Cat. No.: HY-N4225

Aaptamine

2 Cited Publications

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Based on 2 publication(s) in Google Scholar

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.

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

Purity: 99.71%
CAS No.: 85547-22-4
Formula: C₁₃H₁₂N₂O₂
Molecular Weight:228.25

Storage:

4°C, protect from light

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

Aaptamine Chemical Structure

CAS No.: 85547-22-4

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Fluorescent Dye

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

Biological Activity
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Publications (2)
Solvent & Solubility
- In Vitro
Purity & Documentation
References
Help & FAQs
Classifications
Bioz

Biological Activity

Description

IC₅₀ & Target^[5]

AChE

0.23 μg/mL (IC₅₀)

BChE

1.38 μg/mL (IC₅₀)

All Adrenergic Receptor Isoforms :

All Cholinesterase (ChE) Isoforms :

AChE
BChE

All AP-1 Isoforms :

All NF-κB Isoforms :

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]
A498	ED₅₀	3.2 μg/mL Compound: 3	Antineoplastic activity against human A498 cells Antineoplastic activity against human A498 cells	[PMID: 15043446]
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]
KM-20L2	ED₅₀	3.6 μg/mL Compound: 3	Antineoplastic activity against human KM20L2 cells Antineoplastic activity against human KM20L2 cells	[PMID: 15043446]
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]
NCI-H460	ED₅₀	3.2 μg/mL Compound: 3	Antineoplastic activity against human NCI-H460 cells Antineoplastic activity against human NCI-H460 cells	[PMID: 15043446]
OVCAR-3	ED₅₀	4.9 μg/mL Compound: 3	Antineoplastic activity against human OVCAR-3 cells Antineoplastic activity against human OVCAR-3 cells	[PMID: 15043446]
P388	ED₅₀	3.6 μg/mL Compound: 3	Antineoplastic activity against mouse P388 cells Antineoplastic activity against mouse P388 cells	[PMID: 15043446]
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]
SF-295	ED₅₀	4.1 μg/mL Compound: 3	Antineoplastic activity against human SF295 cells Antineoplastic activity against human SF295 cells	[PMID: 15043446]
SK-MEL-5	ED₅₀	4.3 μg/mL Compound: 3	Antineoplastic activity against human SK-MEL-5 cells Antineoplastic activity against human SK-MEL-5 cells	[PMID: 15043446]

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.

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.

Chemical Information

CAS No. 85547-22-4
Appearance Solid
Molecular Weight 228.25
Formula C₁₃H₁₂N₂O₂
Color White to yellow
SMILES

COC1=C2C3=C(N=CC=C3C=C1OC)C=CN2
Structure Classification
- Alkaloids
- Quinoline Alkaloids
Initial Source
- Marine natural products
- Sponge
- Animals
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)

Publications (2)

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Journal Impact Factor

J Exp Pharmacol

Aaptamine Alters Vimentin Expression and Migration Capability of Triple-Negative Breast Cancer Cells. [Abstract]

2025 May 22:17:239-247. PMID: 40420842
Res Sq

2024 Jul 29.

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)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

4.3812 mL

21.9058 mL

43.8116 mL

5 mM

0.8762 mL

4.3812 mL

8.7623 mL

10 mM

0.4381 mL

2.1906 mL

4.3812 mL

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.

Molarity Calculator

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Dilution Calculator

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Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (283 KB)
SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 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]. Ohizumi Y, et al. Alpha-adrenoceptor blocking action of aaptamine, a novel marine natural product, in vascular smooth muscle. J Pharm Pharmacol. 1984 Nov;36(11):785-6. [Content Brief]

[2]. Aoki S, et al. Aaptamine, a spongean alkaloid, activates p21 promoter in a p53-independent manner. Biochem Biophys Res Commun. 2006 Mar 31;342(1):101-6. [Content Brief]

[3]. Tsukamoto S, et al. Aaptamine, an alkaloid from the sponge Aaptos suberitoides, functions as a proteasome inhibitor. Bioorg Med Chem Lett. 2010 Jun 1;20(11):3341-3. [Content Brief]

[4]. Dyshlovoy SA, et al. Aaptamines from the marine sponge Aaptos sp. display anticancer activities in human cancer cell lines and modulate AP-1-, NF-κB-, and p53-dependent transcriptional activity in mouse JB6 Cl41 cells. Biomed Res Int. 2014;2014:469309. [Content Brief]

[5]. Suciati S, et al. In vitro and in silico cholinesterase inhibitory activities of aaptamine and derivatives from Aaptos suberitoides. Journal of Pharmacy and Pharmacognosy Research, 2025, 13(3): 757-773.

[6]. Rajivgandhi G, et al. Marine sponge alkaloid aaptamine enhances the anti-bacterial and anti-cancer activity against ESBL producing Gram negative bacteria and HepG 2 human liver carcinoma cells. Biocatalysis and Agricultural Biotechnology, 2019, 17: 628-637.

[7]. Sung CS, et al. Antinociceptive Effects of Aaptamine, a Sponge Component, on Peripheral Neuropathy in Rats. Mar Drugs. 2023 Feb 4;21(2):113. [Content Brief]

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.

Complete Stock Solution Preparation Table

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

Publications Citing Use of MedChemExpress (MCE) Aaptamine

All Adrenergic Receptor Isoforms

All Cholinesterase (ChE) Isoforms

All AP-1 Isoforms

All NF-κB Isoforms

Biological Activity

Chemical Information

Publications (2)

Solvent & Solubility

Purity & Documentation

References

Help & FAQs

Complete Stock Solution Preparation Table

Aaptamine Related Classifications

HY-N4225 Related Classifications