Page last updated: 2024-12-11

mkt 077

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

Description

MKT 077: structure given in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID6444403
CHEMBL ID33859
MeSH IDM0257225

Synonyms (22)

Synonym
fj-776
mkt-077
pyridinium, 1-ethyl-2-((3-ethyl-5-(3-methyl-2(3h)-benzothiazolylidene)-4-oxo-2-thiazolidinylidene)methyl)-, chloride
fj 776
mkt 077
CHEMBL33859 ,
147366-41-4
1427472-75-0
mkt 077 [who-dd]
unii-8pf5zxi0je
pyridinium, 1-ethyl-2-((3-ethyl-5-(3-methyl-2(3h)-benzothiazolylidene)-4-oxo-2-thiazolidinylidene)methyl)-, chloride (1:1)
8pf5zxi0je ,
mkt-077, >=98% (hplc), powder
HY-15096
CS-0003758
mkt077
A12388
(2z,5e)-3-ethyl-2-[(1-ethylpyridin-1-ium-2-yl)methylidene]-5-(3-methyl-1,3-benzothiazol-2-ylidene)-1,3-thiazolidin-4-one;chloride
pyridinium, 1-ethyl-2-[[3-ethyl-5-(3-methyl-2(3h)-benzothiazolylidene)-4-oxo-2-thiazolidinylidene]methyl]-, chloride (1:1)
EX-A3230
XFA36641
AKOS040758716

Research Excerpts

Pharmacokinetics

ExcerptReferenceRelevance
"This Phase I study was performed to evaluate the tolerability and pharmacokinetic behavior of MKT-077, a water soluble rhodacyanine dye analogue, which partitions into tumor cell mitochondria where it is thought to act as a metabolic poison, leading to G1 arrest and apoptosis."( A phase I and pharmacokinetic study of the mitochondrial-specific rhodacyanine dye analog MKT 077.
Baker, SD; Britten, CD; Collins, W; Cramer, J; Eckhardt, SG; Rothenberg, M; Rowinsky, EK; Smetzer, L; Smith, L; Stephenson, J; Von Hoff, DD; Weiss, GR, 2000
)
0.53

Dosage Studied

ExcerptRelevanceReference
" Although the same dosage of MKT-077 significantly decreased respiratory rates in rat liver mitochondria relative to untreated controls, complete recovery was evident within 3 days following drug withdrawal."( In vivo administration of MKT-077 causes partial yet reversible impairment of mitochondrial function.
Chen, LB; Koya, K; Li, Y; Modica-Napolitano, J; Weisberg, EL, 1996
)
0.29
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Protein Targets (1)

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Telomerase reverse transcriptaseHomo sapiens (human)IC50 (µMol)5.00000.00062.69489.4000AID648338
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (32)

Processvia Protein(s)Taxonomy
telomere maintenanceTelomerase reverse transcriptaseHomo sapiens (human)
RNA-templated transcriptionTelomerase reverse transcriptaseHomo sapiens (human)
RNA-templated DNA biosynthetic processTelomerase reverse transcriptaseHomo sapiens (human)
telomere maintenance via telomeraseTelomerase reverse transcriptaseHomo sapiens (human)
mitochondrion organizationTelomerase reverse transcriptaseHomo sapiens (human)
negative regulation of gene expressionTelomerase reverse transcriptaseHomo sapiens (human)
DNA strand elongationTelomerase reverse transcriptaseHomo sapiens (human)
positive regulation of Wnt signaling pathwayTelomerase reverse transcriptaseHomo sapiens (human)
siRNA processingTelomerase reverse transcriptaseHomo sapiens (human)
regulation of protein stabilityTelomerase reverse transcriptaseHomo sapiens (human)
positive regulation of protein bindingTelomerase reverse transcriptaseHomo sapiens (human)
positive regulation of hair cycleTelomerase reverse transcriptaseHomo sapiens (human)
negative regulation of neuron apoptotic processTelomerase reverse transcriptaseHomo sapiens (human)
positive regulation of angiogenesisTelomerase reverse transcriptaseHomo sapiens (human)
positive regulation of glucose importTelomerase reverse transcriptaseHomo sapiens (human)
response to cadmium ionTelomerase reverse transcriptaseHomo sapiens (human)
positive regulation of nitric-oxide synthase activityTelomerase reverse transcriptaseHomo sapiens (human)
establishment of protein localization to telomereTelomerase reverse transcriptaseHomo sapiens (human)
cellular response to hypoxiaTelomerase reverse transcriptaseHomo sapiens (human)
DNA biosynthetic processTelomerase reverse transcriptaseHomo sapiens (human)
replicative senescenceTelomerase reverse transcriptaseHomo sapiens (human)
siRNA transcriptionTelomerase reverse transcriptaseHomo sapiens (human)
positive regulation of G1/S transition of mitotic cell cycleTelomerase reverse transcriptaseHomo sapiens (human)
positive regulation of miRNA transcriptionTelomerase reverse transcriptaseHomo sapiens (human)
positive regulation of transdifferentiationTelomerase reverse transcriptaseHomo sapiens (human)
positive regulation of vascular associated smooth muscle cell proliferationTelomerase reverse transcriptaseHomo sapiens (human)
positive regulation of protein localization to nucleolusTelomerase reverse transcriptaseHomo sapiens (human)
positive regulation of vascular associated smooth muscle cell migrationTelomerase reverse transcriptaseHomo sapiens (human)
negative regulation of endothelial cell apoptotic processTelomerase reverse transcriptaseHomo sapiens (human)
positive regulation of stem cell proliferationTelomerase reverse transcriptaseHomo sapiens (human)
negative regulation of cellular senescenceTelomerase reverse transcriptaseHomo sapiens (human)
negative regulation of extrinsic apoptotic signaling pathway in absence of ligandTelomerase reverse transcriptaseHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (16)

Processvia Protein(s)Taxonomy
tRNA bindingTelomerase reverse transcriptaseHomo sapiens (human)
transcription coactivator bindingTelomerase reverse transcriptaseHomo sapiens (human)
DNA bindingTelomerase reverse transcriptaseHomo sapiens (human)
telomerase activityTelomerase reverse transcriptaseHomo sapiens (human)
telomerase RNA reverse transcriptase activityTelomerase reverse transcriptaseHomo sapiens (human)
RNA bindingTelomerase reverse transcriptaseHomo sapiens (human)
RNA-directed DNA polymerase activityTelomerase reverse transcriptaseHomo sapiens (human)
RNA-dependent RNA polymerase activityTelomerase reverse transcriptaseHomo sapiens (human)
protein bindingTelomerase reverse transcriptaseHomo sapiens (human)
identical protein bindingTelomerase reverse transcriptaseHomo sapiens (human)
protein homodimerization activityTelomerase reverse transcriptaseHomo sapiens (human)
metal ion bindingTelomerase reverse transcriptaseHomo sapiens (human)
protein-folding chaperone bindingTelomerase reverse transcriptaseHomo sapiens (human)
telomerase RNA bindingTelomerase reverse transcriptaseHomo sapiens (human)
template-free RNA nucleotidyltransferaseTelomerase reverse transcriptaseHomo sapiens (human)
telomeric DNA bindingTelomerase reverse transcriptaseHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (14)

Processvia Protein(s)Taxonomy
PML bodyTelomerase reverse transcriptaseHomo sapiens (human)
chromosome, telomeric regionTelomerase reverse transcriptaseHomo sapiens (human)
nucleusTelomerase reverse transcriptaseHomo sapiens (human)
nucleoplasmTelomerase reverse transcriptaseHomo sapiens (human)
telomerase holoenzyme complexTelomerase reverse transcriptaseHomo sapiens (human)
nucleolusTelomerase reverse transcriptaseHomo sapiens (human)
cytosolTelomerase reverse transcriptaseHomo sapiens (human)
plasma membraneTelomerase reverse transcriptaseHomo sapiens (human)
nuclear speckTelomerase reverse transcriptaseHomo sapiens (human)
mitochondrial nucleoidTelomerase reverse transcriptaseHomo sapiens (human)
TERT-RMRP complexTelomerase reverse transcriptaseHomo sapiens (human)
telomerase catalytic core complexTelomerase reverse transcriptaseHomo sapiens (human)
nuclear telomere cap complexTelomerase reverse transcriptaseHomo sapiens (human)
RNA-directed RNA polymerase complexTelomerase reverse transcriptaseHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (28)

Assay IDTitleYearJournalArticle
AID492545Antiproliferative activity against human colon cancer cells2010Journal of medicinal chemistry, Jun-24, Volume: 53, Issue:12
Heat shock protein 70 (hsp70) as an emerging drug target.
AID443971Cytotoxicity against rat L6 cells after 72 hrs by Alamar blue assay2010Journal of medicinal chemistry, Jan-14, Volume: 53, Issue:1
Fluorinated rhodacyanine (SJL-01) possessing high efficacy for visceral leishmaniasis (VL).
AID492547Antiproliferative activity against human breast cancer cells2010Journal of medicinal chemistry, Jun-24, Volume: 53, Issue:12
Heat shock protein 70 (hsp70) as an emerging drug target.
AID1824232Inhibition of hedgehog signalling in mouse ASZ001 cells assessed as reduction in Gli1 mRNA expression measured after 48 hrs by RT-PCR analysis2022European journal of medicinal chemistry, Jan-15, Volume: 228Affinity-based protein profiling identifies vitamin D3 as a heat shock protein 70 antagonist that regulates hedgehog transduction in murine basal cell carcinoma.
AID160054In vitro antimalarial activity against chloroquine-sensitive Plasmodium falciparum FCR32002Journal of medicinal chemistry, Feb-28, Volume: 45, Issue:5
Rhodacyanine dyes as antimalarials. 1. Preliminary evaluation of their activity and toxicity.
AID1056252Cytotoxicity against C57BL/6 mouse MEF assessed as growth inhibition after 72 hrs by MTT assay2013ACS medicinal chemistry letters, Nov-14, Volume: 4, Issue:11
Analogs of the Allosteric Heat Shock Protein 70 (Hsp70) Inhibitor, MKT-077, as Anti-Cancer Agents.
AID1871222Inhibition of HSP70 in human HeLa C3 cells overexpressing tau protein assessed as reduction in tau protein level measured after 24 hrs by Western blot analysis2021European journal of medicinal chemistry, Jan-01, Volume: 209Small molecule therapeutics for tauopathy in Alzheimer's disease: Walking on the path of most resistance.
AID492546Antiproliferative activity against human bladder cancer cells2010Journal of medicinal chemistry, Jun-24, Volume: 53, Issue:12
Heat shock protein 70 (hsp70) as an emerging drug target.
AID232807Selective toxicity- EC50 value of FM3A / EC50 value of Plasmodium falciparum2002Journal of medicinal chemistry, Feb-28, Volume: 45, Issue:5
Rhodacyanine dyes as antimalarials. 1. Preliminary evaluation of their activity and toxicity.
AID1056253Cytotoxicity against human MCF7 cells assessed as growth inhibition after 72 hrs by MTT assay2013ACS medicinal chemistry letters, Nov-14, Volume: 4, Issue:11
Analogs of the Allosteric Heat Shock Protein 70 (Hsp70) Inhibitor, MKT-077, as Anti-Cancer Agents.
AID47528In vitro inhibition of growth of human carcinoma CX-1 cell line (clonogenic assay).1998Journal of medicinal chemistry, Jan-01, Volume: 41, Issue:1
Structure-activity of novel rhodacyanine dyes as antitumor agents.
AID443972Selectivity ratio of IC50 for rat L6 cells to IC50 for Leishmania donovani MHOM/ET/67/L822010Journal of medicinal chemistry, Jan-14, Volume: 53, Issue:1
Fluorinated rhodacyanine (SJL-01) possessing high efficacy for visceral leishmaniasis (VL).
AID1824241Inhibition of hedgehog signalling in mouse Ptch-KO MEF cells assessed as reduction in Gli1 mRNA expression measured after 48 hrs by RT-PCR analysis2022European journal of medicinal chemistry, Jan-15, Volume: 228Affinity-based protein profiling identifies vitamin D3 as a heat shock protein 70 antagonist that regulates hedgehog transduction in murine basal cell carcinoma.
AID1056232Drug metabolism in mouse liver microsomes assessed as compound life time2013ACS medicinal chemistry letters, Nov-14, Volume: 4, Issue:11
Analogs of the Allosteric Heat Shock Protein 70 (Hsp70) Inhibitor, MKT-077, as Anti-Cancer Agents.
AID1056254Cytotoxicity against human MDA-MB-231 cells assessed as growth inhibition after 72 hrs by MTT assay2013ACS medicinal chemistry letters, Nov-14, Volume: 4, Issue:11
Analogs of the Allosteric Heat Shock Protein 70 (Hsp70) Inhibitor, MKT-077, as Anti-Cancer Agents.
AID648338Inhibition of telomerase2012Bioorganic & medicinal chemistry, Mar-15, Volume: 20, Issue:6
JFCR39, a panel of 39 human cancer cell lines, and its application in the discovery and development of anticancer drugs.
AID122296In vivo ratio of median survival time of drug-treated to control, untreated tumor-bearing mice at a dose of 5 mg/kg for 4 day1998Journal of medicinal chemistry, Jan-01, Volume: 41, Issue:1
Structure-activity of novel rhodacyanine dyes as antitumor agents.
AID72013Cytotoxicity against mouse mammary tumor FM3A cells representing a model of host2002Journal of medicinal chemistry, Feb-28, Volume: 45, Issue:5
Rhodacyanine dyes as antimalarials. 1. Preliminary evaluation of their activity and toxicity.
AID122337Tumor inhibition (TI) ratio at a dose of 3 mg/kg for 4 day1998Journal of medicinal chemistry, Jan-01, Volume: 41, Issue:1
Structure-activity of novel rhodacyanine dyes as antitumor agents.
AID21984The solubility in water was determined1998Journal of medicinal chemistry, Jan-01, Volume: 41, Issue:1
Structure-activity of novel rhodacyanine dyes as antitumor agents.
AID1824236Inhibition of hedgehog signalling in mouse C3H 10T1/2 cells assessed as reduction in Gli1 mRNA expression measured after 48 hrs by RT-PCR analysis2022European journal of medicinal chemistry, Jan-15, Volume: 228Affinity-based protein profiling identifies vitamin D3 as a heat shock protein 70 antagonist that regulates hedgehog transduction in murine basal cell carcinoma.
AID95695In vitro inhibition of growth of KB cells (cytotoxic assay).1998Journal of medicinal chemistry, Jan-01, Volume: 41, Issue:1
Structure-activity of novel rhodacyanine dyes as antitumor agents.
AID1824242Inhibition of hedgehog signalling in mouse Sufu-KO MEF cells assessed as reduction in Gli1 mRNA expression measured after 48 hrs by RT-PCR analysis2022European journal of medicinal chemistry, Jan-15, Volume: 228Affinity-based protein profiling identifies vitamin D3 as a heat shock protein 70 antagonist that regulates hedgehog transduction in murine basal cell carcinoma.
AID1056251Half life in mouse liver microsomes at 1 uM incubated for 15 mins prior to beta-NADPH addition by LC-MS/MS analysis2013ACS medicinal chemistry letters, Nov-14, Volume: 4, Issue:11
Analogs of the Allosteric Heat Shock Protein 70 (Hsp70) Inhibitor, MKT-077, as Anti-Cancer Agents.
AID21982The solubility in 0.9% saline was determined1998Journal of medicinal chemistry, Jan-01, Volume: 41, Issue:1
Structure-activity of novel rhodacyanine dyes as antitumor agents.
AID211995Lethal dose when administered intraperitoneally1998Journal of medicinal chemistry, Jan-01, Volume: 41, Issue:1
Structure-activity of novel rhodacyanine dyes as antitumor agents.
AID443970Antileishmanial activity against Leishmania donovani MHOM/ET/67/L82 amastigotes infected in syrian golden hamster spleen after 72 hrs2010Journal of medicinal chemistry, Jan-14, Volume: 53, Issue:1
Fluorinated rhodacyanine (SJL-01) possessing high efficacy for visceral leishmaniasis (VL).
AID211996Lethal dose when administered intravenously1998Journal of medicinal chemistry, Jan-01, Volume: 41, Issue:1
Structure-activity of novel rhodacyanine dyes as antitumor agents.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (47)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's12 (25.53)18.2507
2000's10 (21.28)29.6817
2010's18 (38.30)24.3611
2020's7 (14.89)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 22.31

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.

MetricThis Compound (vs All)
Research Demand Index22.31 (24.57)
Research Supply Index4.03 (2.92)
Research Growth Index4.69 (4.65)
Search Engine Demand Index23.28 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (22.31)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials2 (3.77%)5.53%
Reviews5 (9.43%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other46 (86.79%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]