2. GPCR/G Protein Neuronal Signaling Metabolic Enzyme/Protease Anti-infection Apoptosis Immunology/Inflammation NF-κB
  3. Adrenergic Receptor Proteasome Cholinesterase (ChE) Bacterial Apoptosis AP-1 NF-κB
  4. Aaptamine

Aaptamine is an alkaloid that can be isolated from the sponge Aaptos suberitoides. Aaptamine is a competitive antagonist of the α-adrenergic receptor, as well as an inhibitor of the proteasome and cholinesterase. Aaptamine is cytotoxic to tumor cells and can induce apoptosis, cell cycle arrest of tumor cells, and the expression of p21 through a p53-independent pathway. Aaptamine has multiple activities such as anti-tumor, antioxidant, antibacterial, and analgesic effects.

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Aaptamine Chemical Structure

Aaptamine Chemical Structure

CAS No. : 85547-22-4

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Based on 1 publication(s) in Google Scholar

Aaptamine Related Antibodies

Top Publications Citing Use of Products

1 Publications Citing Use of MCE Aaptamine

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α adrenergic receptor β adrenergic receptor

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AChE BChE

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c-Fos c-Jun

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NF-κB NF-κB1/p50 RelA/p65 RelB c-Rel

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

Aaptamine is an alkaloid that can be isolated from the sponge Aaptos suberitoides. Aaptamine is a competitive antagonist of the α-adrenergic receptor, as well as an inhibitor of the proteasome and cholinesterase. Aaptamine is cytotoxic to tumor cells and can induce apoptosis, cell cycle arrest of tumor cells, and the expression of p21 through a p53-independent pathway. Aaptamine has multiple activities such as anti-tumor, antioxidant, antibacterial, and analgesic effects[1][2][3][4][5][6][7].

IC50 & Target[5]

AChE

0.23 μg/mL (IC50)

BChE

1.38 μg/mL (IC50)

Cellular Effect
Cell Line Type Value Description References
786-0 EC50
> 100 μM
Compound: 1
Inhibition of HIF2alpha in human 786-0 cells expressing truncated HIF1alpha assessed as reduction in luciferase activity after 24 hrs by reporter gene assay
Inhibition of HIF2alpha in human 786-0 cells expressing truncated HIF1alpha assessed as reduction in luciferase activity after 24 hrs by reporter gene assay
[PMID: 22928967]
A549 IC50
2.8 μg/mL
Compound: 2
Cytotoxicity against human A549 cells after 6 days by MTT assay
Cytotoxicity against human A549 cells after 6 days by MTT assay
[PMID: 10514310]
HeLa IC50
15 μg/mL
Compound: 1
Cytotoxicity against human HeLa cells after 3 days by MTT assay
Cytotoxicity against human HeLa cells after 3 days by MTT assay
[PMID: 20451377]
HeLa IC50
19 μM
Compound: 1
Cytotoxicity against human HeLa cells assessed as reduction in cell viability after 48 hrs by CCK8 assay
Cytotoxicity against human HeLa cells assessed as reduction in cell viability after 48 hrs by CCK8 assay
[PMID: 33170001]
HL-60 IC50
> 55 μM
Compound: 7
Antioxidant activity against TPA-induced ROS production in human HL60 cells by 2',7'-dichlorodihydrofluorescein diacetate cellular-based assay
Antioxidant activity against TPA-induced ROS production in human HL60 cells by 2',7'-dichlorodihydrofluorescein diacetate cellular-based assay
[PMID: 12762791]
HT-29 IC50
6.9 μg/mL
Compound: 2
Cytotoxicity against human HT-29 cells after 6 days by MTT assay
Cytotoxicity against human HT-29 cells after 6 days by MTT assay
[PMID: 10514310]
L5178Y IC50
8.3 μM
Compound: 5
Cytotoxic activity against mouse L5178Y cells by MTT assay
Cytotoxic activity against mouse L5178Y cells by MTT assay
[PMID: 23282083]
MCF7 IC50
> 20 μM
Compound: 1
Cytotoxicity against human MCF7 cells assessed as reduction in cell viability after 48 hrs by CCK8 assay
Cytotoxicity against human MCF7 cells assessed as reduction in cell viability after 48 hrs by CCK8 assay
[PMID: 33170001]
NB-4 IC50
> 20 μM
Compound: 1
Cytotoxicity against human NB4 cells assessed as reduction in cell viability after 48 hrs by CCK8 assay
Cytotoxicity against human NB4 cells assessed as reduction in cell viability after 48 hrs by CCK8 assay
[PMID: 33170001]
P388 IC50
0.6 μg/mL
Compound: 2
Cytotoxicity against mouse P388 cells after 3 days by MTT assay
Cytotoxicity against mouse P388 cells after 3 days by MTT assay
[PMID: 10514310]
In Vitro

Aaptamine (10 μM) can shift the dose-response curve of norepinephrine to the right in a parallel manner in isolated rabbit aorta and renal artery, without affecting the curves of histamine or potassium chloride[1].
Aaptamine (30 μg/mL; 0-48 h) can increase the expression of p21 and induce cell cycle arrest in MG63 cells[2].
Aaptamine (3 days) is cytotoxic to HeLa cells, with an IC50 of 15 μg/mL[3].
Aaptamine (50-100 μM; 6-24 h) can activate AP-1- and NF-κB-dependent transcriptional activity in JB6 Cl41 cells[4].
Aaptamine (5-55 µg/mL; 24 h) has an inhibitory effect on ESBL-producing Gram-negative uropathogenic bacteria[6].

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

Aaptamine Related Antibodies

Western Blot Analysis[2]

Cell Line: MG63 cells
Concentration: 30 μg/mL
Incubation Time: 0, 3, 6, 12, 24 and 48 h
Result: Increased the level of p21.
In Vivo

Aaptamine (5-100 μg; intrathecal injection; single dose) has an analgesic effect in a rat model of chronic constriction injury (CCI)-induced peripheral neuropathy[7].

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

Animal Model: Chronic constriction injury treated adult male Wistar rats (250-285 g)[7]
Dosage: 5, 30 and 100 μg
Administration: Intrathecal injection; single dose
Result: Showed different durations of analgesic effects on CCI-induced nociception. The 5 μg, 30 μg, and 100 μg doses presented analgesic durations of 90, 150, and 150 minutes respectively. However, the variance in the group administered with 100 μg of aaptamine was the largest, and the rats presented some abnormal motor behavior.
Molecular Weight

228.25

Formula

C13H12N2O2
CAS No.
Appearance

Solid

Color

White to yellow

SMILES

COC1=C2C3=C(N=CC=C3C=C1OC)C=CN2
Structure Classification
Initial Source

sponge
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (438.12 mM; Need ultrasonic; 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 4.3812 mL 21.9058 mL 43.8116 mL
5 mM 0.8762 mL 4.3812 mL 8.7623 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 (protect from light). 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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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

Purity: 99.71%

SDS (252 KB)

COA (254 KB) HNMR (203 KB) LCMS (92 KB)

Handling Instructions (2659 KB)
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 (protect from light). 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 4.3812 mL 21.9058 mL 43.8116 mL 109.5290 mL
5 mM 0.8762 mL 4.3812 mL 8.7623 mL 21.9058 mL
10 mM 0.4381 mL 2.1906 mL 4.3812 mL 10.9529 mL
15 mM 0.2921 mL 1.4604 mL 2.9208 mL 7.3019 mL
20 mM 0.2191 mL 1.0953 mL 2.1906 mL 5.4765 mL
25 mM 0.1752 mL 0.8762 mL 1.7525 mL 4.3812 mL
30 mM 0.1460 mL 0.7302 mL 1.4604 mL 3.6510 mL
40 mM 0.1095 mL 0.5476 mL 1.0953 mL 2.7382 mL
50 mM 0.0876 mL 0.4381 mL 0.8762 mL 2.1906 mL
60 mM 0.0730 mL 0.3651 mL 0.7302 mL 1.8255 mL
80 mM 0.0548 mL 0.2738 mL 0.5476 mL 1.3691 mL
100 mM 0.0438 mL 0.2191 mL 0.4381 mL 1.0953 mL
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Aaptamine 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:

Aaptamine85547-22-4Adrenergic ReceptorProteasomeCholinesterase (ChE)BacterialApoptosisAP-1NF-κBBeta ReceptorActivator Protein 1Nuclear factor-κBNuclear factor-kappaBperipheral neuropathy modelMG63 cellsHeLa cellsJB6 Cl41 cellsGram-negative uropathogenic bacteriaInhibitorinhibitorinhibit

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