EZH2/HSP90-IN-29
EZH2/HSP90-IN-29 is a dual inhibitor for EZH2 and HSP90, with IC50s of 6.29 nM and 60.1 nM, for EZH2 and HSP90, respectively. EZH2/HSP90-IN-29 increases apoptosis/necrosis-related gene expression, induces cell cycle arrest at M phase and inhibits reactive oxygen species (ROS) catabolism pathway. EZH2/HSP90-IN-29 is able to cross the blood-brain-barrier (BBB).
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- CAS. Nr.: 3033571-35-3
- Formel: C40H48N4O6
- Molecular Weight:680.83
-
Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
-
Biologische Aktivität
-
Chemical Information
- Protokoll
- Reinheit & Dokumentation
- Verweise
-
Help & FAQs
Alle Histone Methyltransferase Isoform-spezifische Produkte anzeigen
More
Biologische Aktivität
Beschreibung
IC50 & Target
|
EZH2 6.29 nM (IC50) |
HSP90 60.1 nM (IC50) |
Cellular Effect
|
Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| GBM | IC50 |
1.015 μM
Compound: 7
|
Cell growth inhibition of TMZ-resistant patient-derived human GBM cells assessed as cell viability incubated for 72 hrs by CCK8 assay
Cell growth inhibition of TMZ-resistant patient-derived human GBM cells assessed as cell viability incubated for 72 hrs by CCK8 assay
|
[PMID: 38285511] |
In Vitro
EZH2/HSP90-IN-29 inhibits cell proliferation against TMZ-resistant Glioblastoma (GBM) cell lines (with an IC50 of 1.015 μM) through modulation of EZH2 and HSP90 chaperone in a balanced manner[1].
EZH2/HSP90-IN-29 (5 μM) decreases centromere proteins (CENPs), CDK1 and cyclin B1, which regulates the kinetochore assembly and mitosis, arrests cell cycle at M phase[1].
EZH2/HSP90-IN-29 (2 μM) inhibits DNA repair capacity through downregulations of gene expreesions of RB Binding Protein (RBBP8), BRCA1, DNA repair and recombination protein RAD54B, RAD21, crossover junction endonuclease EME1 and BRIP1 in Pt3R cells[1].
EZH2/HSP90-IN-29 (5 μM) upregulates levels of ROS and cleaved caspase-3, increased mitochondria-derived ROS [1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Cell Line:Pt3R
-
Concentration:0-50 μM
-
Incubation Time:72 h
-
Result:Inhibited 50% cell viability with concentration of 1.015 μM.
-
Cell Line:Pt3 and Pt3R
-
Concentration:0-5 μM
-
Incubation Time:72 h
-
Result:Decreased expressions of CDK1 and cyclin B1, increased cleaved caspase-3.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Animal Model:Pt3R xenograft NOD.CB17-Prkdcscid/NCrCrl mice[1]
-
Dosage:10-20 mg/kg
-
Administration:i.p., twice a week for 40 days
-
Result:Inhibited tumor growth.
- RT-PCR
- RNA extraction experimental
- 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
- ROS/oxidative-stress fluorescent staining
- Apoptosis Solutions
- Protocol for Cell Cycle
- Real Time qPCR (Q-PCR)
Chemical Information
-
CAS. Nr. 3033571-35-3
-
Molecular Weight 680.83
-
Formel C40H48N4O6
-
SMILES
O=C(NCC1=C(C=C(NC1=O)C)C)C2=CC(C3=CC=CC(N(C(C4=CC(C(C)C)=C(C=C4O)O)=O)C)=C3)=CC(N(C5CCOCC5)CC)=C2C
-
Versand
Room temperature in continental US; may vary elsewhere.
-
Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Reinheit & Dokumentation
Verweise
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
EZH2/HSP90-IN-29 Related Classifications
HY-163288 Related Classifications
Powered by Bioz