rhosin profile

rhosin: contains two aromatic rings tethered by a linker, no other info available 2/2014 [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

rhosin : A D-tryptophan derivative obtained by formal condensation of the carboxy group of D-tryptophan with the amino group of (quinoxalin-6-yl)methylidenehydrazide. It directly targets the Rho GEF binding domain, thereby preventing Rho from interacting with its GEFs [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]

Cross-References

ID Source	ID
PubMed CID	9552914
CHEMBL ID	4463605
CHEBI ID	137693
SCHEMBL ID	15936925
SCHEMBL ID	17603571
MeSH ID	M0591923

Synonyms (16)

Synonym
d-tryptophan (2e)-2-(6-quinoxalinylmethylene)hydrazide
(quinoxalinylmethylidene-d-tryptophanyl)hydrazide
CHEBI:137693
rhosin
(2r)-2-amino-3-(1h-indol-3-yl)-n'-[(e)-(quinoxalin-6-yl)methylidene]propanehydrazide
CS-3878
AKOS025118596
SCHEMBL15936925
HY-12646A
SCHEMBL17603571
CHEMBL4463605
(r,e)-2-amino-3-(1h-indol-3-yl)-n'-(quinoxalin-6-ylmethylene)propanehydrazide
(2r)-2-amino-3-(1h-indol-3-yl)-n-[(e)-quinoxalin-6-ylmethylideneamino]propanamide
1173671-63-0
EN300-304748
EX-A6255

Role	Description
RhoA inhibitor	Any inhibitor that interferes with the action of the protein RhoA.
RhoC inhibitor	Any inhibitor that interferes with the action of the protein RhoC.
antineoplastic agent	A substance that inhibits or prevents the proliferation of neoplasms.
[role 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]

Drug Classes (3)

Class	Description
D-tryptophan derivative	A non-proteinogenic amino acid derivative resulting from reaction of D-tryptophan at the amino group or the carboxy group, or from the replacement of any hydrogen of D-tryptophan by a heteroatom.
quinoxaline derivative	Any naphthyridine derivative that is a derivative of quinoxaline (1,4-naphthyridine).
hydrazone	Compounds having the structure R2C=NNR2, formally derived from aldehydes or ketones by replacing =O by =NNH2 (or substituted analogues).
[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 Targets (1)

Inhibition Measurements

Protein	Taxonomy	Measurement	Average	Min (ref.)	Avg (ref.)	Max (ref.)	Bioassay(s)
Rho guanine nucleotide exchange factor 12	Homo sapiens (human)	IC50 (µMol)	10.0000	10.0000	10.0000	10.0000	AID1620025
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (3)

Process	via Protein(s)	Taxonomy
G protein-coupled receptor signaling pathway	Rho guanine nucleotide exchange factor 12	Homo sapiens (human)
Rho protein signal transduction	Rho guanine nucleotide exchange factor 12	Homo sapiens (human)
regulation of small GTPase mediated signal transduction	Rho guanine nucleotide exchange factor 12	Homo sapiens (human)
G protein-coupled receptor signaling pathway	Rho guanine nucleotide exchange factor 12	Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (4)

Process	via Protein(s)	Taxonomy
G protein-coupled receptor binding	Rho guanine nucleotide exchange factor 12	Homo sapiens (human)
guanyl-nucleotide exchange factor activity	Rho guanine nucleotide exchange factor 12	Homo sapiens (human)
GTPase activator activity	Rho guanine nucleotide exchange factor 12	Homo sapiens (human)
protein binding	Rho guanine nucleotide exchange factor 12	Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (4)

Process	via Protein(s)	Taxonomy
cytoplasm	Rho guanine nucleotide exchange factor 12	Homo sapiens (human)
cytosol	Rho guanine nucleotide exchange factor 12	Homo sapiens (human)
membrane	Rho guanine nucleotide exchange factor 12	Homo sapiens (human)
extracellular exosome	Rho guanine nucleotide exchange factor 12	Homo sapiens (human)
cytoplasm	Rho guanine nucleotide exchange factor 12	Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Timeframe	Studies, This Drug (%)	All Drugs %
pre-1990	0 (0.00)	18.7374
1990's	0 (0.00)	18.2507
2000's	0 (0.00)	29.6817
2010's	8 (66.67)	24.3611
2020's	4 (33.33)	2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 26.72

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.

Metric	This Compound (vs All)
Research Demand Index	26.72 (24.57)
Research Supply Index	2.56 (2.92)
Research Growth Index	4.62 (4.65)
Search Engine Demand Index	29.35 (26.88)
Search Engine Supply Index	2.00 (0.95)

This Compound (26.72)

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	12 (100.00%)	84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Substance	Relationship Strength	Studies	Classes	Roles
phosphotyrosine Phosphotyrosine: An amino acid that occurs in endogenous proteins. Tyrosine phosphorylation and dephosphorylation plays a role in cellular signal transduction and possibly in cell growth control and carcinogenesis.. O(4)-phospho-L-tyrosine : A non-proteinogenic L-alpha-amino acid that is L-tyrosine phosphorylated at the phenolic hydroxy group.	2.17	1	L-tyrosine derivative; non-proteinogenic L-alpha-amino acid; O(4)-phosphotyrosine	Escherichia coli metabolite; immunogen
paxilline paxilline: structure given in first source; RN given refers to (2R-(2alpha,4bbeta,6aalpha,12bbeta,12calpha,14abeta))-isomer. paxilline : An indole diterpene alkaloid with formula C27H33NO4 isolated from Penicillium paxilli. It is a potent inhibitor of large conductance Ca2(+)- and voltage-activated K(+) (BK)-type channels.	2.17	1	diterpene alkaloid; enone; organic heterohexacyclic compound; terpenoid indole alkaloid; tertiary alcohol	anticonvulsant; Aspergillus metabolite; EC 3.6.3.8 (Ca(2+)-transporting ATPase) inhibitor; genotoxin; geroprotector; mycotoxin; Penicillium metabolite; potassium channel blocker
angiotensin ii Giapreza: injectable form of angiotensin II used to increase blood pressure in adult patients with septic or other distributive shock. Ile(5)-angiotensin II : An angiotensin II that acts on the central nervous system (PDB entry: 1N9V).	2.31	1	amino acid zwitterion; angiotensin II	human metabolite
gastrins Gastrins: A family of gastrointestinal peptide hormones that excite the secretion of GASTRIC JUICE. They may also occur in the central nervous system where they are presumed to be neurotransmitters.	2.17	1

Condition	Relationship Strength	Studies
ER-Negative PR-Negative HER2-Negative Breast Cancer [description not available]	2.25	1
Invasiveness, Neoplasm [description not available]	2.61	2
Triple Negative Breast Neoplasms Breast neoplasms that do not express ESTROGEN RECEPTORS; PROGESTERONE RECEPTORS; and do not overexpress the NEU RECEPTOR/HER-2 PROTO-ONCOGENE PROTEIN.	2.25	1
Chromosome Deletion Actual loss of portion of a chromosome.	2.31	1
Disease Exacerbation [description not available]	2.17	1
Cancer of Pancreas [description not available]	2.17	1
Pancreatic Neoplasms Tumors or cancer of the PANCREAS. Depending on the types of ISLET CELLS present in the tumors, various hormones can be secreted: GLUCAGON from PANCREATIC ALPHA CELLS; INSULIN from PANCREATIC BETA CELLS; and SOMATOSTATIN from the SOMATOSTATIN-SECRETING CELLS. Most are malignant except the insulin-producing tumors (INSULINOMA).	2.17	1
Neointima The new and thickened layer of scar tissue that forms on a PROSTHESIS, or as a result of vessel injury especially following ANGIOPLASTY or stent placement.	2.21	1
Constriction, Pathological [description not available]	2.21	1
Constriction, Pathologic The condition of an anatomical structure's being constricted beyond normal dimensions.	2.21	1

rhosin

Description

Cross-References

Synonyms (16)

Roles (3)

Drug Classes (3)

Protein Targets (1)

Inhibition Measurements

Biological Processes (3)

Molecular Functions (4)

Ceullar Components (4)

Research

Studies (12)

Market Indicators

Research Demand Index: 26.72

Study Types

rhosin

Description

Cross-References

Synonyms (16)

Roles (3)

Drug Classes (3)

Protein Targets (1)

Inhibition Measurements

Biological Processes (3)

Molecular Functions (4)

Ceullar Components (4)

Research

Studies (12)

Market Indicators

Research Demand Index: 26.72

Study Types

Related Drugs (4)

Related Conditions (10)