Page last updated: 2024-12-11
variolin b
Description
Research Excerpts
Clinical Trials
Roles
Classes
Pathways
Study Profile
Bioassays
Related Drugs
Related Conditions
Protein Interactions
Research Growth
Market Indicators
Description
variolin B: from Antartic sponge, Kirkpatrickia variolosa; structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]
Cross-References
ID Source | ID |
---|---|
PubMed CID | 9817550 |
CHEMBL ID | 380500 |
SCHEMBL ID | 13175404 |
MeSH ID | M0450818 |
Synonyms (8)
Synonym |
---|
variolin b |
DB08694 |
CHEMBL380500 |
bdbm50398327 |
9-amino-5-(2-aminopyrimidin-4-yl)pyrido[3',2':4,5]pyrrolo[1,2-c]pyrimidin-4-ol |
SCHEMBL13175404 |
13-amino-8-(2-aminopyrimidin-4-yl)-1,3,12-triazatricyclo[7.4.0.02,7]trideca-2(7),4,8,10,12-pentaen-6-one |
Q27097881 |
Research Excerpts
Overview
Variolin B (VAR-B) is a natural product isolated from the sponge Kirkpatrickia variolosa, found in Antarctica. It showed promising anti-cancer activity soon after its isolation.
Excerpt | Reference | Relevance |
---|---|---|
"Variolin B is a rare marine alkaloid that showed promising anti-cancer activity soon after its isolation. " | ( Intercalative DNA binding of the marine anticancer drug variolin B. Albericio, F; Álvarez, M; Arribas-Bosacoma, R; Aymamí, J; Canals, A; Coll, M, 2017) | 2.14 |
"Variolin B (VAR-B) is a natural product isolated from the sponge Kirkpatrickia variolosa, found in Antarctica. " | ( Variolin B and its derivate deoxy-variolin B: new marine natural compounds with cyclin-dependent kinase inhibitor activity. Bailly, C; Cuevas, C; D'Incalci, M; Damia, G; Di Francesco, AM; Erba, E; Fernandez Sousa-Faro, JM; Riccardi, R; Simone, M; Vikhanskaya, F, 2005) | 3.21 |
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]
Protein Targets (1)
Activation Measurements
Protein | Taxonomy | Measurement | Average | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
---|---|---|---|---|---|---|---|
Endothelial PAS domain-containing protein 1 | Homo sapiens (human) | EC50 (µMol) | 0.7000 | 0.0200 | 0.9330 | 3.3000 | AID707849 |
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] |
Biological Processes (22)
Molecular Functions (9)
Ceullar Components (5)
Process | via Protein(s) | Taxonomy |
---|---|---|
nucleoplasm | Endothelial PAS domain-containing protein 1 | Homo sapiens (human) |
cytosol | Endothelial PAS domain-containing protein 1 | Homo sapiens (human) |
nuclear speck | Endothelial PAS domain-containing protein 1 | Homo sapiens (human) |
chromatin | Endothelial PAS domain-containing protein 1 | Homo sapiens (human) |
transcription regulator complex | Endothelial PAS domain-containing protein 1 | Homo sapiens (human) |
[Information is prepared from geneontology information from the June-17-2024 release] |
Bioassays (42)
Assay ID | Title | Year | Journal | Article |
---|---|---|---|---|
AID707624 | Inhibition of HIF2alpha in human RCC4 cells coexpressing HIF1alpha assessed as reduction in GLUT1 mRNA expression at 1 uM after 48 hrs by RT-PCR analysis | 2012 | Journal of natural products, Sep-28, Volume: 75, Issue:9 | Inhibition of hypoxia inducible factor-2 transcription: isolation of active modulators from marine sponges. |
AID260403 | Inhibition of growth against DU145 cells after 72 hrs exposure | 2006 | Journal of medicinal chemistry, Feb-09, Volume: 49, Issue:3 | Synthesis and cytotoxic evaluation of new derivatives of the marine alkaloid variolin B. |
AID707640 | Inhibition of HIF2alpha in human 786-0 cells assessed as reduction in TGFalpha mRNA expression at 1 uM after 48 hrs by RT-PCR analysis | 2012 | Journal of natural products, Sep-28, Volume: 75, Issue:9 | Inhibition of hypoxia inducible factor-2 transcription: isolation of active modulators from marine sponges. |
AID260415 | Inhibition of growth against LoVo cells after 72 hrs exposure | 2006 | Journal of medicinal chemistry, Feb-09, Volume: 49, Issue:3 | Synthesis and cytotoxic evaluation of new derivatives of the marine alkaloid variolin B. |
AID707423 | Downregulation of HIF2alpha mRNA expression in human SK-RC-28 cells at 1 uM after 48 hrs by RT-PCR analysis | 2012 | Journal of natural products, Sep-28, Volume: 75, Issue:9 | Inhibition of hypoxia inducible factor-2 transcription: isolation of active modulators from marine sponges. |
AID707431 | Downregulation of TGFalpha mRNA expression in human SK-RC-28 cells at 1 uM after 48 hrs by RT-PCR analysis | 2012 | Journal of natural products, Sep-28, Volume: 75, Issue:9 | Inhibition of hypoxia inducible factor-2 transcription: isolation of active modulators from marine sponges. |
AID707437 | Downregulation of HIF2alpha mRNA expression in human RCC4 cells at 1 uM after 48 hrs by RT-PCR analysis | 2012 | Journal of natural products, Sep-28, Volume: 75, Issue:9 | Inhibition of hypoxia inducible factor-2 transcription: isolation of active modulators from marine sponges. |
AID707637 | Inhibition of HIF2alpha in human 786-0 cells assessed as reduction in GLUT1 mRNA expression at 1 uM after 48 hrs by RT-PCR analysis | 2012 | Journal of natural products, Sep-28, Volume: 75, Issue:9 | Inhibition of hypoxia inducible factor-2 transcription: isolation of active modulators from marine sponges. |
AID707635 | Inhibition of HIF2alpha in human 786-0 cells assessed as reduction in CCND1 mRNA expression at 1 uM after 48 hrs by RT-PCR analysis | 2012 | Journal of natural products, Sep-28, Volume: 75, Issue:9 | Inhibition of hypoxia inducible factor-2 transcription: isolation of active modulators from marine sponges. |
AID707439 | Downregulation of HIF1alpha mRNA expression in human RCC4 cells at 1 uM after 48 hrs by RT-PCR analysis | 2012 | Journal of natural products, Sep-28, Volume: 75, Issue:9 | Inhibition of hypoxia inducible factor-2 transcription: isolation of active modulators from marine sponges. |
AID260406 | Inhibition of growth against IGROV cells after 72 hrs exposure | 2006 | Journal of medicinal chemistry, Feb-09, Volume: 49, Issue:3 | Synthesis and cytotoxic evaluation of new derivatives of the marine alkaloid variolin B. |
AID707682 | Cytotoxicity against human SK-RC-28 cells expressing HIF1alpha after 2 days by XTT assay | 2012 | Journal of natural products, Sep-28, Volume: 75, Issue:9 | Inhibition of hypoxia inducible factor-2 transcription: isolation of active modulators from marine sponges. |
AID707627 | Inhibition of HIF1alpha in human RCC4 cells coexpressing HIF2alpha assessed as decrease in carbonic anhydrase 9 mRNA expression at 1 uM after 48 hrs by RT-PCR analysis | 2012 | Journal of natural products, Sep-28, Volume: 75, Issue:9 | Inhibition of hypoxia inducible factor-2 transcription: isolation of active modulators from marine sponges. |
AID707849 | Inhibition of HIF2alpha in human 786-0 cells expressing truncated HIF1alpha assessed as reduction in luciferase activity after 24 hrs by reporter gene assay | 2012 | Journal of natural products, Sep-28, Volume: 75, Issue:9 | Inhibition of hypoxia inducible factor-2 transcription: isolation of active modulators from marine sponges. |
AID707630 | Downregulation of HIF2alpha mRNA expression in human 786-0 cells at 1 uM after 48 hrs by RT-PCR analysis | 2012 | Journal of natural products, Sep-28, Volume: 75, Issue:9 | Inhibition of hypoxia inducible factor-2 transcription: isolation of active modulators from marine sponges. |
AID707436 | Inhibition of HIF1alpha in human SK-RC-28 cells assessed as reduction in carbonic anhydrase 9 expression at 1 uM after 48 hrs by RT-PCR analysis | 2012 | Journal of natural products, Sep-28, Volume: 75, Issue:9 | Inhibition of hypoxia inducible factor-2 transcription: isolation of active modulators from marine sponges. |
AID707428 | Downregulation of GLUT1 mRNA expression in human SK-RC-28 cells at 1 uM after 48 hrs by RT-PCR analysis | 2012 | Journal of natural products, Sep-28, Volume: 75, Issue:9 | Inhibition of hypoxia inducible factor-2 transcription: isolation of active modulators from marine sponges. |
AID707441 | Inhibition of HIF1alpha/2alpha in human RCC4 cells assessed as reduction in VEGFA mRNA expression at 1 uM after 48 hrs by RT-PCR analysis | 2012 | Journal of natural products, Sep-28, Volume: 75, Issue:9 | Inhibition of hypoxia inducible factor-2 transcription: isolation of active modulators from marine sponges. |
AID707631 | Downregulation of HIF1alpha mRNA expression in human 786-0 cells at 1 uM after 48 hrs by RT-PCR analysis | 2012 | Journal of natural products, Sep-28, Volume: 75, Issue:9 | Inhibition of hypoxia inducible factor-2 transcription: isolation of active modulators from marine sponges. |
AID260416 | Inhibition of growth against LoVo-Dox cells after 72 hrs exposure | 2006 | Journal of medicinal chemistry, Feb-09, Volume: 49, Issue:3 | Synthesis and cytotoxic evaluation of new derivatives of the marine alkaloid variolin B. |
AID707621 | Inhibition of HIF2alpha in human RCC4 cells coexpressing HIF1alpha assessed as reduction in CCND1 mRNA expression at 1 uM after 48 hrs by RT-PCR analysis | 2012 | Journal of natural products, Sep-28, Volume: 75, Issue:9 | Inhibition of hypoxia inducible factor-2 transcription: isolation of active modulators from marine sponges. |
AID260409 | Inhibition of growth against MEL28 cells after 72 hrs exposure | 2006 | Journal of medicinal chemistry, Feb-09, Volume: 49, Issue:3 | Synthesis and cytotoxic evaluation of new derivatives of the marine alkaloid variolin B. |
AID260405 | Inhibition of growth against SKOV3 cells after 72 hrs exposure | 2006 | Journal of medicinal chemistry, Feb-09, Volume: 49, Issue:3 | Synthesis and cytotoxic evaluation of new derivatives of the marine alkaloid variolin B. |
AID260412 | Inhibition of growth against K562 cells after 72 hrs exposure | 2006 | Journal of medicinal chemistry, Feb-09, Volume: 49, Issue:3 | Synthesis and cytotoxic evaluation of new derivatives of the marine alkaloid variolin B. |
AID707625 | Inhibition of HIF2alpha in human RCC4 cells coexpressing HIF1alpha assessed as reduction in TGFalpha mRNA expression at 1 uM after 48 hrs by RT-PCR analysis | 2012 | Journal of natural products, Sep-28, Volume: 75, Issue:9 | Inhibition of hypoxia inducible factor-2 transcription: isolation of active modulators from marine sponges. |
AID707848 | Inhibition of HIF-mediated VEGFA protein expression in serum deprived human 786-0 cells at 1 uM after 48 hrs relative to control | 2012 | Journal of natural products, Sep-28, Volume: 75, Issue:9 | Inhibition of hypoxia inducible factor-2 transcription: isolation of active modulators from marine sponges. |
AID260411 | Inhibition of growth against A549 cells after 72 hrs exposure | 2006 | Journal of medicinal chemistry, Feb-09, Volume: 49, Issue:3 | Synthesis and cytotoxic evaluation of new derivatives of the marine alkaloid variolin B. |
AID260407 | Inhibition of growth against IGROV-ET cells after 72 hrs exposure | 2006 | Journal of medicinal chemistry, Feb-09, Volume: 49, Issue:3 | Synthesis and cytotoxic evaluation of new derivatives of the marine alkaloid variolin B. |
AID260417 | Inhibition of growth against HeLa cells after 72 hrs exposure | 2006 | Journal of medicinal chemistry, Feb-09, Volume: 49, Issue:3 | Synthesis and cytotoxic evaluation of new derivatives of the marine alkaloid variolin B. |
AID707841 | Cytotoxicity against human RCC4 cells expressing HIF2alpha and HIF1alpha after 2 days by XTT assay | 2012 | Journal of natural products, Sep-28, Volume: 75, Issue:9 | Inhibition of hypoxia inducible factor-2 transcription: isolation of active modulators from marine sponges. |
AID707641 | Down regulation of carbonic anhydrase 9 expression in human 786-0 cells at 1 uM after 48 hrs by RT-PCR analysis | 2012 | Journal of natural products, Sep-28, Volume: 75, Issue:9 | Inhibition of hypoxia inducible factor-2 transcription: isolation of active modulators from marine sponges. |
AID707425 | Downregulation of HIF1alpha mRNA expression in human SK-RC-28 cells at 1 uM after 48 hrs by RT-PCR analysis | 2012 | Journal of natural products, Sep-28, Volume: 75, Issue:9 | Inhibition of hypoxia inducible factor-2 transcription: isolation of active modulators from marine sponges. |
AID707842 | Cytotoxicity against human 786-0 cells expressing HIF2alpha after 2 days by XTT assay | 2012 | Journal of natural products, Sep-28, Volume: 75, Issue:9 | Inhibition of hypoxia inducible factor-2 transcription: isolation of active modulators from marine sponges. |
AID707427 | Downregulation of CCND1 mRNA expression in human SK-RC-28 cells at 1 uM after 48 hrs by RT-PCR analysis | 2012 | Journal of natural products, Sep-28, Volume: 75, Issue:9 | Inhibition of hypoxia inducible factor-2 transcription: isolation of active modulators from marine sponges. |
AID707634 | Inhibition of HIF2alpha in human 786-0 cells assessed as reduction in VEGFA at 1 uM after 48 hrs by RT-PCR analysis | 2012 | Journal of natural products, Sep-28, Volume: 75, Issue:9 | Inhibition of hypoxia inducible factor-2 transcription: isolation of active modulators from marine sponges. |
AID260414 | Inhibition of growth against HT29 cells after 72 hrs exposure | 2006 | Journal of medicinal chemistry, Feb-09, Volume: 49, Issue:3 | Synthesis and cytotoxic evaluation of new derivatives of the marine alkaloid variolin B. |
AID260408 | Inhibition of growth against SKBR3 cells after 72 hrs exposure | 2006 | Journal of medicinal chemistry, Feb-09, Volume: 49, Issue:3 | Synthesis and cytotoxic evaluation of new derivatives of the marine alkaloid variolin B. |
AID260410 | Inhibition of growth against HMEC1 cells after 72 hrs exposure | 2006 | Journal of medicinal chemistry, Feb-09, Volume: 49, Issue:3 | Synthesis and cytotoxic evaluation of new derivatives of the marine alkaloid variolin B. |
AID707433 | Inhibition of HIF1alpha in human SK-RC-28 cells assessed as reduction in VEGFA at 1 uM after 48 hrs by RT-PCR analysis | 2012 | Journal of natural products, Sep-28, Volume: 75, Issue:9 | Inhibition of hypoxia inducible factor-2 transcription: isolation of active modulators from marine sponges. |
AID260418 | Inhibition of growth against HeLa-Apl cells after 72 hrs exposure | 2006 | Journal of medicinal chemistry, Feb-09, Volume: 49, Issue:3 | Synthesis and cytotoxic evaluation of new derivatives of the marine alkaloid variolin B. |
AID260413 | Inhibition of growth against PANC1 cells after 72 hrs exposure | 2006 | Journal of medicinal chemistry, Feb-09, Volume: 49, Issue:3 | Synthesis and cytotoxic evaluation of new derivatives of the marine alkaloid variolin B. |
AID260404 | Inhibition of growth against LnCAP cells after 72 hrs exposure | 2006 | Journal of medicinal chemistry, Feb-09, Volume: 49, Issue:3 | Synthesis and cytotoxic evaluation of new derivatives of the marine alkaloid variolin B. |
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] |
Research
Studies (12)
Timeframe | Studies, This Drug (%) | All Drugs % |
---|---|---|
pre-1990 | 0 (0.00) | 18.7374 |
1990's | 0 (0.00) | 18.2507 |
2000's | 8 (66.67) | 29.6817 |
2010's | 4 (33.33) | 24.3611 |
2020's | 0 (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: 19.44
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 moderate demand-to-supply ratio for research on this compound.
| This Compound (19.44) All Compounds (24.57) |
Study Types
Publication Type | This drug (%) | All Drugs (%) |
---|---|---|
Trials | 0 (0.00%) | 5.53% |
Reviews | 2 (16.67%) | 6.00% |
Case Studies | 0 (0.00%) | 4.05% |
Observational | 0 (0.00%) | 0.25% |
Other | 10 (83.33%) | 84.16% |
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] |