2. Cell Cycle/DNA Damage Epigenetics Anti-infection Metabolic Enzyme/Protease Vitamin D Related/Nuclear Receptor Apoptosis
  3. HDAC DNA Methyltransferase DNA/RNA Synthesis Bacterial Aminopeptidase Farnesyl Transferase PPAR Apoptosis
  4. Psammaplin A

Psammaplin A is a marine metabolite. Psammaplin A is a selective HDAC1 (IC50: 45 nM), DNA methyltransferases (IC50: 18.6 nM) and aminopeptidase N (APN) (IC50: 18 μM) inhibitor. Psammaplin A also inhibits DNA topoisomerase and farnesyl protein transferase. Psammaplin A is a PPARγ activator and induces apoptosis. Psammaplin A has antitumor and anti-inflammatory activities. Psammaplin A has antibacterial activity against Gram-positive bacteria and inhibits DNA synthesis and DNA gyrase activity. Psammaplin A inhibits angiogenesis.

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Psammaplin A Chemical Structure

Psammaplin A Chemical Structure

CAS No. : 110659-91-1

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Based on 1 publication(s) in Google Scholar

Psammaplin A Related Antibodies

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PPARα PPARβ/δ PPARγ PPAR PPARδ

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Description

Psammaplin A is a marine metabolite. Psammaplin A is a selective HDAC1 (IC50: 45 nM), DNA methyltransferases (IC50: 18.6 nM) and aminopeptidase N (APN) (IC50: 18 μM) inhibitor. Psammaplin A also inhibits DNA topoisomerase and farnesyl protein transferase. Psammaplin A is a PPARγ activator and induces apoptosis. Psammaplin A has antitumor and anti-inflammatory activities. Psammaplin A has antibacterial activity against Gram-positive bacteria and inhibits DNA synthesis and DNA gyrase activity. Psammaplin A inhibits angiogenesis[1][2][3][4][5][6][7][8].

IC50 & Target[1][3][5][8]

HDAC1

45 nM (IC50)

DNA Methyltransferase

18.6 nM (IC50)

PPARγ

 

APN

18 μM (IC50)

Cellular Effect
Cell Line Type Value Description References
A549 IC50
1.18 μM
Compound: 1, PsA
Cytotoxicity against human A549 cells by SRB assay
Cytotoxicity against human A549 cells by SRB assay
[PMID: 25884112]
A549 IC50
1.76 μM
Compound: PsA
Cytotoxicity against human A549 cells assessed as reduction in cell viability by SRB assay
Cytotoxicity against human A549 cells assessed as reduction in cell viability by SRB assay
[PMID: 33636429]
A549 GI50
4.5 μM
Compound: Psammaplin A
Cytotoxicity against human A549 cells assessed as reduction in cell growth inhibition after 96 hrs by MTT assay
Cytotoxicity against human A549 cells assessed as reduction in cell growth inhibition after 96 hrs by MTT assay
[PMID: 27460171]
A549 GI50
7.5 μM
Compound: 11c
Growth inhibition of human A549 cells after 96 hrs by sulphorhodamine B assay
Growth inhibition of human A549 cells after 96 hrs by sulphorhodamine B assay
[PMID: 22280363]
CHO-K1 EC50
0.9 μM
Compound: 4
Cytotoxicity against CHO-K1 cells by Alamar blue assay
Cytotoxicity against CHO-K1 cells by Alamar blue assay
[PMID: 16962325]
HCT-116 IC50
0.61 μM
Compound: PsA
Cytotoxicity against human HCT-116 cells assessed as reduction in cell viability by SRB assay
Cytotoxicity against human HCT-116 cells assessed as reduction in cell viability by SRB assay
[PMID: 33636429]
HCT-116 IC50
1.62 μM
Compound: 1, PsA
Cytotoxicity against human HCT116 cells by SRB assay
Cytotoxicity against human HCT116 cells by SRB assay
[PMID: 25884112]
HeLa IC50
0.05 μM
Compound: Psammaplin A
Inhibition of HDAC in human HeLa cells using Fluor deLys as substrate assessed as deacetylation of substrate by fluorescence assay
Inhibition of HDAC in human HeLa cells using Fluor deLys as substrate assessed as deacetylation of substrate by fluorescence assay
[PMID: 27460171]
HL-60 GI50
0.29 μM
Compound: Psammaplin A
Cytotoxicity against human HL60 cells assessed as reduction in cell growth inhibition after 72 hrs by trypan blue-staining based hemocytometric analysis
Cytotoxicity against human HL60 cells assessed as reduction in cell growth inhibition after 72 hrs by trypan blue-staining based hemocytometric analysis
[PMID: 27460171]
HL-60 GI50
0.37 μM
Compound: 1; PsA
Growth inhibition of human HL-60 cells after 72 hrs by trypan blue dye based assay
Growth inhibition of human HL-60 cells after 72 hrs by trypan blue dye based assay
[PMID: 33488962]
MCF7 GI50
1.27 μM
Compound: 11c
Growth inhibition of human MCF7 cells after 96 hrs by sulphorhodamine B assay
Growth inhibition of human MCF7 cells after 96 hrs by sulphorhodamine B assay
[PMID: 22280363]
MCF7 GI50
2.26 μM
Compound: Psammaplin A
Cytotoxicity against human MCF7 cells assessed as reduction in cell growth inhibition after 96 hrs by MTT assay
Cytotoxicity against human MCF7 cells assessed as reduction in cell growth inhibition after 96 hrs by MTT assay
[PMID: 27460171]
MCF7 IC50
5 μM
Compound: 1
Antiproliferative activity against human MCF7 cells by neutral red method
Antiproliferative activity against human MCF7 cells by neutral red method
[PMID: 16643023]
MCF7 EC50
5.7 μM
Compound: 1
Activation of PPARgamma transfected in human MCF7 cells by luciferase reporter gene assay
Activation of PPARgamma transfected in human MCF7 cells by luciferase reporter gene assay
[PMID: 16643023]
MDA-MB-231 IC50
1.31 μM
Compound: PsA
Cytotoxicity against human MDA-MB-231 cells assessed as reduction in cell viability by SRB assay
Cytotoxicity against human MDA-MB-231 cells assessed as reduction in cell viability by SRB assay
[PMID: 33636429]
PC-3 GI50
3.52 μM
Compound: Psammaplin A
Cytotoxicity against human PC3 cells assessed as reduction in cell growth inhibition after 96 hrs by MTT assay
Cytotoxicity against human PC3 cells assessed as reduction in cell growth inhibition after 96 hrs by MTT assay
[PMID: 27460171]
SK-HEP1 IC50
1.29 μM
Compound: PsA
Cytotoxicity against human SK-HEP1 cells assessed as reduction in cell viability by SRB assay
Cytotoxicity against human SK-HEP1 cells assessed as reduction in cell viability by SRB assay
[PMID: 33636429]
SNU-638 IC50
0.56 μM
Compound: PsA
Cytotoxicity against human SNU-638 cells assessed as reduction in cell viability by SRB assay
Cytotoxicity against human SNU-638 cells assessed as reduction in cell viability by SRB assay
[PMID: 33636429]
T-cell EC50
0.2 μM
Compound: Psammaplin A
Reactivation of latent HIV1 NL4-3-Luc expression in human naive CD4+ T cells treated 7 days post-infection measured after 48 hrs by luminescence plate reader analysis
Reactivation of latent HIV1 NL4-3-Luc expression in human naive CD4+ T cells treated 7 days post-infection measured after 48 hrs by luminescence plate reader analysis
[PMID: 24495105]
WI-38 GI50
3.44 μM
Compound: 11c
Growth inhibition of human WI38 cells after 96 hrs by sulphorhodamine B assay
Growth inhibition of human WI38 cells after 96 hrs by sulphorhodamine B assay
[PMID: 22280363]
In Vitro

Psammaplin A inhibits the viability of A549 (GI50: 7.5 μM), MCF7 (GI50: 1.27 μM), and WI38 (GI50: 3.44 μM) cells[1].
Psammaplin A (72 h) inhibits the viability of A549 (IC50: 1.18 μM) and HCT116 (IC50: 1.62 μM) cells[2].
Psammaplin A (0.5-5 μM) inhibits bFGF-induced angiogenesis in bovine aortic endothelial cells (BAEC) in a dose-dependent manner[3].
Psammaplin A (0-100 μg/mL, 1-4 h) inhibits the toxicity of INT-407 cells induced by V. vulnificus in a concentration- and time-dependent manner[4].
Psammaplin A (0-100 μg/mL, 0-13 h) inhibits the growth of V. vulnificus in a concentration-dependent manner[4].
Psammaplin A (0-40 μM, 12 h) inhibits the viability of the macrophage cell line RAW264.7 in a concentration-dependent manner[6].
Psammaplin A (0-500 μM, 2 h) inhibits SV40 DNA replication in HeLa cells in a concentration-dependent manner. Psammaplin A (125-500 μM, 30 min) inhibits the catalytic activity of topoisomerase I[6].
Psammaplin A (125-500 μM, 15 min) inhibits the binding activity of RPA to single-stranded DNA[6].
Psammaplin A (1-40 μM, 30 min) inhibits the activity of polymerase α-primase in a concentration-dependent manner[6].
Psammaplin A (3-30 μM, 4-16 h) induces apoptosis in T47D and MCF-7 cells[8].

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

Psammaplin A Related Antibodies

Western Blot Analysis[1]

Cell Line: MCF7 cells
Concentration: 5 μM
Incubation Time: 24 h
Result: Up-regulated the expression of Ac-H3 protein.

Cell Cytotoxicity Assay[4]

Cell Line: INT-407 cells
Concentration: 0, 12.5, 25, 50, 100 μg/mL
Incubation Time: 1, 2, 3, 4 h
Result: Reduced cytotoxicity.
Reduced cell damage.

Cell Viability Assay[6]

Cell Line: Macrophage cell line RAW 264.7
Concentration: 0, 1, 5, 10, 20, 40 μM
Incubation Time: 12 h
Result: Reduced the number of viable cells.

Apoptosis Analysis[8]

Cell Line: MCF-7 and T47D cells
Concentration: 3, 10, 30 μM
Incubation Time: 4, 8, 16 h
Result: Increased cells apoptosis.
In Vivo

Psammaplin A (30 mg/kg, i.p., three times a week for 35 d) has antitumor activity in mice in the A549 xenograft model[2].
Psammaplin A (5-50 μg, i.p., once) improves the survival rate of mice in the V. vulnificus-infected model[4].

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

Animal Model: A549 cell-implanted xenograft model (male athymic BALB/c mice, 6 weeks old, 18-20 g)[2]
Dosage: 30 mg/kg
Administration: Intraperitoneal injection (i.p.), three times a week for 35 d
Result: Inhibited the tumor growth.
Inhibited the expression of the proliferation biomarker Ki-67 in both central and edge region of tumor tissues.
Animal Model: V. vulnificus-infected model (35 female ICR mice, 8 weeks old, 20-22 g)[4]
Dosage: 5, 10, 25 and 50 μg
Administration: Intraperitoneal injection (i.p.), once
Result: Prolonged survival time of mice.
Inhibited damage to the intestines, liver and spleen of mice.
Molecular Weight

664.39

Formula

C22H24Br2N4O6S2
CAS No.
Appearance

Solid

Color

Off-white to yellow

SMILES

O=C(NCCSSCCNC(/C(CC1=CC(Br)=C(O)C=C1)=N/O)=O)/C(CC2=CC(Br)=C(O)C=C2)=N/O
Structure Classification
Initial Source

marine sponge
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, stored under nitrogen

*In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)

Solvent & Solubility
In Vitro: 

DMSO : 33.3 mg/mL (50.12 mM; Need ultrasonic and warming; 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 1.5051 mL 7.5257 mL 15.0514 mL
5 mM 0.3010 mL 1.5051 mL 3.0103 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 (stored under nitrogen). 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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  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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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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Calculation results:
Working solution concentration: mg/mL
Purity & Documentation
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 (stored under nitrogen). 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 1.5051 mL 7.5257 mL 15.0514 mL 37.6285 mL
5 mM 0.3010 mL 1.5051 mL 3.0103 mL 7.5257 mL
10 mM 0.1505 mL 0.7526 mL 1.5051 mL 3.7629 mL
15 mM 0.1003 mL 0.5017 mL 1.0034 mL 2.5086 mL
20 mM 0.0753 mL 0.3763 mL 0.7526 mL 1.8814 mL
25 mM 0.0602 mL 0.3010 mL 0.6021 mL 1.5051 mL
30 mM 0.0502 mL 0.2509 mL 0.5017 mL 1.2543 mL
40 mM 0.0376 mL 0.1881 mL 0.3763 mL 0.9407 mL
50 mM 0.0301 mL 0.1505 mL 0.3010 mL 0.7526 mL
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Psammaplin A 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:

Psammaplin A110659-91-1HDACDNA MethyltransferaseDNA/RNA SynthesisBacterialAminopeptidaseFarnesyl TransferasePPARApoptosisHistone deacetylasesDNMTsDNA MTasesFtasePeroxisome proliferator-activated receptorsAnticancerAntibacterialA549MCF7WI38HCT116bFGFV. vulnificusRAW264.7HeLaA549 xenograft modelV. vulnificus-infected modelInhibitorinhibitorinhibit

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