KKII5
Based on 1 Customer Validation
KKII5 is a potent Lipoxygenase (LOX-1) inhibitor with an IC50 of 19 μM. KKII5 inhibits lipid peroxidation.
For research use only. We do not sell to patients.
- Purity : 98.60%
- CAS No.: 6381-55-1
- Formula: C16H14N2S
- Molecular Weight:266.36
-
Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
Biological Activity
Description
IC50 & Target
IC50: 19 μM (LOX-1)[1]
Cellular Effect
|
Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| HEK293 | IC50 |
>10 μM
Compound: 5
|
Antagonist activity at human TRPA1 expressed in HEK293 cells assessed as inhibition of 5H-dibenzo[b,e]azepine-10-carboxylic acid methyl ester-induced increase in intracellular calcium by Fluo4-AM based fluorometric assay
Antagonist activity at human TRPA1 expressed in HEK293 cells assessed as inhibition of 5H-dibenzo[b,e]azepine-10-carboxylic acid methyl ester-induced increase in intracellular calcium by Fluo4-AM based fluorometric assay
|
[PMID: 22222037] |
In Vitro
KKII5 interacts with HIS499 of the cavity by forming one π–π stacking interaction between the phenyl ring of the molecule and the imidazole ring of HIS499[1].
KKII5 (100 μM) strongly inhibits lipid peroxidation with 98% inhibition[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
Chemical Information
-
CAS No. 6381-55-1
-
Appearance Solid
-
Molecular Weight 266.36
-
Formula C16H14N2S
-
Color White to off-white
-
SMILES
C1=CC=C(C=C1)C2C=C(NC(=S)N2)C3=CC=CC=C3
-
Shipping
Room temperature in continental US; may vary elsewhere.
-
Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvent & Solubility
In Vitro:
DMSO : 100 mg/mL (375.43 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)
Protocols
-
Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
-
Ferroptosis Solutions
Ferroptosis is an iron-dependent, non-apoptotic form of regulated cell death characterized by lethal lipid peroxidation and sensitivity to suppression by iron chelators or lipophilic radical-trapping antioxidants. The core pathway links cystine uptake through system Xc−, glutathione availability, GPX4-dependent detoxification of phospholipid hydroperoxides, iron-dependent oxidative reactions, and polyunsaturated-phospholipid metabolism into a cell-death program that is biochemically and morphologically distinct from apoptosis, necrosis, and autophagy. The ferroptosis pathway is experimentally linked to phenotype through chemical and genetic perturbation. Erastin induces ferroptosis by inhibiting cystine uptake through system Xc− and weakening antioxidant defenses, while GPX4 inhibition or depletion causes lipid peroxide accumulation and ferroptotic cancer-cell death. ACSL4 and oxidizable arachidonoyl- or adrenoyl-containing phosphatidylethanolamines shape ferroptosis sensitivity by con
Purity & Documentation
-
Data Sheet (273 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
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 | 3.7543 mL | 18.7716 mL | 37.5432 mL | 93.8579 mL |
| 5 mM | 0.7509 mL | 3.7543 mL | 7.5086 mL | 18.7716 mL | |
| 10 mM | 0.3754 mL | 1.8772 mL | 3.7543 mL | 9.3858 mL | |
| 15 mM | 0.2503 mL | 1.2514 mL | 2.5029 mL | 6.2572 mL | |
| 20 mM | 0.1877 mL | 0.9386 mL | 1.8772 mL | 4.6929 mL | |
| 25 mM | 0.1502 mL | 0.7509 mL | 1.5017 mL | 3.7543 mL | |
| 30 mM | 0.1251 mL | 0.6257 mL | 1.2514 mL | 3.1286 mL | |
| 40 mM | 0.0939 mL | 0.4693 mL | 0.9386 mL | 2.3464 mL | |
| 50 mM | 0.0751 mL | 0.3754 mL | 0.7509 mL | 1.8772 mL | |
| 60 mM | 0.0626 mL | 0.3129 mL | 0.6257 mL | 1.5643 mL | |
| 80 mM | 0.0469 mL | 0.2346 mL | 0.4693 mL | 1.1732 mL | |
| 100 mM | 0.0375 mL | 0.1877 mL | 0.3754 mL | 0.9386 mL |