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| 1mg |
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| Targets |
The primary targets of SB-734117 are kinases from the AGC and CMCG groups. The compound exhibits potent inhibitory activity towards MSK-1 with an IC₅₀ value of 3.0 nM. SB-734117 prevents CREB and histone H3 post-translational modifications. By inhibiting these kinases, the compound disrupts viral protein production and prevents the post-translational modification of cellular factors associated with viral protein production. The mechanism involves interference with host cell signaling pathways required for HCMV replication.
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| ln Vitro |
In vitro studies have demonstrated that SB-734117 inhibits productive replication of several HCMV strains. The compound's anti-HCMV effects have been characterized in infected human foreskin fibroblast (HFF) cells. Treatment with SB-734117 leads to loss of H3S10p or H3K14ac modifications. Kinase selectivity data confirmed that SB-734117 is a multi-kinase inhibitor. The compound's in vitro potency against HCMV makes it a valuable tool for studying viral replication mechanisms.
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| ln Vivo |
In vivo antiviral activity of SB-734117 has not been extensively reported. The compound is primarily studied in cell-based systems to understand the role of host kinases in HCMV replication. Animal model studies evaluating its efficacy against HCMV infection have not been published. Further preclinical investigations in appropriate animal models are needed to assess the compound's therapeutic potential and to confirm whether the in vitro antiviral activity translates to in vivo efficacy.
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| Enzyme Assay |
For kinase inhibition assays, recombinant kinases are incubated with substrates and ATP in the presence of SB-734117. Phosphorylation levels are measured using radioactive (³³P-ATP) or fluorescence-based (TR-FRET) detection methods. IC₅₀ values are calculated from dose-response curves. For binding studies, surface plasmon resonance or other biophysical techniques may be used to measure direct binding affinity to target kinases. Selectivity profiling is performed using kinase panels.
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| Cell Assay |
For in vitro cell-based studies, human foreskin fibroblasts (HFF) are infected with HCMV at a multiplicity of infection (MOI) appropriate for the experiment. Cells are treated with SB-734117 or DMSO control at the time of infection. Viral replication is assessed by measuring viral DNA levels by qPCR, viral protein expression by Western blotting, or infectious virus production by plaque assay. Post-translational modifications of CREB and histone H3 are analyzed by Western blotting.
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| Animal Protocol |
In vivo animal studies for SB-734117 have not been extensively documented. For similar antiviral compounds, mouse models of HCMV or MCMV (murine cytomegalovirus) infection may be used. Immunocompromised or humanized mice are typically required for HCMV infection studies. Test compound is administered via oral, intraperitoneal, or intravenous routes. Efficacy endpoints include viral load reduction in target organs and survival. Standard protocols for in vivo antiviral efficacy studies can be adapted.
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| ADME/Pharmacokinetics |
Pharmacokinetic properties of SB-734117 have not been comprehensively characterized. As a small molecule with a molecular formula of C₁₄H₁₆N₂O, it is expected to have reasonable oral bioavailability and membrane permeability. Specific PK parameters such as half-life, clearance, volume of distribution, and protein binding have not been reported in the available literature. Further pharmacokinetic studies are needed to understand its ADME properties.
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| Toxicity/Toxicokinetics |
Toxicological data for SB-734117 are limited. As a kinase inhibitor, it may have off-target effects due to its polypharmacology. Cytotoxicity against mammalian cell lines has been evaluated in the context of antiviral studies, but systematic toxicological assessments have not been published. Safety and tolerability studies are needed if the compound is to be developed further as a therapeutic agent.
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| References | |
| Additional Infomation |
SB-734117 is a research compound identified as a novel anti-HCMV agent. It has been used as a tool compound to study the role of host kinases in HCMV replication. The compound was identified through screening of a GlaxoSmithKline protein kinase inhibitor set. No clinical trials or regulatory approvals have been reported. SB-734117 serves as a valuable research tool for studying HCMV biology and for the development of new antiviral strategies.
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| Molecular Formula |
C14H16N6O
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| Exact Mass |
284.138
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| CAS # |
607368-97-8
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| PubChem CID |
44397032
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| Appearance |
Typically exists as solid at room temperature
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| LogP |
1.3
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
6
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| Rotatable Bond Count |
2
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| Heavy Atom Count |
21
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| Complexity |
363
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| Defined Atom Stereocenter Count |
0
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| SMILES |
C1CCC(CC1)N2C3=C(C=NC=C3)N=C2C4=NON=C4N
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| InChi Key |
JRYCXZUZWFHQPB-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C14H16N6O/c15-13-12(18-21-19-13)14-17-10-8-16-7-6-11(10)20(14)9-4-2-1-3-5-9/h6-9H,1-5H2,(H2,15,19)
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| Chemical Name |
4-(1-cyclohexylimidazo[4,5-c]pyridin-2-yl)-1,2,5-oxadiazol-3-amine
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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) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
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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