Page last updated: 2024-12-11

bastadin 5

Description Research Excerpts Clinical Trials Roles Classes Pathways Study Profile Bioassays Related Drugs Related Conditions Protein Interactions Research Growth Market Indicators

Cross-References

ID SourceID
PubMed CID9577239
MeSH IDM0274496

Synonyms (3)

Synonym
79067-75-7
5,16,21,32,36-pentabromo-4,20-dihydroxy-2,18-dioxa-10,27-diazapentacyclo(28.2.2.2(14,17).1(3,7).1(19,23))octatriaconta-3,5,7(38),14,16,19,21,23(35),30,32,33,36-dodecaene-11,12,25,26-tetrone 12,25-dioxime
(12z,25z)-5,16,21,32,36-pentabromo-4,20-dihydroxy-12,25-bis(hydroxyimino)-2,18-dioxa-10,27-diazapentacyclo[28.2.2.214,17.13,7.119,23]octatriaconta-1(32),3,5,7(38),14,16,19,21,23(35),30,33,36-dodecaene-11,26-dione
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Protein Targets (6)

Activation Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Neuronal acetylcholine receptor subunit alpha-4Rattus norvegicus (Norway rat)EC50 (µMol)2.20000.01402.272410.0000AID349210
Ryanodine receptor 1Oryctolagus cuniculus (rabbit)EC50 (µMol)2.00002.00002.00002.0000AID355165
Neuronal acetylcholine receptor subunit beta-2Rattus norvegicus (Norway rat)EC50 (µMol)2.20000.01402.310410.0000AID349210
Androgen receptorRattus norvegicus (Norway rat)EC50 (µMol)2.00000.00100.50292.0000AID355165
Ryanodine receptor 1Homo sapiens (human)EC50 (µMol)2.20002.20002.20002.2000AID266719; AID349210
Peptidyl-prolyl cis-trans isomerase FKBP1AHomo sapiens (human)EC50 (µMol)2.20000.00090.44812.2000AID266719
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Other Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Ryanodine receptor 1Homo sapiens (human)ED502.30002.30002.30002.3000AID334201
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (37)

Processvia Protein(s)Taxonomy
response to hypoxiaRyanodine receptor 1Homo sapiens (human)
outflow tract morphogenesisRyanodine receptor 1Homo sapiens (human)
calcium ion transportRyanodine receptor 1Homo sapiens (human)
muscle contractionRyanodine receptor 1Homo sapiens (human)
release of sequestered calcium ion into cytosol by sarcoplasmic reticulumRyanodine receptor 1Homo sapiens (human)
calcium-mediated signalingRyanodine receptor 1Homo sapiens (human)
response to caffeineRyanodine receptor 1Homo sapiens (human)
skin developmentRyanodine receptor 1Homo sapiens (human)
ossification involved in bone maturationRyanodine receptor 1Homo sapiens (human)
skeletal muscle fiber developmentRyanodine receptor 1Homo sapiens (human)
release of sequestered calcium ion into cytosolRyanodine receptor 1Homo sapiens (human)
protein homotetramerizationRyanodine receptor 1Homo sapiens (human)
regulation of cytosolic calcium ion concentrationRyanodine receptor 1Homo sapiens (human)
cellular response to calcium ionRyanodine receptor 1Homo sapiens (human)
cellular response to caffeineRyanodine receptor 1Homo sapiens (human)
striated muscle contractionRyanodine receptor 1Homo sapiens (human)
protein peptidyl-prolyl isomerizationPeptidyl-prolyl cis-trans isomerase FKBP1AHomo sapiens (human)
heart morphogenesisPeptidyl-prolyl cis-trans isomerase FKBP1AHomo sapiens (human)
protein foldingPeptidyl-prolyl cis-trans isomerase FKBP1AHomo sapiens (human)
'de novo' protein foldingPeptidyl-prolyl cis-trans isomerase FKBP1AHomo sapiens (human)
regulation of skeletal muscle contraction by regulation of release of sequestered calcium ionPeptidyl-prolyl cis-trans isomerase FKBP1AHomo sapiens (human)
protein maturation by protein foldingPeptidyl-prolyl cis-trans isomerase FKBP1AHomo sapiens (human)
negative regulation of transforming growth factor beta receptor signaling pathwayPeptidyl-prolyl cis-trans isomerase FKBP1AHomo sapiens (human)
positive regulation of protein bindingPeptidyl-prolyl cis-trans isomerase FKBP1AHomo sapiens (human)
regulation of protein localizationPeptidyl-prolyl cis-trans isomerase FKBP1AHomo sapiens (human)
negative regulation of activin receptor signaling pathwayPeptidyl-prolyl cis-trans isomerase FKBP1AHomo sapiens (human)
protein refoldingPeptidyl-prolyl cis-trans isomerase FKBP1AHomo sapiens (human)
T cell activationPeptidyl-prolyl cis-trans isomerase FKBP1AHomo sapiens (human)
positive regulation of canonical NF-kappaB signal transductionPeptidyl-prolyl cis-trans isomerase FKBP1AHomo sapiens (human)
regulation of immune responsePeptidyl-prolyl cis-trans isomerase FKBP1AHomo sapiens (human)
ventricular cardiac muscle tissue morphogenesisPeptidyl-prolyl cis-trans isomerase FKBP1AHomo sapiens (human)
regulation of ryanodine-sensitive calcium-release channel activityPeptidyl-prolyl cis-trans isomerase FKBP1AHomo sapiens (human)
heart trabecula formationPeptidyl-prolyl cis-trans isomerase FKBP1AHomo sapiens (human)
calcium ion transmembrane transportPeptidyl-prolyl cis-trans isomerase FKBP1AHomo sapiens (human)
supramolecular fiber organizationPeptidyl-prolyl cis-trans isomerase FKBP1AHomo sapiens (human)
regulation of amyloid precursor protein catabolic processPeptidyl-prolyl cis-trans isomerase FKBP1AHomo sapiens (human)
amyloid fibril formationPeptidyl-prolyl cis-trans isomerase FKBP1AHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (19)

Processvia Protein(s)Taxonomy
ryanodine-sensitive calcium-release channel activityRyanodine receptor 1Homo sapiens (human)
voltage-gated calcium channel activityRyanodine receptor 1Homo sapiens (human)
calcium channel activityRyanodine receptor 1Homo sapiens (human)
calcium ion bindingRyanodine receptor 1Homo sapiens (human)
calmodulin bindingRyanodine receptor 1Homo sapiens (human)
ATP bindingRyanodine receptor 1Homo sapiens (human)
intracellularly gated calcium channel activityRyanodine receptor 1Homo sapiens (human)
calcium-induced calcium release activityRyanodine receptor 1Homo sapiens (human)
peptidyl-prolyl cis-trans isomerase activityPeptidyl-prolyl cis-trans isomerase FKBP1AHomo sapiens (human)
transforming growth factor beta receptor bindingPeptidyl-prolyl cis-trans isomerase FKBP1AHomo sapiens (human)
protein bindingPeptidyl-prolyl cis-trans isomerase FKBP1AHomo sapiens (human)
macrolide bindingPeptidyl-prolyl cis-trans isomerase FKBP1AHomo sapiens (human)
FK506 bindingPeptidyl-prolyl cis-trans isomerase FKBP1AHomo sapiens (human)
channel regulator activityPeptidyl-prolyl cis-trans isomerase FKBP1AHomo sapiens (human)
signaling receptor inhibitor activityPeptidyl-prolyl cis-trans isomerase FKBP1AHomo sapiens (human)
type I transforming growth factor beta receptor bindingPeptidyl-prolyl cis-trans isomerase FKBP1AHomo sapiens (human)
transmembrane transporter bindingPeptidyl-prolyl cis-trans isomerase FKBP1AHomo sapiens (human)
I-SMAD bindingPeptidyl-prolyl cis-trans isomerase FKBP1AHomo sapiens (human)
activin receptor bindingPeptidyl-prolyl cis-trans isomerase FKBP1AHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (18)

Processvia Protein(s)Taxonomy
cytoplasmRyanodine receptor 1Homo sapiens (human)
plasma membraneRyanodine receptor 1Homo sapiens (human)
cell cortexRyanodine receptor 1Homo sapiens (human)
junctional sarcoplasmic reticulum membraneRyanodine receptor 1Homo sapiens (human)
terminal cisternaRyanodine receptor 1Homo sapiens (human)
sarcoplasmic reticulumRyanodine receptor 1Homo sapiens (human)
organelle membraneRyanodine receptor 1Homo sapiens (human)
I bandRyanodine receptor 1Homo sapiens (human)
sarcoplasmic reticulum membraneRyanodine receptor 1Homo sapiens (human)
extracellular exosomeRyanodine receptor 1Homo sapiens (human)
ryanodine receptor complexRyanodine receptor 1Homo sapiens (human)
Z discRyanodine receptor 1Homo sapiens (human)
sarcolemmaRyanodine receptor 1Homo sapiens (human)
smooth endoplasmic reticulumRyanodine receptor 1Homo sapiens (human)
sarcoplasmic reticulum membraneRyanodine receptor 1Homo sapiens (human)
calcium channel complexRyanodine receptor 1Homo sapiens (human)
cytoplasmPeptidyl-prolyl cis-trans isomerase FKBP1AHomo sapiens (human)
cytosolPeptidyl-prolyl cis-trans isomerase FKBP1AHomo sapiens (human)
terminal cisternaPeptidyl-prolyl cis-trans isomerase FKBP1AHomo sapiens (human)
membranePeptidyl-prolyl cis-trans isomerase FKBP1AHomo sapiens (human)
sarcoplasmic reticulumPeptidyl-prolyl cis-trans isomerase FKBP1AHomo sapiens (human)
Z discPeptidyl-prolyl cis-trans isomerase FKBP1AHomo sapiens (human)
cytoplasmic side of membranePeptidyl-prolyl cis-trans isomerase FKBP1AHomo sapiens (human)
ryanodine receptor complexPeptidyl-prolyl cis-trans isomerase FKBP1AHomo sapiens (human)
sarcoplasmic reticulum membranePeptidyl-prolyl cis-trans isomerase FKBP1AHomo sapiens (human)
cytoplasmPeptidyl-prolyl cis-trans isomerase FKBP1AHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (17)

Assay IDTitleYearJournalArticle
AID354813Antimicrobial activity against Enterococcus faecalis ATCC 29212 after 16 hrs by disk susceptibility test1996Journal of natural products, Oct, Volume: 59, Issue:10
Isolation and structure of hemibastadinols 1-3 from the Papua New Guinea marine sponge Ianthella basta.
AID354814Antimicrobial activity against Staphylococcus aureus ATCC 29213 after 16 hrs by disk susceptibility test1996Journal of natural products, Oct, Volume: 59, Issue:10
Isolation and structure of hemibastadinols 1-3 from the Papua New Guinea marine sponge Ianthella basta.
AID349212Activity at RYR2 receptor in rat cerebellar granule neurons assessed activation of [45Ca2+] uptake at 20 uM after 10 mins2008Bioorganic & medicinal chemistry letters, Nov-01, Volume: 18, Issue:21
Open-chain half-bastadins mimic the effects of cyclic bastadins on calcium homeostasis in cultured neurons.
AID266719Agonist like activity at skeletal junction sarcoplasmic reticulum RyR1/FKBP12 complex assessed as increase in [3H]ryanodine binding2006Journal of medicinal chemistry, Jul-27, Volume: 49, Issue:15
Simplified cyclic analogues of bastadin-5. Structure-activity relationships for modulation of the RyR1/FKBP12 Ca2+ channel complex.
AID349211Activity at RYR2 receptor in rat cerebellar granule neurons assessed as increase in intracellular calcium level at 20 uM2008Bioorganic & medicinal chemistry letters, Nov-01, Volume: 18, Issue:21
Open-chain half-bastadins mimic the effects of cyclic bastadins on calcium homeostasis in cultured neurons.
AID334201Displacement of [3H]ryanodine from RyR1 calcium channel in sarcoplasmic reticulum assessed as calcium mobilization2003Journal of natural products, Jan, Volume: 66, Issue:1
Cationic reduction of bastadin-4 to bastadin-5. Preparation of 5-[2h]-bastadin-5 by site-specific isotopic labeling.
AID1255367Cytotoxicity against human MDM cells at 5 uM after 24 hrs2015Bioorganic & medicinal chemistry letters, Nov-15, Volume: 25, Issue:22
Bastadins, brominated-tyrosine derivatives, suppress accumulation of cholesterol ester in macrophages.
AID1255366Inhibition of ACAT in human MDM cells assessed as inhibition of foam cell formation by measuring acetylated LDL-induced [3H]cholesterol ester accumulation at 5 uM after 24 hrs in presence of 0.1 mM [3H]oleate2015Bioorganic & medicinal chemistry letters, Nov-15, Volume: 25, Issue:22
Bastadins, brominated-tyrosine derivatives, suppress accumulation of cholesterol ester in macrophages.
AID354812Antimicrobial activity against Neisseria gonorrhoeae ATCC 49226 after 16 hrs by disk susceptibility test1996Journal of natural products, Oct, Volume: 59, Issue:10
Isolation and structure of hemibastadinols 1-3 from the Papua New Guinea marine sponge Ianthella basta.
AID1255369Inhibition of human ACAT2 expressed in CHO cells assessed as inhibition of [3H]cholesterol ester accumulation at 5 uM in presence of 0.1 mM [3H]oleate-conjugated BSA2015Bioorganic & medicinal chemistry letters, Nov-15, Volume: 25, Issue:22
Bastadins, brominated-tyrosine derivatives, suppress accumulation of cholesterol ester in macrophages.
AID349210Binding affinity to RYR1 channels by calcium mobilization assay2008Bioorganic & medicinal chemistry letters, Nov-01, Volume: 18, Issue:21
Open-chain half-bastadins mimic the effects of cyclic bastadins on calcium homeostasis in cultured neurons.
AID463756Antitrypanosomal activity against Trypanosoma brucei brucei 221 after 48 hrs by ATP-bioluminescence assay2010Journal of natural products, Mar-26, Volume: 73, Issue:3
Additional insights on the bastadins: isolation of analogues from the sponge Ianthella cf. reticulata and exploration of the oxime configurations.
AID463757Cytotoxicity against human HCT116 cells after 7 days by methylene blue staining2010Journal of natural products, Mar-26, Volume: 73, Issue:3
Additional insights on the bastadins: isolation of analogues from the sponge Ianthella cf. reticulata and exploration of the oxime configurations.
AID354816Antimicrobial activity against Cryptococcus neoformans ATCC 90112 up to 100 ug/disk after 42 hrs by disk susceptibility test1996Journal of natural products, Oct, Volume: 59, Issue:10
Isolation and structure of hemibastadinols 1-3 from the Papua New Guinea marine sponge Ianthella basta.
AID355165Displacement of [3H]ryanodine from Ry1R/FKBP12 receptor complex in rabbit sarcoplasmic reticulum1996Journal of natural products, Dec, Volume: 59, Issue:12
Bastadin 20 and bastadin O-sulfate esters from Ianthella basta: novel modulators of the Ry1R FKBP12 receptor complex.
AID1255368Inhibition of human ACAT1 expressed in CHO cells assessed as inhibition of [3H]cholesterol ester accumulation at 5 uM in presence of 0.1 mM [3H]oleate-conjugated BSA2015Bioorganic & medicinal chemistry letters, Nov-15, Volume: 25, Issue:22
Bastadins, brominated-tyrosine derivatives, suppress accumulation of cholesterol ester in macrophages.
AID354815Antimicrobial activity against Candida albicans ATCC 90028 up to 100 ug/disk after 42 hrs by disk susceptibility test1996Journal of natural products, Oct, Volume: 59, Issue:10
Isolation and structure of hemibastadinols 1-3 from the Papua New Guinea marine sponge Ianthella basta.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (7)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's2 (28.57)18.2507
2000's3 (42.86)29.6817
2010's2 (28.57)24.3611
2020's0 (0.00)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 12.41

According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be weak demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index12.41 (24.57)
Research Supply Index2.08 (2.92)
Research Growth Index4.49 (4.65)
Search Engine Demand Index0.00 (26.88)
Search Engine Supply Index0.00 (0.95)

This Compound (12.41)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials0 (0.00%)5.53%
Reviews0 (0.00%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other7 (100.00%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]