Count |
11
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| Heavy Atom Count |
54
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| Complexity |
1200
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| Defined Atom Stereocenter Count |
0
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| SMILES |
FC(C1=CC=CC(=C1)NC(C1C=CC(C)=C(C=1)OC(N(C1C=CC(=CC=1OC)OC)C1=CC=NC(=N1)NC1C=CC(=CC=1)N1CCN(C)CC1)=O)=O)(F)F
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| InChi Key |
MWWDOHSKUDECFQ-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C39H38F3N7O5/c1-25-8-9-26(36(50)44-29-7-5-6-27(23-29)39(40,41)42)22-33(25)54-38(51)49(32-15-14-31(52-3)24-34(32)53-4)35-16-17-43-37(46-35)45-28-10-12-30(13-11-28)48-20-18-47(2)19-21-48/h5-17,22-24H,18-21H2,1-4H3,(H,44,50)(H,43,45,46)
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| Chemical Name |
[2-methyl-5-[[3-(trifluoromethyl)phenyl]carbamoyl]phenyl] N-(2,4-dimethoxyphenyl)-N-[2-[4-(4-methylpiperazin-1-yl)anilino]pyrimidin-4-yl]carbamate
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO: 125 mg/mL (168.52 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (2.80 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: 2.08 mg/mL (2.80 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.08 mg/mL (2.80 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.3481 mL | 6.7407 mL | 13.4814 mL | |
| 5 mM | 0.2696 mL | 1.3481 mL | 2.6963 mL | |
| 10 mM | 0.1348 mL | 0.6741 mL | 1.3481 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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