2. Apoptosis
  3. Bcl-2 Family Apoptosis
  4. Mcl-1-IN-22

Mcl-1-IN-22 is a selective Mcl-1 inhibitor with a Ki of 0.015 μM. Mcl-1-IN-22 binds selectively to Mcl-1, disrupts the Mcl-1/Bak complex to release free Bak, triggering intrinsic apoptosis. Mcl-1-IN-22 can be used for the research of ovarian cancer.

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

Mcl-1-IN-22

Mcl-1-IN-22 Chemical Structure

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Other Forms of Mcl-1-IN-22:

Mcl-1-IN-22 Related Antibodies

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Bcl-2 Bcl-xL Bcl-W Mcl-1 Bfl-1 Bcl-B Bax Bak Bim BNIP3 Bad

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Description

Mcl-1-IN-22 is a selective Mcl-1 inhibitor with a Ki of 0.015 μM. Mcl-1-IN-22 binds selectively to Mcl-1, disrupts the Mcl-1/Bak complex to release free Bak, triggering intrinsic apoptosis. Mcl-1-IN-22 can be used for the research of ovarian cancer[1].

IC50 & Target[1]

Mcl-1

0.015 μM (Ki)

Bak

 

In Vitro

Mcl-1-IN-22 (Compound N5) potently and selectively binds to purified Mcl-1 protein with a Ki of 0.015 μM, and exhibits minimal binding to Bcl-2, Bcl-xL, Bcl-w, and Bfl-1[1].
Mcl-1-IN-22 potently inhibits proliferation of Mcl-1-dependent A2780S, HO8910, H929, and MV411 cancer cells, has weak activity against ARH-77 cells, no activity against OVCAR3 cells, and low toxicity to normal HL-7702 and WI-38 cells[1].
Mcl-1-IN-22 (6 μM; 18 h) binds to intracellular Mcl-1 in A2780S cells, increasing the protein's thermal stability by raising its melting temperature by over 10 °C[1].
Mcl-1-IN-22 (3-6 μM) disrupts Bak-Mcl-1 complexes in A2780S cells in vitro in a concentration-dependent manner, increasing levels of free Bak[1].
Mcl-1-IN-22 (3-6 μM) induces apoptosis in A2780S cells in vitro in a concentration-dependent manner, with robust activation of caspase-9 and caspase-3 that exceeds the activity of AZD5991 at matching concentrations[1].
Mcl-1-IN-22 maintains potent antiproliferative activity against Cisplatin (HY-17394)-resistant A2780/CDDP cells, but its activity is dependent on Mcl-1 expression[1].
Mcl-1-IN-22 acts synergistically with Cisplatin and Paclitaxel (HY-B0015) to inhibit proliferation of A2780S and Cisplatin-resistant A2780/CDDP cells, with the strongest synergy observed with Paclitaxel in A2780/CDDP cells (CI = 0.4)[1].
Mcl-1-IN-22 (200 nM) does not exhibit significant binding affinity or inhibitory activity against HDAC 3, HDAC 4, HDAC 6, or HDAC 11 proteins[1].

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

Mcl-1-IN-22 Related Antibodies
In Vivo

Mcl-1-IN-22 (Compound N5) (10-30 mg/kg; i.p.; daily; 14 days) exhibits dose-dependent antitumor efficacy in A2780S ovarian cancer xenografts, with a TGI of 35.2% at 30 mg/kg[1].

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

Animal Model: Balb/c nude (female, 5 weeks old, 16−18 g, subcutaneous inoculation with A2780S cells)[1]
Dosage: 10 mg/kg; 30 mg/kg
Administration: i.p.; daily; 14 days
Result: Achieved 13.2% tumor growth inhibition (TGI) with a T/C value of 85.1%.
Achieved 35.2% TGI with a T/C value of 67.2%.
Caused no significant body weight loss.
Molecular Weight

552.49

Formula

C30H31Cl2N3O3
SMILES

O=C(NO)C1=CC=CC(CN(C2)CCC3=C2N(CCCOC4=CC(C)=C(Cl)C(C)=C4)C5=C3C=C(Cl)C=C5)=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-22 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-22Bcl-2 FamilyApoptosisA2780S cellscisplatin-resistant ovarian cancerBcl-2intrinsic apoptosisBakMcl-1ovarian cancer cellscisplatinovarian cancer xenograft modelsBcl-xLInhibitorinhibitorinhibit

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