Page last updated: 2024-11-12
kw 2581
Description
Research Excerpts
Clinical Trials
Roles
Classes
Pathways
Study Profile
Bioassays
Related Drugs
Related Conditions
Protein Interactions
Research Growth
Description
KW 2581: structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]
Cross-References
| ID Source | ID |
|---|---|
| PubMed CID | 9912111 |
| CHEMBL ID | 3612355 |
| SCHEMBL ID | 5707498 |
| MeSH ID | M0515617 |
Synonyms (18)
| Synonym |
|---|
| kw 2581 |
| kw-2581 |
| kw2581 |
| chembl3612355 , |
| bdbm50116170 |
| SCHEMBL5707498 |
| 17-diisopropylcarbamoyl-1,3,5(10),16-estratetraen-3-yl sulfamate |
| estra-1,3,5(10),16-tetraene-17-carboxamide, 3-((aminodsulfonyl)oxy)-n,n-bis(1-methylethyl)- |
| c38u4wz67t , |
| unii-c38u4wz67t |
| 284045-56-3 |
| [(8s,9s,13s,14s)-17-[di(propan-2-yl)carbamoyl]-13-methyl-6,7,8,9,11,12,14,15-octahydrocyclopenta[a]phenanthren-3-yl] sulfamate |
| 3-((aminosulfonyl)oxy)-n,n-bis(1-methylethyl)estra-1,3,5(10),16-tetraene-17-carboxamide |
| (3as,3bs,9bs,11as)-1-(bis(propan-2-yl)carbamoyl)-11a-methyl-3h,3ah,3bh,4h,5h,9bh,10h,11h,11ah-cyclopenta(a)phenanthren-7-yl sulfamate |
| ((8s,9s,13s,14s)-17-(di(propan-2-yl)carbamoyl)-13-methyl-6,7,8,9,11,12,14,15-octahydrocyclopenta(a)phenanthren-3-yl) sulfamate |
| estra-1,3,5(10),16-tetraene-17-carboxamide, 3-((aminosulfonyl)oxy)-n,n-bis(1-methylethyl)- |
| (8s,9s,13s,14s)-17-(diisopropylcarbamoyl)-13-methyl-7,8,9,11,12,13,14,15-octahydro-6h-cyclopenta[a]phenanthren-3-yl sulfamate |
| STARBLD0038656 |
Research Excerpts
Dosage Studied
| Excerpt | Relevance | Reference |
|---|---|---|
| " Dose-response studies in the same rat model demonstrated that more than 90% inhibition of STS activity in tumors was necessary to induce tumor shrinkage." | ( A novel steroidal selective steroid sulfatase inhibitor KW-2581 inhibits sulfated-estrogen dependent growth of breast cancer cells in vitro and in animal models. Akinaga, S; Anazawa, H; Ishida, H; Kuwabara, T; Li, PK; Murakata, C; Nakata, T; Sato, N; Shiotsu, Y; Suzuki, M; Takebayashi, M; Tanaka, H; Terasaki, Y, 2007) | 0.34 |
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]
Protein Targets (3)
Inhibition Measurements
| Protein | Taxonomy | Measurement | Average | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
|---|---|---|---|---|---|---|---|
| Steryl-sulfatase | Homo sapiens (human) | IC50 (µMol) | 0.0040 | 0.0001 | 0.4071 | 7.6000 | AID1243902 |
| Neuronal acetylcholine receptor subunit beta-3 | Rattus norvegicus (Norway rat) | IC50 (µMol) | 0.0040 | 0.0020 | 0.0268 | 0.1000 | AID1243902 |
| Neuronal acetylcholine receptor subunit alpha-6 | Rattus norvegicus (Norway rat) | IC50 (µMol) | 0.0040 | 0.0020 | 0.6904 | 6.0000 | AID1243902 |
| [prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] | |||||||
Biological Processes (3)
| Process | via Protein(s) | Taxonomy |
|---|---|---|
| steroid catabolic process | Steryl-sulfatase | Homo sapiens (human) |
| female pregnancy | Steryl-sulfatase | Homo sapiens (human) |
| epidermis development | Steryl-sulfatase | Homo sapiens (human) |
| [Information is prepared from geneontology information from the June-17-2024 release] | ||
Molecular Functions (4)
| Process | via Protein(s) | Taxonomy |
|---|---|---|
| steryl-sulfatase activity | Steryl-sulfatase | Homo sapiens (human) |
| sulfuric ester hydrolase activity | Steryl-sulfatase | Homo sapiens (human) |
| metal ion binding | Steryl-sulfatase | Homo sapiens (human) |
| arylsulfatase activity | Steryl-sulfatase | Homo sapiens (human) |
| [Information is prepared from geneontology information from the June-17-2024 release] | ||
Ceullar Components (9)
| Process | via Protein(s) | Taxonomy |
|---|---|---|
| lysosome | Steryl-sulfatase | Homo sapiens (human) |
| endosome | Steryl-sulfatase | Homo sapiens (human) |
| endoplasmic reticulum | Steryl-sulfatase | Homo sapiens (human) |
| endoplasmic reticulum lumen | Steryl-sulfatase | Homo sapiens (human) |
| endoplasmic reticulum membrane | Steryl-sulfatase | Homo sapiens (human) |
| Golgi apparatus | Steryl-sulfatase | Homo sapiens (human) |
| plasma membrane | Steryl-sulfatase | Homo sapiens (human) |
| membrane | Steryl-sulfatase | Homo sapiens (human) |
| intracellular membrane-bounded organelle | Steryl-sulfatase | Homo sapiens (human) |
| [Information is prepared from geneontology information from the June-17-2024 release] | ||
Bioassays (1)
| Assay ID | Title | Year | Journal | Article |
|---|---|---|---|---|
| AID1243902 | Inhibition of recombinant human STS transfected in CHO cells using MUS as substrate after 30 mins by fluorescence assay | 2015 | European journal of medicinal chemistry, Aug-28, Volume: 101 | Synthesis of bicoumarin thiophosphate derivatives as steroid sulfatase inhibitors. |
| [information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||||
Research
Studies (6)
| Timeframe | Studies, This Drug (%) | All Drugs % |
|---|---|---|
| pre-1990 | 0 (0.00) | 18.7374 |
| 1990's | 0 (0.00) | 18.2507 |
| 2000's | 3 (50.00) | 29.6817 |
| 2010's | 3 (50.00) | 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] | ||
Study Types
| Publication Type | This drug (%) | All Drugs (%) |
|---|---|---|
| Trials | 0 (0.00%) | 5.53% |
| Reviews | 1 (16.67%) | 6.00% |
| Case Studies | 0 (0.00%) | 4.05% |
| Observational | 0 (0.00%) | 0.25% |
| Other | 5 (83.33%) | 84.16% |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||