1. Apoptosis
  2. Apoptosis
  3. Agelastatin A

Agelastatin A ((-)-Agelastatin A; AglA), a tetracyclic alkaloid isolated from the sponge Agelas dendromorpha, induces apoptosis and arrests cells in the G2/M phase of the cell cycle, exhibiting antitumor activity.

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Agelastatin A

Agelastatin A Chemical Structure

CAS No. : 152406-28-5

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Based on 1 publication(s) in Google Scholar

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Description

Agelastatin A ((-)-Agelastatin A; AglA), a tetracyclic alkaloid isolated from the sponge Agelas dendromorpha, induces apoptosis and arrests cells in the G2/M phase of the cell cycle, exhibiting antitumor activity[1].

Cellular Effect
Cell Line Type Value Description References
A-431 IC50
0.46 μM
Compound: 1; AglA
Cytotoxicity against human A431 cells after 48 hrs by crystal violet staining based assay
Cytotoxicity against human A431 cells after 48 hrs by crystal violet staining based assay
[PMID: 26951751]
BXPC-3 GI50
0.089 μg/mL
Compound: 82
Growth inhibition of human BXPC-3 cells assessed as reduction in cell viability measured after 3 days by CCK-8 assay
Growth inhibition of human BXPC-3 cells assessed as reduction in cell viability measured after 3 days by CCK-8 assay
[PMID: 38181652]
DU-145 GI50
0.056 μg/mL
Compound: 82
Growth inhibition of human DU-145 cells
Growth inhibition of human DU-145 cells
[PMID: 38181652]
DU-145 IC50
2.3 μM
Compound: 1, AA, (-)-Agelastatin A
Cytotoxicity against human DU145 cells assessed as inhibition of cell proliferation after 24 hrs by MTT assay
Cytotoxicity against human DU145 cells assessed as inhibition of cell proliferation after 24 hrs by MTT assay
10.1039/C3MD00094J
FaDu GI50
0.24 μg/mL
Compound: 82
Growth inhibition of human FaDu cells
Growth inhibition of human FaDu cells
[PMID: 38181652]
HeLa EC50
0.11 μM
Compound: 1a
Antitumor activity against human HeLa cells assessed as cell viability by MTT assay
Antitumor activity against human HeLa cells assessed as cell viability by MTT assay
[PMID: 24673739]
HeLa IC50
0.084 μM
Compound: 1; AglA
Cytotoxicity against human HeLa cells after 24 hrs by [3H]-thymidine incorporation assay
Cytotoxicity against human HeLa cells after 24 hrs by [3H]-thymidine incorporation assay
[PMID: 26951751]
JVM-2 EC50
0.28 μM
Compound: 1a
Antitumor activity against human JVM2 cells assessed as cell viability after 48 hrs by FACS analysis
Antitumor activity against human JVM2 cells assessed as cell viability after 48 hrs by FACS analysis
[PMID: 24673739]
KB IC50
0.5 μg/mL
Compound: 1a
Cytotoxicity against human KB cells
Cytotoxicity against human KB cells
[PMID: 24673739]
KM-20L2 GI50
0.036 μg/mL
Compound: 82
Growth inhibition of human KM-20L2 cells
Growth inhibition of human KM-20L2 cells
[PMID: 38181652]
MCF7 GI50
0.033 μg/mL
Compound: 82
Growth inhibition of human MCF7 cells
Growth inhibition of human MCF7 cells
[PMID: 38181652]
NCI-H460 GI50
0.036 μg/mL
Compound: 82
Growth inhibition of human NCI-H460 cells
Growth inhibition of human NCI-H460 cells
[PMID: 38181652]
P388 ED50
0.052 μg/mL
Compound: 82
Anticancer activity against mouse P388 cells assessed as inhibition of cell growth
Anticancer activity against mouse P388 cells assessed as inhibition of cell growth
[PMID: 38181652]
Raji IC50
0.14 μM
Compound: 1, AA, (-)-Agelastatin A
Cytotoxicity against human Raji cells assessed as inhibition of cell proliferation after 3 days by coulter counter analysis
Cytotoxicity against human Raji cells assessed as inhibition of cell proliferation after 3 days by coulter counter analysis
10.1039/C3MD00094J
SF-268 GI50
0.038 μg/mL
Compound: 82
Growth inhibition of human SF-268 cells
Growth inhibition of human SF-268 cells
[PMID: 38181652]
SJSA-1 IC50
0.44 μM
Compound: 1; AglA
Cytotoxicity against human SJSA1 cells after 48 hrs by crystal violet staining based assay
Cytotoxicity against human SJSA1 cells after 48 hrs by crystal violet staining based assay
[PMID: 26951751]
SK-N-SH GI50
0.042 μg/mL
Compound: 82
Growth inhibition of human SK-N-SH cells
Growth inhibition of human SK-N-SH cells
[PMID: 38181652]
SW-1736 GI50
0.12 μg/mL
Compound: 82
Growth inhibition of human SW-1736 cells
Growth inhibition of human SW-1736 cells
[PMID: 38181652]
In Vitro

Agelastatin A(0-2 μM, 48 h) has IC50 values of 67 nM, 708 nM, 1.05 μM, 278 nM and 1.11 μM on U-937, HeLa, A549, BT549 and IMR90 cells, respectively[1].
Agelastatin A(0-1 μM, 48 h) has IC50 values of 20, 74, 20, 138 and 187 nM on CEM, Jurkat, Daudi, HL-60 and CA46 cells, respectively[1].
Agelastatin A (0-150 nM, 16 h) can dose-dependently induce U-937 cell cycle arrest at G2/M[1].

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

In Vivo

The pharmacokinetic parameters of Agelastatin A(1a) a single 2.5 mg/kg dose in mice[2].

Parameter/td> intravenous (IV) intraperitoneal (IP)
ACU 1742 2946
Cmax 4.5 μM 1.65 μM
Tmax 2 min 30 min
t1/2 4 min 1 h

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

Molecular Weight

341.16

Formula

C12H13BrN4O3

CAS No.
SMILES

BrC(N1[C@@]2([H])[C@](N3)([H])[C@@]4([H])[C@@](C2)(N(C(N4)=O)C)O)=CC=C1C3=O

Structure Classification
Initial Source

A. dendromorpha

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
References
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Help & FAQs
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    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.

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Agelastatin A
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HY-125132
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