Kokusaginine

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Kokusaginine is a furoquinoline alkaloids, which exhibits inhibitory efficacy for acetylcholinesterase (AChE) with an IC₅₀ of 28.2 μM. Kokusaginine exhibits anti-proliferative and apoptotic inducing effects in MCF-7/ADR cells.

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Kokusaginine Chemical Structure

CAS No. : 484-08-2

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Description

IC₅₀ & Target

AChE

28.2 μM (IC₅₀)

Cellular Effect

Cell Line	Type	Value	Description	References
BMDM	IC₅₀	3.16 μM Compound: AC-542/20643020	Inhibition of GST-tagged recombinant RANKL/M-CSF-induced osteoclastogenesis in C57BL/6 mouse bone marrow derived macrophages assessed as TRAcP enzymatic activity incubated for 5 days with subsequent replenishment of media for 2 days and measured by leucoc Inhibition of GST-tagged recombinant RANKL/M-CSF-induced osteoclastogenesis in C57BL/6 mouse bone marrow derived macrophages assessed as TRAcP enzymatic activity incubated for 5 days with subsequent replenishment of media for 2 days and measured by leucoc	[PMID: 33158578]
MCF7	IC₅₀	7.23 μM Compound: Kokusaginine	Growth inhibition of human MCF7 cells after 48 hrs by MTT assay Growth inhibition of human MCF7 cells after 48 hrs by MTT assay	[PMID: 29903663]
MDA-MB-231	IC₅₀	9.01 μM Compound: Kokusaginine	Growth inhibition of human MDA-MB-231 cells after 48 hrs by MTT assay Growth inhibition of human MDA-MB-231 cells after 48 hrs by MTT assay	[PMID: 29903663]
NCI/ADR-RES	IC₅₀	4.62 μM Compound: Kokusaginine	Growth inhibition of human MCF7/ADR cells after 48 hrs by MTT assay Growth inhibition of human MCF7/ADR cells after 48 hrs by MTT assay	[PMID: 29903663]
Neutrophil	IC₅₀	61.8 μM Compound: 10	Immunomodulatory activity in polymorphoneutrophils assessed as inhibition of luminol-induced oxidative burst by chemiluminescence assay Immunomodulatory activity in polymorphoneutrophils assessed as inhibition of luminol-induced oxidative burst by chemiluminescence assay	[PMID: 18950230]

In Vitro

Kokusaginine (0-30 μM) inhibits proliferations of cells MCF-7, MDA-MB-231 and their multidrug resistant sublines MCF-7/ADR, MDA-MB-231/ADR, with IC₅₀s of 7.23, 4.62, 9.01 and 10.19 μM through inhibition of tubulin polymerization^[2].
Kokusaginine (6-24 μM) induces apoptosis in cells MCF-7 and MCF-7/ADR in a dose-dependent manner^[2].

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

Apoptosis Analysis^[2]

Cell Line:	MCF-7 and MCF-7/ADR
Concentration:	0-24 μM
Incubation Time:
Result:	Induced apoptosis.

Real Time qPCR^[2]

Cell Line:	MCF-7 and MCF-7/ADR
Concentration:	0-24 μM
Incubation Time:
Result:	Decreased mRNA levels of P-gp in cells MCF-7/ADR.

Molecular Weight

259.26

Formula

C₁₄H₁₃NO₄

CAS No.

484-08-2

SMILES

COC1=C(C=C2C(OC)=C3C(OC=C3)=NC2=C1)OC

Structure Classification

Initial Source

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

Handling Instructions (2659 KB)

References

[1]. Sichaem J, et al., Furoquinoline Alkaloids from the Leaves of Evodia lepta as Potential Cholinesterase Inhibitors and their Molecular Docking. Nat Prod Commun. 2015 Aug;10(8):1359-62. [Content Brief]

[2]. Chen H, et al., The inhibitory effect of kokusaginine on the growth of human breast cancer cells and MDR-resistant cells is mediated by the inhibition of tubulin assembly. Bioorg Med Chem Lett. 2018 Aug 1;28(14):2490-2492. [Content Brief]

Kokusaginine 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:

Kokusaginine484-08-2Cholinesterase (ChE)ApoptosisMicrotubule/TubulinMCF-7MDA-MB-231breast cancerneurodegenerative diseasesInhibitorinhibitorinhibit

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