| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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| 50mg | |||
| Other Sizes |
| Targets |
The primary target of TIBI is Rio1, an atypical protein kinase that is involved in ribosome biogenesis and cell cycle progression. TIBI acts as an ATP-competitive inhibitor, meaning it competes with ATP for binding to the kinase active site. It inhibits Rio1 with an IC50 of 0.09 μM and a Ki of 0.05 μM. TIBI enhances the thermal stability of the Rio1 enzyme, confirming its direct binding to the target.
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| ln Vitro |
In vitro, TIBI demonstrates potent inhibition of Rio1 kinase activity. The compound inhibits Rio1 with an IC50 of 0.09 μM and a Ki of 0.05 μM. TIBI enhances the thermal stability of the Rio1 enzyme, indicating that it stabilizes the protein upon binding. The compound's ATP-competitive mechanism of action is similar to that of fungamycin. However, detailed cellular activity data are not extensively reported in the available literature.
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| ln Vivo |
In vivo data for TIBI are not extensively reported in the available literature. As a potent Rio1 inhibitor, the compound has potential for in vivo applications in studying the role of Rio1 in cell growth and ribosome biogenesis. However, specific in vivo efficacy data, including animal models, dosing regimens, and pharmacokinetic-pharmacodynamic relationships, are not detailed in the available sources. The compound is classified as a research-use-only chemical.
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| Enzyme Assay |
In vitro enzyme assays for TIBI typically involve measuring its inhibition of Rio1 kinase activity. Recombinant Rio1 enzyme is incubated with a peptide substrate and ATP in the presence of varying concentrations of TIBI. The incorporation of phosphate into the substrate is measured, and the IC50 for inhibition is calculated. TIBI shows an IC50 of 0.09 μM. The Ki of 0.05 μM is determined from enzyme kinetics at different ATP concentrations. The compound's ability to enhance Rio1 thermal stability is assessed by thermal shift assays.
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| Cell Assay |
Cellular assays for TIBI are performed in cells to assess its effects on Rio1 function and downstream cellular processes. Cells are treated with TIBI, and the phosphorylation of Rio1 substrates is measured. The compound's effects on cell growth, proliferation, and ribosome biogenesis are also assessed. However, specific cellular assay protocols are not detailed in the available literature.
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| Animal Protocol |
In vivo animal studies with TIBI are not extensively documented in the available literature. Based on its inhibition of Rio1, potential in vivo models could include cancer models or models of ribosomopathies. However, specific protocols are not detailed in the available sources. The compound is intended for laboratory research use only.
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| ADME/Pharmacokinetics |
TIBI has a molecular weight of 621.72 and a molecular formula of C7H2I4N2. It is typically dissolved in DMSO for in vitro studies. The compound is stable when stored as a powder at -20°C and in solution at -80°C for up to 1 year. However, detailed pharmacokinetic parameters are not available in the literature for this research compound.
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| Toxicity/Toxicokinetics |
Comprehensive toxicology data for TIBI are not extensively reported. The compound is classified as a research-use-only chemical and is not intended for human consumption. As a tetraiodinated compound, it may have potential for iodine-related toxicity. Specific toxicological data, including acute toxicity, genotoxicity, and target organ effects, are not reported in the available literature.
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| Additional Infomation |
Structure in the first source
TIBI is a research-grade compound not approved for clinical use. Its primary application is as a pharmacological tool for studying Rio1 kinase. The compound is used to investigate the role of Rio1 in ribosome biogenesis, cell growth, and cell cycle progression. Its potent and ATP-competitive inhibition of Rio1 makes it a valuable tool for studying the structure and function of this atypical kinase. |
| Exact Mass |
621.639
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|---|---|
| CAS # |
1196457-06-3
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| PubChem CID |
44263430
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| Appearance |
White to off-white solid powder
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| LogP |
4.1
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
1
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| Rotatable Bond Count |
0
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| Heavy Atom Count |
13
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| Complexity |
203
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| Defined Atom Stereocenter Count |
0
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| SMILES |
C1=NC2=C(N1)C(=C(C(=C2I)I)I)I
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| InChi Key |
ZUHFPYANLLWSJR-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C7H2I4N2/c8-2-3(9)5(11)7-6(4(2)10)12-1-13-7/h1H,(H,12,13)
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| Chemical Name |
4,5,6,7-tetraiodo-1H-benzimidazole
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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 : ~50 mg/mL (~80.42 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.) |
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.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT00507806 | TERMINATED | Drug: perflutren lipid microsphere | Acute Ischemic Stroke | ImaRx Therapeutics | 2005-03 | Phase 1 Phase 2 |
| NCT01100918 | COMPLETED | Device: BiV ICD Device: ICD |
Heart Failure | Barts & The London NHS Trust | 2007-02 | Phase 4 |
| NCT05195983 | NOT YET RECRUITING | Acute Stroke | Assiut University | 2022-01-10 | ||
| NCT03764852 | RECRUITING | Procedure: outpatient laparoscopic Procedure: outpatient laparoscopic |
Pelvic Organ Prolapse | Centre Hospitalier Universitaire de Nice | 2019-12-14 | Not Applicable |
| NCT03290053 | TERMINATED | Drug: SonoVue Drug: Sodium chloride Procedure: Transcranial Ultrasound Procedure: Sham Transcranial Ultrasound |
Ischemic Stroke | Umeå University | 2017-11-28 | Phase 3 |
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