2. Apoptosis
  3. Bcl-2 Family Apoptosis
  4. Mcl-1 inhibitor 6

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.

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Mcl-1 inhibitor 6 Chemical Structure

Mcl-1 inhibitor 6 Chemical Structure

CAS No. : 2598978-56-2

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
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10 mM * 1 mL in DMSO USD 199 In-stock
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Based on 1 publication(s) in Google Scholar

Mcl-1 inhibitor 6 Related Antibodies

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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].

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

Mcl-1 inhibitor 6 Related Antibodies

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].

MedChemExpress (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.
Appearance

Solid

Color

White to off-white

SMILES

O=C(C1=C(C)C(S(=O)(C2=CC=C(C(C)=O)C=C2)=O)=C(C)N1CCCOC3=CC(C)=C(Cl)C(C)=C3)O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (193.04 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.9304 mL 9.6521 mL 19.3043 mL
5 mM 0.3861 mL 1.9304 mL 3.8609 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.9304 mL 9.6521 mL 19.3043 mL 48.2607 mL
5 mM 0.3861 mL 1.9304 mL 3.8609 mL 9.6521 mL
10 mM 0.1930 mL 0.9652 mL 1.9304 mL 4.8261 mL
15 mM 0.1287 mL 0.6435 mL 1.2870 mL 3.2174 mL
20 mM 0.0965 mL 0.4826 mL 0.9652 mL 2.4130 mL
25 mM 0.0772 mL 0.3861 mL 0.7722 mL 1.9304 mL
30 mM 0.0643 mL 0.3217 mL 0.6435 mL 1.6087 mL
40 mM 0.0483 mL 0.2413 mL 0.4826 mL 1.2065 mL
50 mM 0.0386 mL 0.1930 mL 0.3861 mL 0.9652 mL
60 mM 0.0322 mL 0.1609 mL 0.3217 mL 0.8043 mL
80 mM 0.0241 mL 0.1207 mL 0.2413 mL 0.6033 mL
100 mM 0.0193 mL 0.0965 mL 0.1930 mL 0.4826 mL
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Mcl-1 inhibitor 6 Related Classifications

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 inhibitor 62598978-56-2Bcl-2 FamilyApoptosisorallyPARPH929MV4-11SK-BR-3NCI-H23Inhibitorinhibitorinhibit

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