Mcl-1 inhibitor 6

Name: Mcl-1 inhibitor 6
Brand: MedChemExpress
SKU: HY-132307
Rating: 4.5 (1 reviews)

Cat. No.: HY-132307 Purity: 98.40%: FAQs
Data Sheet SDS COA Handling Instructions

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Mcl-1 inhibitor 6 is an orally active, selective myeloid cell leukemia 1 (Mcl-1) protein inhibitor with a K_d of 0.23 nM and a K_i 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, K_d>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

CAS No. : 2598978-56-2

Size	Price	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 199	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 199	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	USD 175	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 280	In-stock	Estimated Time of Arrival: December 31
25 mg	USD 590	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 950	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 1500	In-stock	Estimated Time of Arrival: December 31
200 mg		Get quote
500 mg		Get quote

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Customer Review

Based on 1 publication(s) in Google Scholar

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

Biological Activity
Purity & Documentation
References
Customer Review

Description

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)

Cellular Effect

Cell Line	Type	Value	Description	References
K562	IC₅₀	> 30 μM Compound: 40	Antiproliferative activity against human K562 cells assessed as decrease in cell viability measured after 72 hrs by MTT assay Antiproliferative activity against human K562 cells assessed as decrease in cell viability measured after 72 hrs by MTT assay	[PMID: 34342996]
MV4-11	IC₅₀	0.7 μM Compound: 40	Antiproliferative activity against human MV4-11 cells assessed as decrease in cell viability measured after 72 hrs by MTT assay Antiproliferative activity against human MV4-11 cells assessed as decrease in cell viability measured after 72 hrs by MTT assay	[PMID: 34342996]
NCI-H23	IC₅₀	3.02 μM Compound: 40	Antiproliferative activity against human NCI-H23 cells assessed as decrease in cell viability measured after 72 hrs by MTT assay Antiproliferative activity against human NCI-H23 cells assessed as decrease in cell viability measured after 72 hrs by MTT assay	[PMID: 34342996]
NCI-H929	IC₅₀	0.36 μM Compound: 40	Antiproliferative activity against human NCI-H929 cells assessed as decrease in cell viability measured after 72 hrs by MTT assay Antiproliferative activity against human NCI-H929 cells assessed as decrease in cell viability measured after 72 hrs by MTT assay	[PMID: 34342996]
SK-BR-3	IC₅₀	2.84 μM Compound: 40	Antiproliferative activity against human SK-BR-3 cells assessed as decrease in cell viability measured after 72 hrs by MTT assay Antiproliferative activity against human SK-BR-3 cells assessed as decrease in cell viability measured after 72 hrs by MTT assay	[PMID: 34342996]

In Vitro

Mcl-1 inhibitor 6 has K_is 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.

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 T_1/2 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 T_1/2 of 2.3 hours, a CL of 15.18 mL/min•kg by IV. Had a T_1/2 of 2.1 hours, a CL of 36.8 mL/min•kg and a C_max of 2012.95 ng/mL.

Molecular Weight

518.02

Formula

C₂₆H₂₈ClNO₆S

CAS No.

2598978-56-2

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
10 mM	0.1930 mL	0.9652 mL	1.9304 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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Dilution Calculator

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

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

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(per animal)

μL

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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

Purity: 98.40%

Select Batch:

Data Sheet (277 KB) SDS (251 KB)

COA (249 KB) HNMR (142 KB) RP-HPLC (270 KB) MS (97 KB)

Handling Instructions (2659 KB)

References

[1]. Peng-Ju Zhu, et al. Discovery of 3,5-Dimethyl-4-Sulfonyl-1 H-Pyrrole-Based Myeloid Cell Leukemia 1 Inhibitors with High Affinity, Selectivity, and Oral Bioavailability. J Med Chem. 2021 Aug 12;64(15):11330-11353. [Content Brief]

Complete Stock Solution Preparation Table

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

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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Mcl-1 inhibitor 6

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Mcl-1 inhibitor 6 Related Classifications

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