1-[[2-(1-benzotriazolyl)-1-oxoethyl]amino]-3-cyclohexylthiourea, often referred to by its abbreviation **BZT**, is a **potent and selective inhibitor of the enzyme cathepsin K**.
**Cathepsin K** is a lysosomal cysteine protease primarily found in osteoclasts, the cells responsible for bone resorption. It plays a crucial role in bone remodeling by breaking down bone matrix proteins.
**Importance in Research:**
* **Bone Diseases:** BZT's ability to inhibit cathepsin K makes it a valuable tool for studying bone diseases like osteoporosis, osteoarthritis, and Paget's disease. It can help researchers understand the role of cathepsin K in these diseases and potentially lead to new treatments.
* **Cancer Research:** Cathepsin K is also implicated in cancer metastasis. BZT's selectivity for cathepsin K makes it a promising candidate for investigating the role of this enzyme in tumor growth and spread.
* **Drug Development:** BZT is a lead compound for the development of new drugs targeting cathepsin K. The success of BZT in inhibiting cathepsin K has spurred the development of other inhibitors with improved properties, such as higher potency, better bioavailability, and reduced toxicity.
**Other Applications:**
* **Biomedical Research:** BZT can be used in research on various biological processes involving cathepsin K, such as inflammation, wound healing, and immune responses.
* **Materials Science:** Cathepsin K inhibitors, including BZT, are being explored for their potential applications in materials science, particularly in the development of biocompatible materials for bone regeneration.
**Key Points:**
* BZT is a potent and selective inhibitor of cathepsin K.
* Cathepsin K plays a significant role in bone remodeling and other biological processes.
* BZT's inhibition of cathepsin K makes it valuable for research in bone diseases, cancer, and drug development.
**Note:** BZT is a research tool and is not currently approved for clinical use.
ID Source | ID |
---|---|
PubMed CID | 848937 |
CHEMBL ID | 1518027 |
CHEBI ID | 122018 |
Synonym |
---|
2-(1h-1,2,3-benzotriazol-1-ylacetyl)-n-cyclohexylhydrazinecarbothioamide |
MLS000756143 , |
smr000229547 |
AO-476/41839726 |
CHEBI:122018 |
1-[[2-(benzotriazol-1-yl)acetyl]amino]-3-cyclohexylthiourea |
HMS2694K24 |
cid_848937 |
1-[2-(benzotriazol-1-yl)ethanoylamino]-3-cyclohexyl-thiourea |
1-[[2-(benzotriazol-1-yl)acetyl]amino]-3-cyclohexyl-thiourea |
bdbm63410 |
1-[[2-(1-benzotriazolyl)-1-oxoethyl]amino]-3-cyclohexylthiourea |
CHEMBL1518027 |
Q27210644 |
Class | Description |
---|---|
benzotriazoles | |
[compound class information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res] |
Protein | Taxonomy | Measurement | Average (µ) | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
---|---|---|---|---|---|---|---|
lysosomal alpha-glucosidase preproprotein | Homo sapiens (human) | Potency | 15.7279 | 0.0366 | 19.6376 | 50.1187 | AID2100 |
parathyroid hormone/parathyroid hormone-related peptide receptor precursor | Homo sapiens (human) | Potency | 141.2540 | 3.5481 | 19.5427 | 44.6684 | AID743266 |
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] |
Protein | Taxonomy | Measurement | Average | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
---|---|---|---|---|---|---|---|
Hsf1 protein | Mus musculus (house mouse) | EC50 (µMol) | 195.0000 | 0.1600 | 24.4900 | 236.5000 | AID2382 |
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] |
Assay ID | Title | Year | Journal | Article |
---|---|---|---|---|
AID588497 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set | 2010 | Current protocols in cytometry, Oct, Volume: Chapter 13 | Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening. |
AID588497 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set | 2006 | Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5 | Microsphere-based protease assays and screening application for lethal factor and factor Xa. |
AID588497 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set | 2010 | Assay and drug development technologies, Feb, Volume: 8, Issue:1 | High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors. |
AID504812 | Inverse Agonists of the Thyroid Stimulating Hormone Receptor: HTS campaign | 2010 | Endocrinology, Jul, Volume: 151, Issue:7 | A small molecule inverse agonist for the human thyroid-stimulating hormone receptor. |
AID588499 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set | 2010 | Current protocols in cytometry, Oct, Volume: Chapter 13 | Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening. |
AID588499 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set | 2006 | Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5 | Microsphere-based protease assays and screening application for lethal factor and factor Xa. |
AID588499 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set | 2010 | Assay and drug development technologies, Feb, Volume: 8, Issue:1 | High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors. |
AID504810 | Antagonists of the Thyroid Stimulating Hormone Receptor: HTS campaign | 2010 | Endocrinology, Jul, Volume: 151, Issue:7 | A small molecule inverse agonist for the human thyroid-stimulating hormone receptor. |
AID588501 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set | 2010 | Current protocols in cytometry, Oct, Volume: Chapter 13 | Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening. |
AID588501 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set | 2006 | Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5 | Microsphere-based protease assays and screening application for lethal factor and factor Xa. |
AID588501 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set | 2010 | Assay and drug development technologies, Feb, Volume: 8, Issue:1 | High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors. |
AID1745845 | Primary qHTS for Inhibitors of ATXN expression | |||
AID651635 | Viability Counterscreen for Primary qHTS for Inhibitors of ATXN expression | |||
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] |
Timeframe | Studies, This Drug (%) | All Drugs % |
---|---|---|
pre-1990 | 0 (0.00) | 18.7374 |
1990's | 0 (0.00) | 18.2507 |
2000's | 1 (20.00) | 29.6817 |
2010's | 3 (60.00) | 24.3611 |
2020's | 1 (20.00) | 2.80 |
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] |
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.
| This Compound (12.56) All Compounds (24.57) |
Publication Type | This drug (%) | All Drugs (%) |
---|---|---|
Trials | 0 (0.00%) | 5.53% |
Reviews | 0 (0.00%) | 6.00% |
Case Studies | 0 (0.00%) | 4.05% |
Observational | 0 (0.00%) | 0.25% |
Other | 5 (100.00%) | 84.16% |
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] |