MitoBloCK-1
Based on 1 Customer Validation
MitoBloCK-1 (MB-1) is a TIM22 inhibitor. MitoBloCK-1 inhibits substrate translocation by preventing substrate binding to the tim9/10 complex, thereby preventing substrates from reaching the TIM22 translocase. MitoBloCK-1 inhibits the import of TIM22 substrate proteins into mitochondria. MitoBloCK-1 can be used in research on cardiac arrhythmia and P. aeruginosa infection.
For research use only. We do not sell to patients.
- Purity : 98.87%
- CAS No.: 373370-73-1
- Formula: C14H14BrN3O2S
- Molecular Weight:368.25
-
Storage:Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
Biological Activity
Description
In Vitro
MitoBloCK-1 blocks AAC translocation at an early outer-membrane stage by impairing Tim9-Tim10 complex binding in tim10-1 tim9S mitochondria[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Animal Model:CF-1 (female)[2]
-
Dosage:50 mg/kg
-
Administration:every 3 h; for 24 h
-
Result:Reduced the P. aeruginosa UC12120 population only by approximately 1 log at 24 h.
Some killing effects were observed after repeated dosing at the 18- and 21-h time points.
No recoverable resistant colonies were detected when mouse thigh samples were plated onto MHB plates containing 0.5, 1, and 2 µg/mL.
Clinical Trial
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | 2011-05 | PHASE1 |
Chemical Information
-
CAS No. 373370-73-1
-
Appearance Solid
-
Molecular Weight 368.25
-
Formula C14H14BrN3O2S
-
Color Off-white to light yellow
-
SMILES
S=C(N/N=C/C1=C2C(CCCC3)=C3OC2=CC(Br)=C1O)N
-
Synonyms
MB-1
-
Shipping
Room temperature in continental US; may vary elsewhere.
-
Storage
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
Solvent & Solubility
In Vitro:
DMSO : 1 mg/mL (2.72 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Purity & Documentation
-
Data Sheet (282 KB)
-
SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
-
Handling Instructions (2659 KB)
References
[3]. Hasson SA, et al. Substrate specificity of the TIM22 mitochondrial import pathway revealed with small molecule inhibitor of protein translocation. Proceedings of the National Academy of Sciences of the United States of America. 2010 May 25;107(21):9578-83. [Content Brief]
[4]. Ding YY, et al. Design, Synthesis, and Antimicrobial Activity Evaluation of Novel Isocryptolepine Derivatives against Phytopathogenic Fungi and Bacteria. Journal of agricultural and food chemistry. 2024 Sep 25;72(38):20831-20841. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.7155 mL | 13.5777 mL | 27.1555 mL | 67.8887 mL |