| Size | Price | Stock | Qty |
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| 1mg |
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| 100mg | |||
| Other Sizes |
| Targets |
JI130 targets the Hes1-PHB2 interaction, similar to its parent compound JI051. By stabilizing this complex, it inhibits the transcriptional repressor activity of Hes1, a key downstream effector of the Notch signaling pathway. This leads to the derepression of genes involved in cell-cycle regulation and differentiation, ultimately reducing tumor growth.
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| ln Vitro |
In vitro, JI130 impairs the ability of Hes1 to repress transcription. It is a cell-penetrant compound that effectively stabilizes the Hes1-PHB2 interaction. Its activity is characterized by the inhibition of Hes1-mediated transcriptional repression in cellular models.
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| ln Vivo |
In vivo, JI130 significantly reduced tumor volume in a murine pancreatic tumor xenograft model. This demonstrates its potential as a novel therapeutic candidate for managing pancreatic cancer. The compound's efficacy in this model highlights its promise in oncology research.
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| Enzyme Assay |
In vitro binding assays for JI130 typically measure the stabilization of the Hes1-PHB2 interaction. These assays can be performed using techniques such as co-immunoprecipitation, pull-down assays, or biophysical methods to quantify the formation of the Hes1-PHB2 complex in the presence of the compound.
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| Cell Assay |
In vitro cellular assays for JI130 involve treating cancer cell lines with the compound and measuring its effects on Hes1 transcriptional activity and cell proliferation. The compound's ability to impair Hes1-mediated repression is assessed by measuring the expression of Hes1 target genes. These assays confirm its mechanism of action.
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| Animal Protocol |
In vivo animal models for JI130 include murine pancreatic tumor xenograft models. The compound is administered by appropriate routes, and tumor growth inhibition is measured. JI130 has been shown to significantly reduce tumor volume in these models, demonstrating its in vivo efficacy.
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| ADME/Pharmacokinetics |
JI130 has a molecular formula of C23H24N2O3 and a molecular weight of 376.45 g/mol. It is a derivative of JI051 and is a cell-penetrant small molecule. The compound is typically stored as a powder at -20°C for long-term stability. It is soluble in DMSO.
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| Toxicity/Toxicokinetics |
JI130 is a small-molecule stabilizer of the Hes1-PHB2 interaction with a well-characterized mechanism of action. As with any experimental compound, potential toxicity should be evaluated in preclinical studies. The compound is for research use only and is not approved for human therapeutic use. It is a valuable tool for studying Notch signaling and pancreatic cancer.
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| References | |
| Additional Infomation |
JI130 (CAS# 2234271-86-2) is a derivative of JI051 and a stabilizer of the Hes1-PHB2 protein-protein interaction. It impairs Hes1-mediated transcriptional repression and has shown significant anti-tumor activity in murine pancreatic cancer models. The compound is for research use only and is not approved for human therapeutic use.
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| Molecular Formula |
C23H24N2O3
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|---|---|
| Molecular Weight |
376.448266029358
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| Exact Mass |
376.178
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| CAS # |
2234271-86-2
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| PubChem CID |
154730572
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| Appearance |
White to light yellow solid powder
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| LogP |
4.3
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
3
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| Rotatable Bond Count |
9
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| Heavy Atom Count |
28
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| Complexity |
536
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| Defined Atom Stereocenter Count |
0
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| SMILES |
O(C)C1=CC=CC2C(/C=C/C(NCCC3C=CC=CC=3OCC=C)=O)=CNC=21
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| InChi Key |
BNTYDBBGNPFECO-VAWYXSNFSA-N
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| InChi Code |
InChI=1S/C23H24N2O3/c1-3-15-28-20-9-5-4-7-17(20)13-14-24-22(26)12-11-18-16-25-23-19(18)8-6-10-21(23)27-2/h3-12,16,25H,1,13-15H2,2H3,(H,24,26)/b12-11+
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| Chemical Name |
(E)-3-(7-methoxy-1H-indol-3-yl)-N-[2-(2-prop-2-enoxyphenyl)ethyl]prop-2-enamide
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| Synonyms |
JI 130; JI-130; JI130
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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.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.6564 mL | 13.2820 mL | 26.5640 mL | |
| 5 mM | 0.5313 mL | 2.6564 mL | 5.3128 mL | |
| 10 mM | 0.2656 mL | 1.3282 mL | 2.6564 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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