2. Apoptosis
  3. Bcl-2 Family Caspase Apoptosis
  4. Mcl-1-IN-16

Mcl-1-IN-16 is an effective macrocyclic myeloid cell leukemia 1 (Mcl-1) inhibitor with a Ki of below 0.08 nM. Mcl-1-IN-16 maintains high selectivity (>50,000-fold) for Mcl-1 over other antiapoptotic Bcl-2 family members Bcl-2 and Bcl-xL. Mcl-1-IN-16 leads to the activation of caspase-3/7, thereby initiating cell apoptosis. Mcl-1-IN-16 achieves tumor regression in a lung cancer-derived tumor xenograft mice model. Mcl-1-IN-16 can be used in the research of solid tumor such as nonsmall cell lung cancer (NSCLC).

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

Mcl-1-IN-16

Mcl-1-IN-16 Chemical Structure

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Mcl-1-IN-16 Related Antibodies

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Description

Mcl-1-IN-16 is an effective macrocyclic myeloid cell leukemia 1 (Mcl-1) inhibitor with a Ki of below 0.08 nM. Mcl-1-IN-16 maintains high selectivity (>50,000-fold) for Mcl-1 over other antiapoptotic Bcl-2 family members Bcl-2 and Bcl-xL. Mcl-1-IN-16 leads to the activation of caspase-3/7, thereby initiating cell apoptosis. Mcl-1-IN-16 achieves tumor regression in a lung cancer-derived tumor xenograft mice model. Mcl-1-IN-16 can be used in the research of solid tumor such as nonsmall cell lung cancer (NSCLC)[1].

IC50 & Target[1]

Mcl-1

< 0.08 nM (Ki)

Caspase-3

8.8 nM (EC50)

Caspase-7

11 nM (EC50)

In Vitro

Mcl-1-IN-16 (Compound 13) inhibits cell proliferation with an GI50 value of 14 and 25 nM against H929 and A427 cells, and does not show inhibitory effect on K562 cells[1].
Mcl-1-IN-16 (4 h) activates Caspase 3/7 in H929 and A427 cells of EC50s of 8.8 and 11 nM[1].

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

Mcl-1-IN-16 Related Antibodies
In Vivo

Mcl-1-IN-16 (Compound 13) (30-60 mg/kg, i.v., once every 14 days for 28 days) induces tumor regression as a single agent in a NSCLC A427-derived xenograft mice model[1].

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

Animal Model: A427 cell line-derived NSCLC xenograft model established in Balb/c nude, female mice[1]
Dosage: 30 and 60 mg/kg
Administration: Intravenous injection (i.v.), once every 14 days for 28 days
Result: Achieved complete tumor regression at 60 mg/kg, with the therapeutic effect lasting for 50 days after administration.
No weight loss or clinical signs of toxicity.
Molecular Weight

800.73

Formula

C42H43Cl2N5O7
SMILES

CC1=C(Cl)C(C)=CC(OCCCC2=C(C(N(C3=CC(OC)=C(OC)C4=C3N(CCCOC5)C(C(O)=O)=C4)C[C@H]6C)=O)N6C7=C2C=CC(Cl)=C7C(C5=N8)=CN8C)=C1
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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Mcl-1-IN-16 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    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.

Keywords:

Mcl-1-IN-16Bcl-2 FamilyCaspaseApoptosisH929 cellsA427 cellssolid tumornonsmall cell lung cancermice modelInhibitorinhibitorinhibit

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