TKL002
Based on 1 Customer Validation
TKL002 is a blood-brain barrier-permeable inhibitor of the CTH/H2S/NF-κB/EMT signaling axis. TKL002 induces G2/M phase cell cycle arrest and apoptosis in glioblastoma cells. TKL002 inhibits the migration and invasion of glioblastoma cells by upregulating E-cadherin and downregulating N-cadherin and vimentin. TKL002 is applicable to relevant research on glioblastoma.
연구목적의 판매만을 진행합니다. 환자를 대상으로 한 판매는 하지 않습니다.
- Purity : 98.08%
- CAS No.: 3098518-95-4
- 화학식: C21H20F4N4O
- 분자량:420.40
-
보관:Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
-
Biological Activity
-
Chemical Information
-
용액&용해도
- Protocol
- 순도&문서
- References
-
Help & FAQs
All Caspase Isoforms
More
Biological Activity
제품 설명
IC50 & Target
[1]|
NF-κB |
Caspase 3 |
Bax |
Bcl-2 |
Cellular Effect
|
Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| LNCaP | IC50 |
1.62 μM
Compound: 7d
|
Cytotoxicity against human LNCaP cells assessed as inhibition of cell viability incubated for 48 hrs by MTT assay
Cytotoxicity against human LNCaP cells assessed as inhibition of cell viability incubated for 48 hrs by MTT assay
|
[PMID: 39908792] |
In Vitro
TKL002 (0.625-10 μmol/L; 24-72 h) potently inhibits the proliferation of U87MG, U118MG, and U251MG glioblastoma cells in a dose- and time-dependent manner with selectivity over normal LX2 cells, exhibiting IC50 values ranging from 4.141 to 6.506 μmol/L across cell lines and time points[1].
TKL002 (6 μmol/L; 48 h) induces late apoptosis in U87MG glioblastoma cells, mediated via upregulation of Bax and caspase-3 and downregulation of Bcl-2 and active-caspase-3[1].
TKL002 (2-6 μmol/L; 24 h) induces G2/M phase cell cycle arrest in U87MG and U118MG glioblastoma cells in a concentration-dependent manner, with maximum G2/M fractions of 22.68% and 30.31% at 6 μmol/L respectively[1].
TKL002 (2-6 μmol/L; 48 h) reduces CTH, cysteine, and H2S levels, increases GSH levels, and inhibits NF-κB signaling and pro-inflammatory cytokine expression in U87MG and U118MG glioblastoma cells in vitro in a dose-dependent manner[1].
TKL002 (2-6 μmol/L; 48 h) inhibits migration and invasion of U87MG and U118MG glioblastoma cells in a dose-dependent manner, mediated via upregulation of E-cadherin and downregulation of N-cadherin and vimentin to suppress epithelial-mesenchymal transition[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Cell Line:U87MG
-
Concentration:2, 4, 6 μM
-
Incubation Time:48 h
-
Result:Increased late apoptosis to 22.63%.
-
Cell Line:U87MG, U118MG glioblastoma cells
-
Concentration:2, 4, 6 μM
-
Incubation Time:24 h
-
Result:Increased the G2/M phase fraction in a concentration-dependent manner.
-
Cell Line:U87MG, U118MG glioblastoma cells
-
Concentration:2, 4, 6 μM
-
Incubation Time:48 h
-
Result:Inhibited GBM cell migration.
-
Cell Line:U87MG, U118MG glioblastoma cells
-
Concentration:2, 4, 6 μM
-
Incubation Time:48 h
-
Result:Inhibited GBM cell invasion.
In Vivo
TKL002 (10-20 mg/kg; i.v., once every three days for a total of 5 administrations) can cross the blood-brain barrier, inhibit the growth of orthotopic glioblastoma in a dose-dependent manner, reduce tumor burden, maintain the physical condition of mice, and cause no obvious organ toxicity[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Animal Model:BALB/c nude (male, 4−5 weeks old, 16−18 g, subcutaneous xenograft model)[1]
-
Dosage:5 mg/kg; 20 mg/kg
-
Administration:i.p.; every other day; 7 total doses
-
Result:Reduced mean subcutaneous tumor weight to 1.117 g (5 mg/kg) and 0.530 g, compared to 1.458 g in vehicle control.
Achieved similar tumor weight and volume reduction as 5 mg/kg temozolomide at 20 mg/kg.
Showed dose-dependent reductions in splenic index.
Caused minimal pathological changes in liver, spleen, and kidney; no significant changes in heart, liver, lung, or kidney indices.
-
Animal Model:BALB/c nude (male, 4−5 weeks old, 16−18 g, orthotopic xenograft model)[1]
-
Dosage:10 mg/kg; 20 mg/kg
-
Administration:i.v. via tail vein; every 3 days; 5 total doses
-
Result:Reduced in vivo bioluminescent signal intensity to 13.62×104 photons/s (10 mg/kg) and 8.52×104 photons/s (20 mg/kg) on days 15 and 20, versus 25.21×104 photons/s in vehicle control.
Reduced ex vivo tumor bioluminescent signal intensity to 21.48×104 photons/s (10 mg/kg) and 9.20×104 photons/s (20 mg/kg), versus 63.88×104 photons/s in controls.
Maintained normal body condition in 20 mg/kg group, while control mice exhibited weight loss, reduced activity, and cachexia.
Showed marked, dose-dependent reductions in CTH-positive tumor area, with the 20 mg/kg group showing the most pronounced decrease.
Showed a higher survival rate in the 20 mg/kg group, though the difference was not statistically significant.
Caused no significant differences in organ indices among groups.
- Detection of Apoptosis
- TUNEL staining for apoptotic DNA fragmentation
- Flow cytometric DNA-content cell-cycle staining
- Annexin V plus membrane-impermeant dye apoptosis staining
- BrdU Incorporation Assay
- Cell migration
- Apoptosis Solutions
- Protocol for Cell Cycle
- Cell invasion
- Research Protocol for Inflammation-related Diseases
Chemical Information
-
CAS No. 3098518-95-4
-
Appearance Solid
-
분자량 420.40
-
화학식 C21H20F4N4O
-
Color Light yellow to yellow
-
SMILES
COC1=CC=C(C2=C1)N=C(C=C2C(F)(F)F)NC3=CC=C(C(F)=C3)N4CCNCC4
-
선적
Room temperature in continental US; may vary elsewhere.
-
보관
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
용액&용해도
In Vitro:
DMSO : 10 mg/mL (23.79 mM; ultrasonic and warming and heat to 60°C; 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)
순도&문서
-
Data Sheet (277 KB)
-
SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 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 | 2.3787 mL | 11.8934 mL | 23.7869 mL | 59.4672 mL |
| 5 mM | 0.4757 mL | 2.3787 mL | 4.7574 mL | 11.8934 mL | |
| 10 mM | 0.2379 mL | 1.1893 mL | 2.3787 mL | 5.9467 mL | |
| 15 mM | 0.1586 mL | 0.7929 mL | 1.5858 mL | 3.9645 mL | |
| 20 mM | 0.1189 mL | 0.5947 mL | 1.1893 mL | 2.9734 mL |
TKL002 Related Classifications
HY-181717 Related Classifications
Powered by Bioz