Mcl-1-IN-23
Mcl-1-IN-23 is a Mcl-1 inhibitor with a Ki value of 0.024 μM. Mcl-1-IN-23 binds directly to Mcl-1 and displaces the pro-apoptotic proteins Bak and Bim from Mcl-1 complexes. Mcl-1-IN-23 induces cell apoptosis, activates caspase-3, promotes PARP cleavage, and exerts antiproliferative activity against cancer cells. Mcl-1-IN-23 can be used for the research of leukemia.
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- CAS. Nr.: 2756736-34-0
- Formel: C38H39ClN2O4S
- Molecular Weight:655.25
-
Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
Alle Caspase Isoform-spezifische Produkte anzeigen
More
Biologische Aktivität
|
MCL1 24 nM (IC50) |
Caspase 3 |
Bim |
Bak |
Mcl-1-IN-23 (Compound 53) reversibly binds to purified Mcl-1 protein at a 1:1 ratio, with a Kd value of 0.31 μM, and the binding process is jointly mediated by enthalpy and entropy[1].
Mcl-1-IN-23 serves as a long-acting ligand for purified GST-Mcl-1 protein, with a Kd value of 1.89 μM, and exhibits slow binding and dissociation kinetic processes[1].
Mcl-1-IN-23 (48 h) potently inhibits the proliferation of Mcl-1-sensitive Molm-13 cells with an IC50 of 0.45 μM; it remains active against Venetoclax (HY-15531)-resistant Molm-13_VenR cells with an IC50 of 1.16 μM; and it exhibits low micromolar activity against other hematological tumor cell lines[1].
Mcl-1-IN-23 (0-10 μM; 4 h) dose-dependently displaces the pro-apoptotic proteins Bim and Bak from Mcl-1 in Molm-13 cells, indicating that it can target and inhibit Mcl-1[1].
Mcl-1-IN-23 (0.3-3 μM; 48 h) induces apoptosis in Molm-13 cells in a dose-dependent manner[1].
Mcl-1-IN-23 (0-10 μM; 24 h) activates the apoptotic pathway in Molm-13 cells via concentration-dependent cleavage of PARP and Caspase-3, without affecting the expression levels of Bcl-2 or Bcl-xL, confirming that the apoptosis it induces is dependent on Mcl-1[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Cell Line:Molm-13 cells
-
Concentration:0.3, 1 and 3 μM
-
Incubation Time:48 h
-
Result:Induced apoptosis in Molm-13 cells, with significant increases in apoptotic cell populations observed at concentrations as low as 0.3 μM after 48 h.
-
Cell Line:Molm-13 cells
-
Concentration:0, 0.3, 1, 3 and 10 μM
-
Incubation Time:24 h
-
Result:Significantly increased the levels of cleaved RARP and Caspase 3.
Did not affect Bcl-2 or Bcl-xL levels.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
-
CAS. Nr. 2756736-34-0
-
Molecular Weight 655.25
-
Formel C38H39ClN2O4S
-
SMILES
ClC1=C(C)C=C(OCCCN2C(C)=C(S(=NCC3=CC=C(C4=CC=CC=C4)C=C3)(C5=CC=C(C)C=C5)=O)C(C)=C2C(O)=O)C=C1C
-
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)