Cat. No.: HY-N21890

O-Methylbulbocapnine

O-Methylbulbocapnine is an aporphine alkaloid that acts as an inhibitor of LPS-induced inflammatory signaling and a dopamine D1R antagonist. O-Methylbulbocapnine inhibits LPS-induced phosphorylation of p38, ERK1/2, c-Jun, NF-κB p65 at Ser536, and Akt, decreases MyD88 protein levels, and reduces NF-κB nuclear translocation and DNA-binding activity. O-Methylbulbocapnine inhibits LPS-induced production of IL-6, TNF-α, PGE₂, and NO, and decreases COX-2 and iNOS expression. O-Methylbulbocapnine can be used for research on Alzheimer's disease, cervical cancer, breast cancer, and malaria.

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

CAS No.: 2490-83-7
Formula: C₂₀H₂₁NO₄
Molecular Weight:339.39

Storage:

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

O-Methylbulbocapnine Chemical Structure

CAS No.: 2490-83-7

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Use of MCE Products

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

^[1]^[2]^[3]^[4]^[5]^[6]^[7]^[8]^[9]^[10]

p38

ERK1

ERK2

c-Jun

NF-κB

p65

Akt

IL-6

COX-2

TNF-α

PGE2

iNOS

All p38 MAPK Isoforms :

All ERK Isoforms :

All NF-κB Isoforms :

All Akt Isoforms :

All Interleukin Related Isoforms :

All TNF Receptor Isoforms :

All COX Isoforms :

All NO Synthase Isoforms :

Cellular Effect

Cell Line	Type	Value	Description	References
HeLa	IC50	70.37 μM	Antiproliferative activity against human HeLa cells assessed as reduction in cell viability incubated for 72 hrs by Sulforhodamine B assay. Antiproliferative activity against human HeLa cells assessed as reduction in cell viability incubated for 72 hrs by Sulforhodamine B assay.	28703314
MDA-MB-231	IC50	56.59 μM	Antiproliferative activity against human MDA-MB231 cells assessed as reduction in cell viability incubated for 72 hrs by Sulforhodamine B assay. Antiproliferative activity against human MDA-MB231 cells assessed as reduction in cell viability incubated for 72 hrs by Sulforhodamine B assay.	28703314
MCF7	IC50	39.36 μM	Antiproliferative activity against human MCF-7 cells assessed as reduction in cell viability incubated for 72 hrs by Sulforhodamine B assay. Antiproliferative activity against human MCF-7 cells assessed as reduction in cell viability incubated for 72 hrs by Sulforhodamine B assay.	28703314
184B5	IC50	73.26 μM	Antiproliferative activity against human 184B5 cells assessed as reduction in cell viability incubated for 72 hrs by Sulforhodamine B assay. Antiproliferative activity against human 184B5 cells assessed as reduction in cell viability incubated for 72 hrs by Sulforhodamine B assay.	28703314

In Vitro

Innate ImmunityLipid Inflammatory MediatorsCytokines & ChemokinesOxidative StressAnti-cancerOthersAβ/Tau/α-Synuclein Aggregation

Innate Immunity

O-Methylbulbocapnine (OMP) (2.5-15 µg/mL; 2 h pretreatment and 24 h LPS stimulation) inhibits LPS-induced IL-6 production, TNF-α production, and reduces TNF-α production to 42% in RAW264.7 macrophages at 15 µg/mL^[1].

Lipid Inflammatory Mediators

Innate Immunity

Cytokines & Chemokines

O-Methylbulbocapnine (2.5-15 µg/mL; 2 h pre-treatment and 24 h LPS stimulation) inhibits LPS-induced PGE₂ production and suppresses COX-2 expression in RAW264.7 macrophages^[1].

Oxidative Stress

Innate Immunity

Cytokines & Chemokines

O-Methylbulbocapnine (2.5-15 µg/mL; 2 h pre-treatment and 24 h LPS stimulation) inhibits LPS-induced iNOS protein expression in RAW264.7 macrophages^[1].

Innate Immunity

Cytokines & Chemokines

O-Methylbulbocapnine (2.5-15 µg/mL; 2 h pre-treatment and 30 min LPS stimulation) inhibits LPS-induced c-Jun translocation and phosphorylation in RAW264.7 macrophages^[1].
O-Methylbulbocapnine (2.5-15 µg/mL; 2 h pre-treatment and 30 min LPS stimulation) inhibits LPS-induced phosphorylation of NF-κB p65 at Ser536 in RAW264.7 macrophages, but does not affect IκB-α degradation or p65 nuclear translocation^[1].
O-Methylbulbocapnine (2.5-15 µg/mL) inhibits LPS-induced phosphorylation of ERK1/2, p38, and Akt, and decreases MyD88 protein levels in RAW264.7 macrophages^[1].

Anti-cancer

O-Methylbulbocapnine (OMBC) (5-30 µg/mL; 24 h) is cytotoxic to HT1080 human fibrosarcoma cells only at concentrations above 20 µg/mL, thereby establishing a non-toxic dose range below 15 µg/mL^[2].
O-Methylbulbocapnine (5-15 µg/mL; 18 h) inhibits HT1080 human fibrosarcoma cell invasion in a dose-dependent manner^[2].
O-Methylbulbocapnine (2.5-15 µg/mL; 24 h) decreases uPA secretion from HT1080 human fibrosarcoma cells in a dose-dependent manner^[2].
O-Methylbulbocapnine (5-15 µg/mL; 24 h) decreases MT1-MMP expression in HT1080 human fibrosarcoma cells in a dose-dependent manner^[2].
O-methylbulbocapnine (72 h) exhibits moderate antiproliferative activity against HeLa, MDA-MB231, MCF-7, and 184B5 cell lines, with IC₅₀ values ranging from 39.36 to 73.26 μM^[10].

Others

O-Methylbulbocapnine (0-15 µg/mL; 24 h) reduces the secretion of MMP-9 (IC₅₀ 15 µg/mL) and MMP-2 in HT1080 human fibrosarcoma cells in a dose-dependent manner^[2].
O-methylbulbocapnine (50 μM; 1 h) acts as a D1R antagonist in HEK293-D1R cells^[3].
O-methylbulbocapnine displays relatively low micromolar D1R antagonistic activity in HEK293-D1R cells, with an IC₅₀ of 79.6 μM^[3].

Innate Immunity

Anti-cancer

O-Methylbulbocapnine (10 µg/mL; 24 h) significantly reduces NF-κB DNA-binding activity in HT1080 human fibrosarcoma cells at a concentration of 10 µg/mL^[2].

Aβ/Tau/α-Synuclein Aggregation

O-methylbulbocapnine (A2) (0.002-0.01 mg/mL; 24 h) inhibits human proinsulin fibril formation in a dose-dependent manner^[4].

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

ELISA Assay^[1]

Cell Line:

RAW264.7
Concentration:

2.5 µg/mL; 5 µg/mL; 10 µg/mL; 15 µg/mL
Incubation Time:

2 h (pre-treatment); 24 h (LPS stimulation)
Result:

Decreased LPS-induced IL-6 production in a dose-dependent manner.
Reduced LPS-induced TNF-α to 42% compared with the control at 15 µg/mL.

ELISA Assay^[1]

Cell Line:

RAW264.7
Concentration:

2.5 µg/mL; 5 µg/mL; 10 µg/mL; 15 µg/mL
Incubation Time:

2 h (pre-treatment); 24 h (LPS stimulation)
Result:

Inhibited PGE₂ production.
Suppressed the LPS-induced expression of COX-2 in a dose-dependent manner.

Western Blot Analysis^[1]

Cell Line:

RAW264.7
Concentration:

2.5 µg/mL; 5 µg/mL; 10 µg/mL; 15 µg/mL
Incubation Time:

2 h (pre-treatment); 24 h (LPS stimulation)
Result:

Decreased LPS-induced COX-2 expression by more than 50% at 10 µg/mL.
Decreased LPS-stimulated iNOS protein expression in a dose-dependent manner.
Reduced LPS-induced iNOS expression by more than 50% at 5 µg/mL.

Western Blot Analysis^[1]

Cell Line:

RAW264.7
Concentration:

2.5 µg/mL; 5 µg/mL; 10 µg/mL; 15 µg/mL
Incubation Time:

2 h (pre-treatment); 30 min (LPS stimulation)
Result:

Reduced LPS-induced translocation of c-Jun (AP-1) in a dose-dependent manner.
Inhibited LPS-induced phosphorylation of c-Jun.

Western Blot Analysis^[1]

Cell Line:

RAW264.7
Concentration:

2.5 µg/mL; 5 µg/mL; 10 µg/mL; 15 µg/mL
Incubation Time:

2 h (pre-treatment); 30 min (LPS stimulation)
Result:

Did not affect LPS-induced IκB-α degradation.
Did not affect the LPS-induced translocation of p65.
Inhibited the LPS-induced phosphorylation of p65.

Cell Cytotoxicity Assay^[2]

Cell Line:

HT1080 human fibrosarcoma cells
Concentration:

5 µg/mL; 10 µg/mL; 15 µg/mL; 20 µg/mL; 25 µg/mL; 30 µg/mL
Incubation Time:

24 h
Result:

Showed a cytotoxic effect on HT1080 cells at concentrations of more than 20 µg/mL.
Selected a non-toxic dose of less than 15 µg/mL for subsequent experiments.

Cell Invasion Assay^[2]

Cell Line:

HT1080 human fibrosarcoma cells
Concentration:

5 µg/mL; 10 µg/mL; 15 µg/mL
Incubation Time:

18 h
Result:

Reduced chemo-invasion to 49% at 15 µg/mL.

ELISA Assay^[2]

Cell Line:

HT1080 human fibrosarcoma cells
Concentration:

10 µg/mL
Incubation Time:

24 h
Result:

Significantly reduced NF-κB DNA binding activity.

Related Protocols :

Chemical Information

CAS No. 2490-83-7
Molecular Weight 339.39
Formula C₂₀H₂₁NO₄
SMILES

COC1=C2C3=C(OCO4)C4=CC5=C3[C@](N(CC5)C)([H])CC2=CC=C1OC
Structure Classification
- Alkaloids
- Quinoline Alkaloids
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]. Yodkeeree S, et al. O-Methylbulbocapnine and Dicentrine Suppress LPS-Induced Inflammatory Response by Blocking NF-κB and AP-1 Activation through Inhibiting MAPKs and Akt Signaling in RAW264.7 Macrophages. Biological & pharmaceutical bulletin. 2018;41(8):1219-1227.

[2]. Yodkeeree S, et al. Anti-invasion effect of crebanine and O-methylbulbocapnine from Stephania venosa via down-regulated matrix metalloproteinases and urokinase plasminogen activator. Chemical & pharmaceutical bulletin. 2013;61(11):1156-65.

[3]. Kang H, et al. Discovery of dopamine D1 receptor antagonists from Stephania epigaea using label-free cell phenotypic assays. Fitoterapia. 2025 Oct;186:106832.

[4]. HY-N21890-3.pdf

[5]. Chen JJ, et al. Anti-platelet aggregation alkaloids and lignans from Hernandia nymphaeifolia. Planta medica. 2000 Apr;66(3):251-6.

[6]. Stévigny C, et al. Cytotoxic and antitumor potentialities of aporphinoid alkaloids. Current medicinal chemistry. Anti-cancer agents. 2005 Mar;5(2):173-82.

[7]. HY-N21890-8.pdf

[8]. Peng CaiYing PC, et al. A new alkaloid from the fruit of Nandina domestica Thunb.

[9]. Chen KS, et al. Bioactive alkaloids from Illigera luzonensis. Journal of natural products. 1997 Jun;60(6):645-7.

[10]. Le PM, et al. Stephanine from Stephania venosa (Blume) Spreng Showed Effective Antiplasmodial and Anticancer Activities, the Latter by Inducing Apoptosis through the Reverse of Mitotic Exit. Phytotherapy research : PTR. 2017 Sep;31(9):1357-1368. [Content Brief]

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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.

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O-Methylbulbocapnine

All p38 MAPK Isoforms

All ERK Isoforms

All NF-κB Isoforms

All Akt Isoforms

All Interleukin Related Isoforms

All TNF Receptor Isoforms

All COX Isoforms

All NO Synthase Isoforms