THK01
Based on 1 publication(s) in Google Scholar
THK01 is a potent ROCK2 inhibitor with IC50 values of 5.7 and 923 nM for ROCK2 and ROCK1, respectively. THK01 inhibits breast cancer metastasis through the ROCK2-STAT3 signaling pathway. THK01 can be used in research of breast cancer.
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- Reinheit: 99.80%
- CAS. Nr.: 2226941-26-8
- Formel: C20H13N3O2
- Molecular Weight:327.34
-
Speicherung:
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
-
Biologische Aktivität
-
Chemical Information
-
Lösungsmittel & Löslichkeit
- Reinheit & Dokumentation
- Verweise
-
Help & FAQs
-
Cell Cycle/DNA Damage Compound Library
HY-L004
-
Kinase Inhibitor Library
HY-L009
-
Stem Cell Signaling Compound Library
HY-L017
-
TGF-beta/Smad Compound Library
HY-L018
-
Anti-Cancer Compound Library
HY-L025
-
Anti-Aging Compound Library
HY-L034
-
Reprogramming Compound Library
HY-L039
-
Cytoskeleton Compound Library
HY-L060
-
Anti-Breast Cancer Compound Library
HY-L074
-
Anti-Pulmonary Fibrosis Compound Library
HY-L125
-
Cancer Stem Cells Compound Library
HY-L135
-
Highly Selective Inhibitors Library
HY-L158
-
Serine/Threonine Kinase Inhibitor Library
HY-L164
-
Extracellular Vesicles (EVs) Compound Library
HY-L168
-
Multi-Target Compound Library
HY-L176
-
Bioactive Compound Library Max
HY-L181
-
MCE Bioactive Compound Library
HY-L001V
-
Bioactive Compound Library
HY-L001
-
High-Throughput Bioactive Compound Library
HY-L205
-
Posttranslational Modification Library
HY-L226
Publications Citing Use of MedChemExpress (MCE) THK01
More
Biologische Aktivität
|
ROCK2 5.7 nM (IC50) |
ROCK1 923 nM (IC50) |
|
Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| MDA-MB-231 | IC50 |
7.19 μM
Compound: 7; THK01
|
Antiproliferative activity against human MDA-MB-231 cells assessed as suppression of cell growth incubated for 72 hrs by SRB assay
Antiproliferative activity against human MDA-MB-231 cells assessed as suppression of cell growth incubated for 72 hrs by SRB assay
|
[PMID: 36764122] |
| PC-3 | IC50 |
21 μM
Compound: 2
|
Cytotoxicity against human PC3 cells after 72 hrs by SRB assay
Cytotoxicity against human PC3 cells after 72 hrs by SRB assay
|
[PMID: 29558119] |
| SK-OV-3 | IC50 |
4.44 μM
Compound: 7; THK01
|
Antiproliferative activity against human SK-OV-3 cells assessed as suppression of cell growth incubated for 72 hrs by SRB assay
Antiproliferative activity against human SK-OV-3 cells assessed as suppression of cell growth incubated for 72 hrs by SRB assay
|
[PMID: 36764122] |
THK01 (1.25-10 μM; 48 h) suppresses the migration and invasion abilities of MDA-MB-231 cells in a dose-dependent manner[1].
THK01 (5 μM; 24 h; MDA-MB-231 cells) suppresses breast cancer metastasis through STAT signal pathway[1].
THK01 (1.25-10 μM; 24 h; MDA-MB-231 cells) down-regulates the phosphorylation level of STAT3Y705 in a dose-dependent manner, while slightly up-regulates the level of STAT3S727[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Cell Line:MDA-MB-231 cells
-
Concentration:5 μM
-
Incubation Time:24 hours
-
Result:Down-regulated the phosphorylation levels (p-STAT) of STAT1, STAT2, and STAT3, up-regulated of p-STAT5A and STAT6.
-
Cell Line:MDA-MB-231 cells
-
Concentration:1.25, 2.5, 5, 10 μM
-
Incubation Time:24 hours
-
Result:Reduced the level of p-STAT3Y705 and increased the expression of p-STAT3S727 in MDA-MB-231 cells.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Animal Model:Female BALB/c nude mice with MDAMB-231-Luc-mcherry xenografts (6 weeks old, weight about 20 g)[1]
-
Dosage:15 mg/kg
-
Administration:Intravenous injection; once a day for 43 days
-
Result:Reduced the pulmonary metastasis of MDA-MB-231 in vivo with negligible toxicity.
Chemical Information
-
CAS. Nr. 2226941-26-8
-
Appearance Solid
-
Molecular Weight 327.34
-
Formel C20H13N3O2
-
Color Off-white to gray
-
SMILES
O=C1NCC2=C3C4=C(NC3=C5NC6=C(C5=C12)C=C(C=C6)O)C=CC=C4
-
Versand
Room temperature in continental US; may vary elsewhere.
-
Speicherung
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
Publications (1)
-
Journal Impact Factor
-
Most Recent
-
Clin Neuropharmacol
In Vitro Experiment Present ROCK2 Inhibition Promotes the Therapeutic Effect of Bevacizumab in the Treatment of Glioblastoma Multiforme. [Abstract]2024 Nov-Dec;47(6):193-200. PMID: 39792535
Lösungsmittel & Löslichkeit
DMSO : 125 mg/mL (381.87 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 (protect from light). 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 (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
Reinheit & Dokumentation
-
Data Sheet (278 KB)
-
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
-
Handling Instructions (2659 KB)
Verweise
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 (protect from light). 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 | 3.0549 mL | 15.2746 mL | 30.5493 mL | 76.3732 mL |
| 5 mM | 0.6110 mL | 3.0549 mL | 6.1099 mL | 15.2746 mL | |
| 10 mM | 0.3055 mL | 1.5275 mL | 3.0549 mL | 7.6373 mL | |
| 15 mM | 0.2037 mL | 1.0183 mL | 2.0366 mL | 5.0915 mL | |
| 20 mM | 0.1527 mL | 0.7637 mL | 1.5275 mL | 3.8187 mL | |
| 25 mM | 0.1222 mL | 0.6110 mL | 1.2220 mL | 3.0549 mL | |
| 30 mM | 0.1018 mL | 0.5092 mL | 1.0183 mL | 2.5458 mL | |
| 40 mM | 0.0764 mL | 0.3819 mL | 0.7637 mL | 1.9093 mL | |
| 50 mM | 0.0611 mL | 0.3055 mL | 0.6110 mL | 1.5275 mL | |
| 60 mM | 0.0509 mL | 0.2546 mL | 0.5092 mL | 1.2729 mL | |
| 80 mM | 0.0382 mL | 0.1909 mL | 0.3819 mL | 0.9547 mL | |
| 100 mM | 0.0305 mL | 0.1527 mL | 0.3055 mL | 0.7637 mL |
Powered by Bioz