1. Apoptosis Epigenetics Cell Cycle/DNA Damage
  2. Bcl-2 Family Apoptosis Caspase PARP
  3. 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.

For research use only. We do not sell to patients.

Mcl-1-IN-23

Mcl-1-IN-23 Chemical Structure

CAS No. : 2756736-34-0

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Description

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[1].

IC50 & Target[1]

MCL1

24 nM (IC50)

Caspase 3

 

Bim

 

Bak

 

In Vitro

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.

Apoptosis Analysis[1]

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.

Western Blot Analysis[1]

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.
Parmacokinetics
Species Dose Route Cmax Tmax T1/2 CL Vz AUC0-t Bioavailability
Rat[1] 2 mg/kg i.v. 3778.085 ng/mL / 3.86 h 36.42 mL/min/kg 11531.3 mL/kg 45884.4 min·ng/mL /
Rat[1] 10 mg/kg p.o. 591.421 ng/mL 1.0 h 3.05 h 121.68 mL/min/kg 32351.4 mL/kg 73456.4 min·ng/mL 32 %
In Vivo

Mcl-1-IN-23 (Compound 53) (2-10 mg/kg; intravenous injection, oral administration; single dose) exhibits excellent in vivo pharmacokinetic properties in SD rats, including an oral bioavailability of 32%[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Molecular Weight

655.25

Formula

C38H39ClN2O4S

CAS No.
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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation
References
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    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Mcl-1-IN-23
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HY-184310
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