| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg | |||
| 25mg | |||
| 50mg | |||
| 100mg | |||
| 250mg | |||
| Other Sizes |
Purity: ≥98%
| Targets |
JI051 targets the protein-protein interaction between Hes1 (a downstream effector of the Notch signaling pathway) and prohibitin 2 (PHB2). By stabilizing this interaction, JI051 promotes the formation of a complex that inhibits Hes1-mediated transcription. This leads to the suppression of Notch signaling and the induction of cell-cycle arrest.
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| ln Vitro |
G2/M cell cycle arrest is caused by JI051 [1]. HEK293 cell growth is markedly inhibited by JI051 (0.1-10 µM, 24 hours) with an EC50 of 0.3 µM [1].
In vitro, JI051 interacts with prohibitin 2 (PHB2) and inhibits the transcription of the Notch downstream effector Hes1. This leads to cell-cycle arrest and inhibits the proliferation of HEK293 cells and pancreatic cancer cells. The compound has demonstrated antitumor activity in various cancer cell lines. |
| ln Vivo |
In vivo, JI051 has been shown to have antitumor activity. However, detailed in vivo efficacy data for specific disease models are limited. JI051 is primarily used as a research tool for studying the role of Hes1-PHB2 interactions in cancer and Notch signaling. It has potential for use in oncology research.
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| Enzyme Assay |
In vitro binding assays for JI051 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 like surface plasmon resonance (SPR) to quantify the formation of the Hes1-PHB2 complex in the presence of the compound.
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| Cell Assay |
Cell Proliferation Assay[1]
Cell Types: HEK293 Cell Tested Concentrations: 0.1-10 µM Incubation Duration: 24 hrs (hours) Experimental Results: Dose-dependent inhibition of HEK293 cell proliferation at low concentrations. In vitro cellular assays for JI051 involve treating cancer cell lines with the compound and measuring cell viability, proliferation, and cell-cycle progression. The effects of the compound on Hes1 transcriptional activity are assessed by measuring the expression of Hes1 target genes. These assays confirm the compound's mechanism of action in a cellular context. |
| Animal Protocol |
In vivo animal models for JI051 may include xenograft tumor models to evaluate its antitumor efficacy. The compound is administered by appropriate routes, and tumor growth inhibition is measured. However, detailed animal protocol information for JI051 is limited in the available literature. The compound is primarily used as a research tool.
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| ADME/Pharmacokinetics |
JI051 has a molecular formula of C22H24N2O3 and a molecular weight of 364.44 g/mol. It is a solid compound that is soluble in DMSO at 125 mg/mL. The compound should be stored as a powder at -20°C for long-term stability. Its chemical name is (2E)-N-[2-(2-ethoxyphenyl)ethyl]-3-(7-methoxy-1H-indol-3-yl)prop-2-enamide.
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| Toxicity/Toxicokinetics |
JI051 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 cancer biology.
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| References | |
| Additional Infomation |
JI051 (CAS# 2234281-75-3) is a stabilizer of the Hes1-PHB2 protein-protein interaction. It interacts with prohibitin 2 (PHB2) and induces cell-cycle arrest by inhibiting the Notch downstream effector Hes1. The compound has antitumor activity and is for research use only. It is not approved for human therapeutic use.
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| Molecular Formula |
C22H24N2O3
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|---|---|
| Molecular Weight |
364.437565803528
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| Exact Mass |
364.178
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| CAS # |
2234281-75-3
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| Related CAS # |
2234281-75-3;
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| PubChem CID |
138319697
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| Appearance |
Light yellow to yellow solid powder
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| LogP |
4
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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 |
8
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| Heavy Atom Count |
27
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| Complexity |
496
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| Defined Atom Stereocenter Count |
0
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| SMILES |
O(CC)C1C=CC=CC=1CCNC(/C=C/C1=CNC2C(=CC=CC=21)OC)=O
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| InChi Key |
XIXIBPRUNJKZQI-VAWYXSNFSA-N
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| InChi Code |
InChI=1S/C22H24N2O3/c1-3-27-19-9-5-4-7-16(19)13-14-23-21(25)12-11-18-15-17-8-6-10-20(26-2)22(17)24-18/h4-12,15,24H,3,13-14H2,1-2H3,(H,23,25)/b12-11+
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| Chemical Name |
(E)-N-(2-Ethoxyphenethyl)-3-(7-methoxy-1H-indol-2-yl)acrylamide
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| Synonyms |
JI051 JI-051 JI 051
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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 (~342.99 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (5.71 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 (5.71 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (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 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.7439 mL | 13.7197 mL | 27.4394 mL | |
| 5 mM | 0.5488 mL | 2.7439 mL | 5.4879 mL | |
| 10 mM | 0.2744 mL | 1.3720 mL | 2.7439 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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