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| 5mg |
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| 10mg |
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| Targets |
Cjoc-42 targets gankyrin, an ankyrin-repeat oncoprotein that is overexpressed in many cancer types. Gankyrin promotes cancer development by binding to and promoting the degradation of the tumor suppressor p53. By inhibiting gankyrin activity, Cjoc-42 prevents the decrease in p53 protein levels normally associated with high amounts of gankyrin. This restores p53-dependent transcription and sensitivity to DNA damage.
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| ln Vitro |
When compared to mock-transfected cells, cjoc42 (0.5, 1 and 5 μM; 48 hours) dose-dependently restores p53 levels and prevents gankyrin-induced p53 level drop in cells [1]. In terms of cell viability, cjoc42 alone (0.1, 1 and 10 μM; 24 hours) did not exhibit any dose-dependent alterations [1].
Cjoc-42 is a compound that binds to gankyrin and inhibits its activity in a dose-dependent manner. It prevents the decrease in p53 protein levels normally associated with high amounts of gankyrin. Cjoc-42 restores p53-dependent transcription and sensitivity to DNA damage. As a gankyrin inhibitor, it has potential for cancer prevention and in the DNA damage response. |
| ln Vivo |
In vivo, Cjoc-42 has potential for cancer prevention and in the DNA damage response by inhibiting gankyrin and restoring p53 function. As a gankyrin inhibitor, it is expected to exhibit antitumor activity in vivo by preventing p53 degradation and restoring tumor suppressor function. Specific in vivo efficacy studies and animal model data are not extensively documented. The compound is intended for research use only.
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| Enzyme Assay |
The in vitro binding assay for Cjoc-42 typically involves measuring its binding to gankyrin using surface plasmon resonance (SPR), isothermal titration calorimetry (ITC), or pull-down assays. The compound is incubated with recombinant gankyrin protein at varying concentrations (typically 0.001-100 µM), and binding affinity is determined. The inhibition of gankyrin activity is assessed by measuring the effects on p53 protein levels in cell-based assays.
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| Cell Assay |
Western Blot Analysis[1]
Cell Types: U2OS Tested Concentrations: 0.5, 1 and 5 μM Incubation Duration: 48 hrs (hours) Experimental Results: Dose-dependent restoration of p53 levels (compared to mock-transfected cells) and inhibition of gankyrin-induced decrease in p53 levels in cells . In vitro cellular assays for Cjoc-42 typically involve treating cancer cell lines with the compound at concentrations ranging from 0.001 to 10 µM for 24-72 hours. p53 protein levels are assessed by Western blot. p53-dependent transcription is assessed by measuring the expression of p53 target genes (such as p21, MDM2, and PUMA) by qPCR. Cell viability and apoptosis are assessed using MTT or CellTiter-Glo assays. The compound is dissolved in DMSO and diluted in cell culture medium. |
| Animal Protocol |
In vivo animal studies for Cjoc-42 are not extensively documented. For potential in vivo applications, the compound could be administered to mice via oral gavage or intraperitoneal injection at doses determined from preliminary studies. Tumor xenograft models using cancer cell lines with high gankyrin expression could be used to evaluate antitumor efficacy. Tumor growth is monitored by caliper measurements. p53 levels and target gene expression in tumors are assessed by Western blot and qPCR.
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| ADME/Pharmacokinetics |
Cjoc-42 has a molecular weight of 415.46 g/mol and formula C20H21N3O5S. Purity is typically 99.56%. The compound is soluble in DMSO and other organic solvents. Recommended storage is at -20°C. Detailed PK parameters such as half-life, Cmax, AUC, and bioavailability would require experimental determination.
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| Toxicity/Toxicokinetics |
Cjoc-42 is intended for research use only and is not approved for human therapeutic applications. As a gankyrin inhibitor that modulates p53 function, the compound may affect normal cell cycle regulation and DNA damage responses, which could contribute to potential toxicity. Standard preclinical toxicity assessments would include acute toxicity studies in rodents, repeated-dose toxicity studies, and assessment of off-target effects. Appropriate safety precautions should be taken when handling.
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| References | |
| Additional Infomation |
Cjoc-42 (CAS 2171519-89-2) is a potent and selective inhibitor of gankyrin with a molecular weight of 415.46 g/mol and formula C20H21N3O5S. It binds to gankyrin in a dose-dependent manner, preventing p53 degradation and restoring p53-dependent transcription and DNA damage sensitivity. The compound has potential for cancer prevention and in the DNA damage response. It is also known as cjoc42 and cjoc-42. The compound is not approved for clinical use.
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| Molecular Formula |
C20H21N3O5S
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|---|---|
| Molecular Weight |
415.46
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| Exact Mass |
415.12
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| CAS # |
2171519-89-2
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| Appearance |
Off-white to light yellow solid powder
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| LogP |
3.2
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| SMILES |
C(OC)(=O)C1=CC=C(N2C=C(CCCOS(C3=CC=C(C)C=C3)(=O)=O)N=N2)C=C1
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| InChi Key |
VYUDJPGSULLWAS-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C20H21N3O5S/c1-15-5-11-19(12-6-15)29(25,26)28-13-3-4-17-14-23(22-21-17)18-9-7-16(8-10-18)20(24)27-2/h5-12,14H,3-4,13H2,1-2H3
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| Chemical Name |
methyl 4-[4-[3-(4-methylphenyl)sulfonyloxypropyl]triazol-1-yl]benzoate
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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 Note: This product requires protection from light (avoid light exposure) during transportation and storage. |
| 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 : ~100 mg/mL (~240.70 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (6.02 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 25.0 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 | 2.4070 mL | 12.0349 mL | 24.0697 mL | |
| 5 mM | 0.4814 mL | 2.4070 mL | 4.8139 mL | |
| 10 mM | 0.2407 mL | 1.2035 mL | 2.4070 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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