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  3. Mcl-1 inhibitor 6

Mcl-1 inhibitor 6 

Cat. No.: HY-132307
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Mcl-1 inhibitor 6 is an orally active, selective myeloid cell leukemia 1 (Mcl-1) protein inhibitor with a Kd of 0.23 nM and a Ki of 0.02 μM. Mcl-1 inhibitor 6 possesses superior selectivity over other Bcl-2 family members (Bcl-2, Bcl2A1, Bcl-xL, and Bcl-w, Kd>10 μM). Mcl-1 inhibitor 6 is a potent antitumor agent.

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

Mcl-1 inhibitor 6 Chemical Structure

Mcl-1 inhibitor 6 Chemical Structure

CAS No. : 2598978-56-2

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Description

Mcl-1 inhibitor 6 is an orally active, selective myeloid cell leukemia 1 (Mcl-1) protein inhibitor with a Kd of 0.23 nM and a Ki of 0.02 μM. Mcl-1 inhibitor 6 possesses superior selectivity over other Bcl-2 family members (Bcl-2, Bcl2A1, Bcl-xL, and Bcl-w, Kd>10 μM). Mcl-1 inhibitor 6 is a potent antitumor agent[1].

IC50 & Target[1]

Mcl-1

0.23 nM (Kd)

Mcl-1

0.02 μM (Ki)

Bcl-2

>10 μM (Kd)

Bcl-2

10 μM (Ki)

Bcl2A1

>10 μM (Kd)

Bcl-xL

>10 μM (Kd)

Bcl-W

>10 μM (Kd)

Bfl-1

1.57 μM (Ki)

In Vitro

Mcl-1 inhibitor 6 has Kis of 10 μM and 1.57μM for Bcl-2 and Bfl-1, respectively[1].
Mcl-1 inhibitor 6 (1, 5 μM; for 48 h) significantly induces apoptosis in a concentration-dependent manner[1].
Mcl-1 inhibitor 6 (0.1, 5 μM; for 4 h) remarkably upregulates PARP cleavage in H929 cells in a concentration-dependent manner[1].
Mcl-1 inhibitor 6 (for 72 h) shows antiproliferative activities against the tumor cell lines (H929, MV4-11, SK-BR-3, NCI-H23; IC50=0.36-3.02 μM). Mcl-1 inhibitor 6 shows ideal selectivity against CML cell line K562 (IC50>30 μM)[1].

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

Apoptosis Analysis[1]

Cell Line: H929 cells
Concentration: 1, 5 μM
Incubation Time: For 48 hours
Result: Significantly induced apoptosis in a concentration-dependent manner.

Western Blot Analysis[1]

Cell Line: H929 cells
Concentration: 0.1, 0.5, 1, 5 μM
Incubation Time: For 4 hours
Result: Remarkably upregulated PARP cleavage in H929 cells in a concentration-dependent manner.
In Vivo

Mcl-1 inhibitor 6 (compound 40; 60 mg/kg with PO or 20 mg/kg with IP; every two days for 14 days) shows desired in vivo tumor growth inhibition activity[1].
Mcl-1 inhibitor 6 (3 mg/kg with IV or 10 mg/kg with PO) has a T1/2 of 2.3 hours, a CL of 15.18 mL/min•kg by IV[1].

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

Animal Model: Balb/c nude female mice (7 weeks) loaded with MV4-11 xenografts[1]
Dosage: 60 mg/kg (PO) or 20 mg/kg (IP)
Administration: IP or PO; every two days for 14 days
Result: Showed desired in vivo tumor growth inhibition activity (T/C = 37.30% and 5.52% by po and ip administration, respectively).
Animal Model: SD rats (200-250 g)[1]
Dosage: 3 mg/kg (IV) or 10 mg/kg (PO) (Pharmacokinetic Analysis)
Administration: IV or PO
Result: Had a T1/2 of 2.3 hours, a CL of 15.18 mL/min•kg by IV.
Had a T1/2 of 2.1 hours, a CL of 36.8 mL/min•kg and a Cmax of 2012.95 ng/mL.
Molecular Weight

518.02

Formula

C₂₆H₂₈ClNO₆S

CAS No.
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Storage

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

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Mcl-1 inhibitor 6
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