Page last updated: 2024-11-09

fatostatin

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

Description

fatostatin: inhibits activation of SREBP; structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID1889993
CHEMBL ID1621019
CHEBI ID95052
SCHEMBL ID2742732
MeSH IDM0541890

Synonyms (35)

Synonym
AKOS005434229
2-propyl-4-(4-p-tolyl-thiazol-2-yl)-pyridine
smr000221636
MLS000332366 ,
OPREA1_120708
STK326446
4-[4-(4-methylphenyl)-1,3-thiazol-2-yl]-2-propylpyridine
4-(4-methylphenyl)-2-(2-propylpyridin-4-yl)-1,3-thiazole
CHEMBL1621019 ,
fatostatin
S9785
125256-00-0
ZROSUBKIGBSZCG-UHFFFAOYSA-N
4-(4-methylphenyl)-2-(2-propylpyridin-4-yl)-1,3-thiazole;hydrobromide
bdbm78179
cid_2850562
2-(2-propyl-4-pyridyl)-4-(p-tolyl)thiazole;hydrobromide
4-(4-methylphenyl)-2-(2-propyl-4-pyridinyl)thiazole;hydrobromide
SCHEMBL2742732
fatostatin a
AC-35652
2-(2-propyl-4-pyridyl)-4-(p-tolyl)thiazole
CS-5810
HY-14452
CHEBI:95052
2-(2-propylpyridin-4-yl)-4-(p-tolyl)thiazole ,
fatostatin;125b11
BCP20994
4-(4-methylphenyl)-2-(2-propyl-4-pyridinyl)thiazole
Q27166821
BS-15072
AMY41632
D84076
pyridine, 4-[4-(4-methylphenyl)-2-thiazolyl]-2-propyl-
4-(4-methylphenyl)-2-(2-propyl-4-pyridyl)-1,3-thiazole

Research Excerpts

Overview

Fatostatin is a small molecule that inhibits the maturation and function of SREBP. Its role in regulating inflammation is poorly understood.

ExcerptReferenceRelevance
"Fatostatin is a small molecule that inhibits the maturation and function of SREBP, and its role in regulating inflammation is poorly understood."( Fatostatin ameliorates inflammation without affecting cell viability.
Akizuki, S; Hashimoto, M; Kitagori, K; Ma, S; Mimori, T; Morinobu, A; Murakami, K; Nakashima, R; Ohmura, K; Tanaka, K; Tanaka, M; Yoshifuji, H, 2022
)
2.89
"Fatostatin is a small molecule non-sterol diarylthiazole derivative that acts as a chemical inhibitor of the sterol regulatory-element binding protein (SREBP) pathway."( Fatostatin inhibits the development of endometrial carcinoma in endometrial carcinoma cells and a xenograft model by targeting lipid metabolism.
Chen, S; Li, W; Yao, L, 2020
)
2.72
"Fatostatin is a chemical inhibitor of the SREBP pathway that directly binds SCAP and blocks its ER-to-Golgi transport."( Fatostatin blocks ER exit of SCAP but inhibits cell growth in a SCAP-independent manner.
Espenshade, PJ; Machamer, CE; Shao, W, 2016
)
2.6

Actions

Fatostatin's ability to inhibit SREBP activity and cell division could prove beneficial in treating aggressive types of cancers such as glioblastomas that have elevated lipid metabolism and fast proliferation rates.

ExcerptReferenceRelevance
"Fatostatin inhibited the increase of both isoforms of SREBP (types 1 and 2) in diabetic kidneys."( Inhibition of SREBP With Fatostatin Does Not Attenuate Early Diabetic Nephropathy in Male Mice.
Gao, B; Ingram, AJ; Krepinsky, JC; Marway, M; Mehta, N; Parthasarathy, P; Van Krieken, R, 2018
)
1.51
"Thus Fatostatin's ability to inhibit SREBP activity and cell division could prove beneficial in treating aggressive types of cancers such as glioblastomas that have elevated lipid metabolism and fast proliferation rates and often develop resistance to current anticancer therapies."( Fatostatin Inhibits Cancer Cell Proliferation by Affecting Mitotic Microtubule Spindle Assembly and Cell Division.
Bensinger, SJ; Cheung, K; Gholkar, AA; Hamideh, SA; Khuu, C; Lo, YC; Nnebe, C; Torres, JZ; Williams, KJ, 2016
)
2.33

Compound-Compound Interactions

ExcerptReferenceRelevance
" These data suggest for the first time that fatostatin alone or in combination with docetaxel could be exploited as a novel and promising therapy for metastatic PCa harboring p53 mutations."( Anti-cancer efficacy of SREBP inhibitor, alone or in combination with docetaxel, in prostate cancer harboring p53 mutations.
Chung, LW; Huang, WC; Li, X; Wu, JB, 2015
)
0.68
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Drug Classes (1)

ClassDescription
thiazolesAn azole in which the five-membered heterocyclic aromatic skeleton contains a N atom and one S atom.
[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

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Sterol regulatory element-binding protein 2Homo sapiens (human)IC50 (µMol)7.80000.30005.300010.0000AID615677; AID615679
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (16)

Processvia Protein(s)Taxonomy
positive regulation of cholesterol storageSterol regulatory element-binding protein 2Homo sapiens (human)
negative regulation of cholesterol effluxSterol regulatory element-binding protein 2Homo sapiens (human)
positive regulation of transcription by RNA polymerase IISterol regulatory element-binding protein 2Homo sapiens (human)
negative regulation of transcription by RNA polymerase IISterol regulatory element-binding protein 2Homo sapiens (human)
lipid metabolic processSterol regulatory element-binding protein 2Homo sapiens (human)
cholesterol metabolic processSterol regulatory element-binding protein 2Homo sapiens (human)
regulation of Notch signaling pathwaySterol regulatory element-binding protein 2Homo sapiens (human)
cellular response to starvationSterol regulatory element-binding protein 2Homo sapiens (human)
SREBP signaling pathwaySterol regulatory element-binding protein 2Homo sapiens (human)
cholesterol homeostasisSterol regulatory element-binding protein 2Homo sapiens (human)
positive regulation of cholesterol biosynthetic processSterol regulatory element-binding protein 2Homo sapiens (human)
positive regulation of transcription by RNA polymerase IISterol regulatory element-binding protein 2Homo sapiens (human)
cellular response to low-density lipoprotein particle stimulusSterol regulatory element-binding protein 2Homo sapiens (human)
cellular response to laminar fluid shear stressSterol regulatory element-binding protein 2Homo sapiens (human)
regulation of mitophagySterol regulatory element-binding protein 2Homo sapiens (human)
positive regulation of miRNA transcriptionSterol regulatory element-binding protein 2Homo sapiens (human)
positive regulation of protein targeting to mitochondrionSterol regulatory element-binding protein 2Homo sapiens (human)
positive regulation of cholesterol storageSterol regulatory element-binding protein 2Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (8)

Processvia Protein(s)Taxonomy
C-8 sterol isomerase activitySterol regulatory element-binding protein 2Homo sapiens (human)
RNA polymerase II cis-regulatory region sequence-specific DNA bindingSterol regulatory element-binding protein 2Homo sapiens (human)
DNA-binding transcription factor activity, RNA polymerase II-specificSterol regulatory element-binding protein 2Homo sapiens (human)
DNA-binding transcription repressor activity, RNA polymerase II-specificSterol regulatory element-binding protein 2Homo sapiens (human)
protein bindingSterol regulatory element-binding protein 2Homo sapiens (human)
protein dimerization activitySterol regulatory element-binding protein 2Homo sapiens (human)
E-box bindingSterol regulatory element-binding protein 2Homo sapiens (human)
sequence-specific double-stranded DNA bindingSterol regulatory element-binding protein 2Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (11)

Processvia Protein(s)Taxonomy
Golgi membraneSterol regulatory element-binding protein 2Homo sapiens (human)
nucleusSterol regulatory element-binding protein 2Homo sapiens (human)
nucleoplasmSterol regulatory element-binding protein 2Homo sapiens (human)
cytoplasmSterol regulatory element-binding protein 2Homo sapiens (human)
endoplasmic reticulumSterol regulatory element-binding protein 2Homo sapiens (human)
endoplasmic reticulum membraneSterol regulatory element-binding protein 2Homo sapiens (human)
cytosolSterol regulatory element-binding protein 2Homo sapiens (human)
ER to Golgi transport vesicle membraneSterol regulatory element-binding protein 2Homo sapiens (human)
intracellular membrane-bounded organelleSterol regulatory element-binding protein 2Homo sapiens (human)
chromatinSterol regulatory element-binding protein 2Homo sapiens (human)
SREBP-SCAP-Insig complexSterol regulatory element-binding protein 2Homo sapiens (human)
nucleusSterol regulatory element-binding protein 2Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (18)

Assay IDTitleYearJournalArticle
AID1181169Antimicrobial activity against second mutant generation Mycobacterium tuberculosis 1024_18 assessed as fold shift in MIC relative to parent strain2014Journal of medicinal chemistry, Aug-14, Volume: 57, Issue:15
Diarylthiazole: an antimycobacterial scaffold potentially targeting PrrB-PrrA two-component system.
AID615770Metabolic stability in mouse hepatocytes at 1 uM after 90 mins by LC-MS/MS analysis2011Journal of medicinal chemistry, Jul-14, Volume: 54, Issue:13
Synthesis and evaluation of diarylthiazole derivatives that inhibit activation of sterol regulatory element-binding proteins.
AID1181168Antimicrobial activity against first mutant generation Mycobacterium tuberculosis 1024_18 assessed as fold shift in MIC relative to parent strain2014Journal of medicinal chemistry, Aug-14, Volume: 57, Issue:15
Diarylthiazole: an antimycobacterial scaffold potentially targeting PrrB-PrrA two-component system.
AID615766Aqueous solubility of the compound at pH 3 after 24 hrs by LC-MS/MS analysis2011Journal of medicinal chemistry, Jul-14, Volume: 54, Issue:13
Synthesis and evaluation of diarylthiazole derivatives that inhibit activation of sterol regulatory element-binding proteins.
AID1181170Antimicrobial activity against second mutant generation Mycobacterium tuberculosis 1024_8.12 assessed as fold shift in MIC relative to parent strain2014Journal of medicinal chemistry, Aug-14, Volume: 57, Issue:15
Diarylthiazole: an antimycobacterial scaffold potentially targeting PrrB-PrrA two-component system.
AID1181148Solubility of the compound2014Journal of medicinal chemistry, Aug-14, Volume: 57, Issue:15
Diarylthiazole: an antimycobacterial scaffold potentially targeting PrrB-PrrA two-component system.
AID1181171Antimicrobial activity against second mutant generation Mycobacterium tuberculosis 1024_16.5 assessed as fold shift in MIC relative to parent strain2014Journal of medicinal chemistry, Aug-14, Volume: 57, Issue:15
Diarylthiazole: an antimycobacterial scaffold potentially targeting PrrB-PrrA two-component system.
AID1181167Antimicrobial activity against first mutant generation Mycobacterium tuberculosis 1024_1 assessed as fold shift in MIC relative to parent strain2014Journal of medicinal chemistry, Aug-14, Volume: 57, Issue:15
Diarylthiazole: an antimycobacterial scaffold potentially targeting PrrB-PrrA two-component system.
AID615771Apparent permeability at 10 uM after 4 hrs by PAMPA2011Journal of medicinal chemistry, Jul-14, Volume: 54, Issue:13
Synthesis and evaluation of diarylthiazole derivatives that inhibit activation of sterol regulatory element-binding proteins.
AID615679Inhibition of SREBP2 activation expressed in CHO-K1 cells by densitometric analysis2011Journal of medicinal chemistry, Jul-14, Volume: 54, Issue:13
Synthesis and evaluation of diarylthiazole derivatives that inhibit activation of sterol regulatory element-binding proteins.
AID615769Half life in mouse hepatocytes at 1 uM after 90 mins by LC-MS/MS analysis2011Journal of medicinal chemistry, Jul-14, Volume: 54, Issue:13
Synthesis and evaluation of diarylthiazole derivatives that inhibit activation of sterol regulatory element-binding proteins.
AID1181176Antimicrobial activity against Mycobacterium tuberculosis H37Rv over-expressing InhA cells assessed as upshift of MIC relative to wild type2014Journal of medicinal chemistry, Aug-14, Volume: 57, Issue:15
Diarylthiazole: an antimycobacterial scaffold potentially targeting PrrB-PrrA two-component system.
AID615778Apparent permeability assessed as membrane retention at 10 uM after 4 hrs by PAMPA2011Journal of medicinal chemistry, Jul-14, Volume: 54, Issue:13
Synthesis and evaluation of diarylthiazole derivatives that inhibit activation of sterol regulatory element-binding proteins.
AID1181172Antimicrobial activity against second mutant generation Mycobacterium tuberculosis 1024_16.6 assessed as fold shift in MIC relative to parent strain2014Journal of medicinal chemistry, Aug-14, Volume: 57, Issue:15
Diarylthiazole: an antimycobacterial scaffold potentially targeting PrrB-PrrA two-component system.
AID615768Intrinsic clearance in mouse hepatocytes at 1 uM after 90 mins by LC-MS/MS analysis2011Journal of medicinal chemistry, Jul-14, Volume: 54, Issue:13
Synthesis and evaluation of diarylthiazole derivatives that inhibit activation of sterol regulatory element-binding proteins.
AID615677Inhibition of SREBP2 activation expressed in CHO-K1 cells co-transfected with pSRE-Luc plasmid assessed as inhibition of luciferase expression after 20 hrs by luciferase reporter gene assay2011Journal of medicinal chemistry, Jul-14, Volume: 54, Issue:13
Synthesis and evaluation of diarylthiazole derivatives that inhibit activation of sterol regulatory element-binding proteins.
AID1181147Antimicrobial activity against Mycobacterium tuberculosis H37Rv ATCC 27294 assessed as growth inhibition after 5 days by microdilution method2014Journal of medicinal chemistry, Aug-14, Volume: 57, Issue:15
Diarylthiazole: an antimycobacterial scaffold potentially targeting PrrB-PrrA two-component system.
AID615767Aqueous solubility of the compound at pH 7 after 24 hrs by LC-MS/MS analysis2011Journal of medicinal chemistry, Jul-14, Volume: 54, Issue:13
Synthesis and evaluation of diarylthiazole derivatives that inhibit activation of sterol regulatory element-binding proteins.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (34)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's1 (2.94)29.6817
2010's24 (70.59)24.3611
2020's9 (26.47)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 35.38

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 strong demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index35.38 (24.57)
Research Supply Index3.56 (2.92)
Research Growth Index6.55 (4.65)
Search Engine Demand Index42.51 (26.88)
Search Engine Supply Index2.04 (0.95)

This Compound (35.38)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials0 (0.00%)5.53%
Reviews2 (5.88%)6.00%
Case Studies1 (2.94%)4.05%
Observational0 (0.00%)0.25%
Other31 (91.18%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]