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Cat. No.: HY-152191

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ChoKα inhibitor-3

ChoKα inhibitor-3 is a sulphur-containing choline kinase inhibitor. ChoKα inhibitor-3 can inhibit HChoK α1 with an IC₅₀ value of 0.66 μM. ChoKα inhibitor-3 also can induce apoptosis. ChoKα inhibitor-3 can be used for the research of cancer.

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

CAS No.: 2883822-56-6
Formula: C₄₂H₄₂Br₂Cl₂N₄S₂
Molecular Weight:897.65

Storage:

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

Data Sheet (271 KB)

ChoKα inhibitor-3 Chemical Structure

CAS No.: 2883822-56-6

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Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
Chemical Information
Purity & Documentation
References
Calculators
Help & FAQs
Classifications
Bioz

Biological Activity

Description

IC₅₀ & Target

IC50: 0.66 μM (HChoK α1); 0.53 μM (A549); 0.26 μM (HeLa); 3.0 μM (HT-29); 1.34 μM (MCF7)^[1]

Cellular Effect

Cell Line	Type	Value	Description	References
A549	GI₅₀	0.53 μM Compound: PL 48	Antiproliferative activity against human A549 cells assessed as inhibition of cell growth incubated for 72 hrs Antiproliferative activity against human A549 cells assessed as inhibition of cell growth incubated for 72 hrs	[PMID: 36493617]
Astrocyte	GI₅₀	5 μM Compound: PL 48	Antiproliferative activity against human Astrocyte cells assessed as inhibition of cell growth incubated for 72 hrs by resazurin dye based assay Antiproliferative activity against human Astrocyte cells assessed as inhibition of cell growth incubated for 72 hrs by resazurin dye based assay	[PMID: 36493617]
HeLa	GI₅₀	0.26 μM Compound: PL 48	Antiproliferative activity against human HeLa cells assessed as inhibition of cell growth incubated for 72 hrs Antiproliferative activity against human HeLa cells assessed as inhibition of cell growth incubated for 72 hrs	[PMID: 36493617]
HT-29	GI₅₀	3 μM Compound: PL 48	Antiproliferative activity against human HT-29 cells assessed as inhibition of cell growth incubated for 72 hrs Antiproliferative activity against human HT-29 cells assessed as inhibition of cell growth incubated for 72 hrs	[PMID: 36493617]
MCF-10A	GI₅₀	2.6 μM Compound: PL 48	Antiproliferative activity against human MCF-10A cells assessed as inhibition of cell growth incubated for 72 hrs by resazurin dye based assay Antiproliferative activity against human MCF-10A cells assessed as inhibition of cell growth incubated for 72 hrs by resazurin dye based assay	[PMID: 36493617]
MCF7	GI₅₀	1.34 μM Compound: PL 48	Antiproliferative activity against human MCF7 cells assessed as inhibition of cell growth incubated for 72 hrs Antiproliferative activity against human MCF7 cells assessed as inhibition of cell growth incubated for 72 hrs	[PMID: 36493617]

In Vitro

ChoKα inhibitor-3 (PL 48) has HChoK α1 inhibition activity with an IC₅₀ value of 0.66 μM^[1].
ChoKα inhibitor-3 (1.46 μM; 72 h) can inhibit cell proliferation for A549, HeLa, HT-29 and MCF7 cells with IC₅₀ values of 0.53 μM, 0.26 μM, 3.0 μM and1.34 μM, respectively^[1].
ChoKα inhibitor-3 (1, 5 μM; 48, 72 h) induces apoptosis in cancer cells through the mitochondrial pathway^[1].

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

Cell Proliferation Assay^[1]

Cell Line:

HT29, A549, HeLa, HT-29 and MCF7 cells
Concentration:

1.46 μM
Incubation Time:

72 h
Result:

Had excellent growth inhibitory property.

Apoptosis Analysis^[1]

Cell Line:

A549 and HeLa cells
Concentration:

1, 5 μM
Incubation Time:

48, 72 h
Result:

Induced a stronger mitochondrial depolarization in HeLa cells at early time-point treatment (24 h).

Western Blot Analysis^[1]

Cell Line:

HeLa and NHA cells
Concentration:

5 μM
Incubation Time:

48 h
Result:

Significantly reduced the expression of the anti-apoptotic protein MCL-1.

Chemical Information

CAS No. 2883822-56-6
Molecular Weight 897.65
Formula C₄₂H₄₂Br₂Cl₂N₄S₂
SMILES

ClC1=CC2=[N+](CC3=CC=C(SCCSC4=CC=C(C[N+]5=C6C=C(Cl)C=CC6=C(N7CCCC7)C=C5)C=C4)C=C3)C=CC(N8CCCC8)=C2C=C1.[Br-].[Br-]
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

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (271 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[1]. Pilar M Luque-Navarro, et al. New bioisosteric sulphur-containing choline kinase inhibiPilar M Luque-Navarro, et al. New bioisosteric sulphur-containing choline kinase inhibitors with a tracked mode of action. Eur J Med Chem. 2023 Jan 15;246:115003.tors with a tracked mode of action. Eur J Med Chem. 2023 Jan 15;246:115003. [Content Brief]

Calculators

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Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Keywords

100 mg

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