| Size | Price | Stock | Qty |
|---|---|---|---|
| 100mg |
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| 500mg |
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| 1g | |||
| Other Sizes |
| Targets |
SP-600125-Me is structurally related to SP600125 but is designed to have minimal activity against its targets. Its primary purpose is to serve as a negative control in experiments. It has a much lower affinity for JNK isoforms (IC50s = 18 and 24 µM for JNK2 and JNK3, respectively) compared to the potent inhibition exhibited by SP600125 (Ki = 0.19 µM). This allows researchers to distinguish between specific JNK-mediated effects and off-target effects of SP600125.
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|---|---|
| ln Vitro |
In vitro, SP-600125-Me is characterized by its significantly reduced activity against JNK isoforms compared to SP600125. It is used in parallel with SP600125 in cell-based assays to validate that the observed effects are specific to JNK inhibition. Its lack of potent activity makes it an ideal negative control.
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| ln Vivo |
In vivo, SP-600125-Me is not used as a therapeutic agent but as a tool to confirm target specificity in animal models. By administering both SP600125 and its negative control, researchers can assess whether the in vivo effects of SP600125 are attributable to JNK inhibition or other mechanisms.
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| Enzyme Assay |
The inhibitory activity of SP-600125-Me against JNK isoforms is assessed using in vitro kinase assays, similar to those used for SP600125. Recombinant JNK enzymes are incubated with a substrate and varying concentrations of the compound. The IC50 is calculated from the dose-response curve to confirm its low potency compared to SP600125.
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| Cell Assay |
The cellular activity of SP-600125-Me is evaluated in cell lines where JNK signaling is activated. Cells are treated with the compound, and its effect on JNK-mediated phosphorylation of substrates is measured by Western blot. Its minimal effect confirms its utility as a negative control.
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| Animal Protocol |
In animal studies, SP-600125-Me would be administered via the same route as SP600125, typically intraperitoneal (i.p.) injection, to serve as a control. Its effect on JNK signaling and disease endpoints would be compared to that of SP600125 to confirm target specificity.
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| ADME/Pharmacokinetics |
Pharmacokinetic properties of SP-600125-Me are not extensively documented, as it is a research tool rather than a therapeutic candidate. As a small molecule (MW 234.25, C15H10N2O), it is likely to have similar properties to SP600125.
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| Toxicity/Toxicokinetics |
Formal toxicology studies have not been conducted for SP-600125-Me, as it is not intended for therapeutic use. Its use is limited to research applications as a negative control.
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| References | |
| Additional Infomation |
SP-600125-Me (CAS: 54642-23-8) is an essential research tool for validating the specificity of JNK inhibitors. By providing a structurally similar but inactive compound, it allows researchers to confidently attribute biological effects to JNK inhibition. Its use is critical in studies investigating the role of JNK in various cellular processes and diseases.
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| Molecular Formula |
C15H10N2O
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|---|---|
| Molecular Weight |
234.253
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| Exact Mass |
234.079
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| Elemental Analysis |
C, 76.91; H, 4.30; N, 11.96; O, 6.83
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| CAS # |
54642-23-8
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| Related CAS # |
54642-23-8
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| PubChem CID |
11665831
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| Appearance |
Yellow to orange solid
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| Density |
1.4±0.1 g/cm3
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| Boiling Point |
448.0±14.0 °C at 760 mmHg
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| Flash Point |
224.7±20.1 °C
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| Vapour Pressure |
0.0±1.1 mmHg at 25°C
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| Index of Refraction |
1.737
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| LogP |
3.29
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
2
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| Rotatable Bond Count |
0
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| Heavy Atom Count |
18
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| Complexity |
370
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| Defined Atom Stereocenter Count |
0
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| SMILES |
CN1C2=CC=CC3=C2C(=N1)C4=CC=CC=C4C3=O
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| InChi Key |
ODZGYELAMAOARP-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C15H10N2O/c1-17-12-8-4-7-11-13(12)14(16-17)9-5-2-3-6-10(9)15(11)18/h2-8H,1H3
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| Chemical Name |
14-methyl-14,15-diazatetracyclo[7.6.1.02,7.013,16]hexadeca-1(15),2,4,6,9(16),10,12-heptaen-8-one
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| Synonyms |
Negative Control; JNK Inhibitor II, N1-Methyl-1,9-pyrazoloanthrone; SP 600125, negative control; 2-methyldibenzo[cd,g]indazol-6(2H)-one
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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: ~10 mg/mL (42.7 mM）
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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.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 4.2689 mL | 21.3447 mL | 42.6894 mL | |
| 5 mM | 0.8538 mL | 4.2689 mL | 8.5379 mL | |
| 10 mM | 0.4269 mL | 2.1345 mL | 4.2689 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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