Page last updated: 2024-11-13

cblc137

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

Description

CBLC137: a FACT histone chaperone inhibitor with antineoplastic activity; structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

CBL0137 : A member of the class of carbazoles that is 9H-carbazole which is substituted by acetyl groups at positions 3 and 6, and by a 2-isopropylethyl group on the nitrogen atom (position 9). It is a modulator of histone chaperone FACT (FAcilitates Chromatin Transcription) - interaction of CBL0137 with the FACT complex results in simultaneous NF-kappa beta suppression, Heat Shock Transcription Factor 1 (HSF1) suppression and p53 activation - and shows antitumour effects in animal models of various cancers. [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 SourceID
PubMed CID44519124
CHEMBL ID4640631
CHEBI ID138650
SCHEMBL ID2361265
MeSH IDM000609020

Synonyms (37)

Synonym
CHEBI:138650
curaxin-137
1197996-80-7
1,1'-{9-[2-(propan-2-ylamino)ethyl]-9h-carbazole-3,6-diyl}diethanone
1,1'-{9-[2-(isopropylamino)ethyl]-9h-carbazole-3,6-diyl}diethanone
3,6-diacetyl-9-(2-isopropylethyl)-9h-carbazole
cbl0137
cbl-0137 free base
AKOS016012947
cbl-0137
8xkr07h9er ,
unii-8xkr07h9er
JKCSODVERGVDLT-UHFFFAOYSA-N
SCHEMBL2361265
1,1'-(9-(2-(isopropylamino)ethyl)-9h-carbazole-3,6-diyl)diethanone
cbl 137; curaxin 137
DTXSID10152589
1,1'-(9-(2-(isopropylamino)ethyl)-9h-carbazole-3,6-diyl)bis(ethan-1-one)
cblc137
curaxin 137
cbl-0137; cbl 0137; curaxin 137
BCP29977
SB17204
cbl 0137
Q27271162
1-[6-acetyl-9-[2-(propan-2-ylamino)ethyl]carbazol-3-yl]ethanone
EX-A4237
1-[6-acetyl-9-[2-(isopropylamino)ethyl]carbazol-3-yl]ethanone
nsc-789040
nsc789040
bdbm50544058
ethanone, 1,1'-[9-[2-[(1-methylethyl)amino]ethyl]-9h-carbazole-3,6-diyl]bis-
BC165662
CHEMBL4640631 ,
CS-0014629
HY-18935
F78005

Research Excerpts

Dosage Studied

ExcerptRelevanceReference
" In vivo, we implanted the cells orthotopically in nude mice and administered CBL0137 in various dosing regimens to assess brain and tumor accumulation of CBL0137, its effect on tumor cell proliferation and apoptosis, and on survival of mice with and without temozolomide (TMZ)."( Anticancer drug candidate CBL0137, which inhibits histone chaperone FACT, is efficacious in preclinical orthotopic models of temozolomide-responsive and -resistant glioblastoma.
Barone, TA; Burkhart, CA; Gudkov, AV; Gurova, KV; Haderski, G; Plunkett, RJ; Purmal, AA; Safina, A, 2017
)
0.46
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Roles (4)

RoleDescription
NF-kappaB inhibitorAn inhibitor of NF-kappaB (nuclear factor kappa-light-chain-enhancer of activated B cells), a protein complex involved in the transcription of DNA.
p53 activatorAny activator of tumour protein p53.
antineoplastic agentA substance that inhibits or prevents the proliferation of neoplasms.
apoptosis inducerAny substance that induces the process of apoptosis (programmed cell death) in multi-celled organisms.
[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 (5)

ClassDescription
carbazoles
secondary amino compoundA compound formally derived from ammonia by replacing two hydrogen atoms by organyl groups.
tertiary amino compoundA compound formally derived from ammonia by replacing three hydrogen atoms by organyl groups.
aromatic ketoneA ketone in which the carbonyl group is attached to an aromatic ring.
methyl ketoneA ketone of formula RC(=O)CH3 (R =/= H).
[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 (3)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
PPM1D proteinHomo sapiens (human)Potency1.47400.00529.466132.9993AID1347411
Interferon betaHomo sapiens (human)Potency1.47400.00339.158239.8107AID1347411
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
DNA (cytosine-5)-methyltransferase 3AMus musculus (house mouse)IC50 (µMol)7.00005.00007.00009.0000AID1664312; AID1664313
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Activation Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
DNA (cytosine-5)-methyltransferase 3AMus musculus (house mouse)Kd1.30000.90001.30001.7000AID1664314; AID1664315; AID1664316; AID1664317; AID1664318; AID1664319
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (30)

Processvia Protein(s)Taxonomy
cell surface receptor signaling pathway via JAK-STATInterferon betaHomo sapiens (human)
response to exogenous dsRNAInterferon betaHomo sapiens (human)
B cell activation involved in immune responseInterferon betaHomo sapiens (human)
cell surface receptor signaling pathwayInterferon betaHomo sapiens (human)
cell surface receptor signaling pathway via JAK-STATInterferon betaHomo sapiens (human)
response to virusInterferon betaHomo sapiens (human)
positive regulation of autophagyInterferon betaHomo sapiens (human)
cytokine-mediated signaling pathwayInterferon betaHomo sapiens (human)
natural killer cell activationInterferon betaHomo sapiens (human)
positive regulation of peptidyl-serine phosphorylation of STAT proteinInterferon betaHomo sapiens (human)
cellular response to interferon-betaInterferon betaHomo sapiens (human)
B cell proliferationInterferon betaHomo sapiens (human)
negative regulation of viral genome replicationInterferon betaHomo sapiens (human)
innate immune responseInterferon betaHomo sapiens (human)
positive regulation of innate immune responseInterferon betaHomo sapiens (human)
regulation of MHC class I biosynthetic processInterferon betaHomo sapiens (human)
negative regulation of T cell differentiationInterferon betaHomo sapiens (human)
positive regulation of transcription by RNA polymerase IIInterferon betaHomo sapiens (human)
defense response to virusInterferon betaHomo sapiens (human)
type I interferon-mediated signaling pathwayInterferon betaHomo sapiens (human)
neuron cellular homeostasisInterferon betaHomo sapiens (human)
cellular response to exogenous dsRNAInterferon betaHomo sapiens (human)
cellular response to virusInterferon betaHomo sapiens (human)
negative regulation of Lewy body formationInterferon betaHomo sapiens (human)
negative regulation of T-helper 2 cell cytokine productionInterferon betaHomo sapiens (human)
positive regulation of apoptotic signaling pathwayInterferon betaHomo sapiens (human)
response to exogenous dsRNAInterferon betaHomo sapiens (human)
B cell differentiationInterferon betaHomo sapiens (human)
natural killer cell activation involved in immune responseInterferon betaHomo sapiens (human)
adaptive immune responseInterferon betaHomo sapiens (human)
T cell activation involved in immune responseInterferon betaHomo sapiens (human)
humoral immune responseInterferon betaHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (6)

Processvia Protein(s)Taxonomy
DNA (cytosine-5-)-methyltransferase activity, acting on CpN substratesDNA (cytosine-5)-methyltransferase 3AMus musculus (house mouse)
cytokine activityInterferon betaHomo sapiens (human)
cytokine receptor bindingInterferon betaHomo sapiens (human)
type I interferon receptor bindingInterferon betaHomo sapiens (human)
protein bindingInterferon betaHomo sapiens (human)
chloramphenicol O-acetyltransferase activityInterferon betaHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (3)

Processvia Protein(s)Taxonomy
nucleoplasmDNA (cytosine-5)-methyltransferase 3AMus musculus (house mouse)
extracellular spaceInterferon betaHomo sapiens (human)
extracellular regionInterferon betaHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (17)

Assay IDTitleYearJournalArticle
AID1347412qHTS assay to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: Counter screen cell viability and HiBit confirmation2020ACS chemical biology, 07-17, Volume: 15, Issue:7
High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle.
AID1347414qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: Secondary screen by immunofluorescence2020ACS chemical biology, 07-17, Volume: 15, Issue:7
High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle.
AID1347411qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS Mechanism Interrogation Plate v5.0 (MIPE) Libary2020ACS chemical biology, 07-17, Volume: 15, Issue:7
High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle.
AID1347415qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: tertiary screen by RT-qPCR2020ACS chemical biology, 07-17, Volume: 15, Issue:7
High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle.
AID1664316Binding affinity to murine DNMT3A catalytic domain assessed as enzyme-DNA complex formation at 30 uM using 30-mer duplex DNA (17 AT bp) as substrate preincubated for 30 mins followed by enzyme addition by fluorescence polarization assay (Rvb = 0.9 +/- 0.12020Bioorganic & medicinal chemistry letters, 08-15, Volume: 30, Issue:16
Novel anticancer drug curaxin CBL0137 impairs DNA methylation by eukaryotic DNA methyltransferase Dnmt3a.
AID1664311Binding affinity to 5'-6FAM-tagged 30-mer duplex DNA (22 AT bp) (unknown origin) assessed as dissociation constant for complound-DNA complex by fluorescence polarization assay2020Bioorganic & medicinal chemistry letters, 08-15, Volume: 30, Issue:16
Novel anticancer drug curaxin CBL0137 impairs DNA methylation by eukaryotic DNA methyltransferase Dnmt3a.
AID1664324Inhibition of murine DNMT3A catalytic domain-mediated DNA methylation using 5'-6FAM-tagged 30-mer duplex DNA (22 AT bp) as substrate at 60 uM preincubated for 30 mins followed by enzyme addition relative to control2020Bioorganic & medicinal chemistry letters, 08-15, Volume: 30, Issue:16
Novel anticancer drug curaxin CBL0137 impairs DNA methylation by eukaryotic DNA methyltransferase Dnmt3a.
AID1664317Binding affinity to murine DNMT3A catalytic domain assessed as enzyme-DNA complex formation at 5 uM using 30-mer duplex DNA (22 AT bp) as substrate preincubated for 30 mins followed by enzyme addition by fluorescence polarization assay (Rvb = 0.4 +/- 0.1 2020Bioorganic & medicinal chemistry letters, 08-15, Volume: 30, Issue:16
Novel anticancer drug curaxin CBL0137 impairs DNA methylation by eukaryotic DNA methyltransferase Dnmt3a.
AID1664315Binding affinity to murine DNMT3A catalytic domain assessed as enzyme-DNA complex formation at 15 uM using 30-mer duplex DNA (17 AT bp) as substrate preincubated for 30 mins followed by enzyme addition by fluorescence polarization assay (Rvb = 0.9 +/- 0.12020Bioorganic & medicinal chemistry letters, 08-15, Volume: 30, Issue:16
Novel anticancer drug curaxin CBL0137 impairs DNA methylation by eukaryotic DNA methyltransferase Dnmt3a.
AID1664313Inhibition of murine DNMT3A catalytic domain-mediated DNA methylation using 5'-6FAM-tagged 30-mer duplex DNA (22 AT bp) as substrate preincubated for 30 mins followed by enzyme addition2020Bioorganic & medicinal chemistry letters, 08-15, Volume: 30, Issue:16
Novel anticancer drug curaxin CBL0137 impairs DNA methylation by eukaryotic DNA methyltransferase Dnmt3a.
AID1664323Inhibition of murine DNMT3A catalytic domain-mediated DNA methylation using 5'-6FAM-tagged 30-mer duplex DNA (17 AT bp) as substrate at 60 uM preincubated for 30 mins followed by enzyme addition relative to control2020Bioorganic & medicinal chemistry letters, 08-15, Volume: 30, Issue:16
Novel anticancer drug curaxin CBL0137 impairs DNA methylation by eukaryotic DNA methyltransferase Dnmt3a.
AID1664314Binding affinity to murine DNMT3A catalytic domain assessed as enzyme-DNA complex formation at 5 uM using 30-mer duplex DNA (17 AT bp) as substrate preincubated for 30 mins followed by enzyme addition by fluorescence polarization assay (Rvb = 0.9 +/- 0.1 2020Bioorganic & medicinal chemistry letters, 08-15, Volume: 30, Issue:16
Novel anticancer drug curaxin CBL0137 impairs DNA methylation by eukaryotic DNA methyltransferase Dnmt3a.
AID1664318Binding affinity to murine DNMT3A catalytic domain assessed as enzyme-DNA complex formation at 15 uM using 30-mer duplex DNA (22 AT bp) as substrate preincubated for 30 mins followed by enzyme addition by fluorescence polarization assay (Rvb = 0.4 +/- 0.12020Bioorganic & medicinal chemistry letters, 08-15, Volume: 30, Issue:16
Novel anticancer drug curaxin CBL0137 impairs DNA methylation by eukaryotic DNA methyltransferase Dnmt3a.
AID1664319Binding affinity to murine DNMT3A catalytic domain assessed as enzyme-DNA complex formation at 30 uM using 30-mer duplex DNA (22 AT bp) as substrate preincubated for 30 mins followed by enzyme addition by fluorescence polarization assay (Rvb = 0.4 +/- 0.12020Bioorganic & medicinal chemistry letters, 08-15, Volume: 30, Issue:16
Novel anticancer drug curaxin CBL0137 impairs DNA methylation by eukaryotic DNA methyltransferase Dnmt3a.
AID1664312Inhibition of murine DNMT3A catalytic domain-mediated DNA methylation using 5'-6FAM-tagged 30-mer duplex DNA (17 AT bp) as substrate preincubated for 30 mins followed by enzyme addition2020Bioorganic & medicinal chemistry letters, 08-15, Volume: 30, Issue:16
Novel anticancer drug curaxin CBL0137 impairs DNA methylation by eukaryotic DNA methyltransferase Dnmt3a.
AID1664322Binding affinity to murine DNMT3A catalytic domain assessed as fold reduction in compound fluorescence at 5 uM by dialysis method relative to control2020Bioorganic & medicinal chemistry letters, 08-15, Volume: 30, Issue:16
Novel anticancer drug curaxin CBL0137 impairs DNA methylation by eukaryotic DNA methyltransferase Dnmt3a.
AID1664310Binding affinity to 5'-6FAM-tagged 30-mer duplex DNA (17 AT bp) (unknown origin) assessed as dissociation constant for complound-DNA complex by fluorescence polarization assay2020Bioorganic & medicinal chemistry letters, 08-15, Volume: 30, Issue:16
Novel anticancer drug curaxin CBL0137 impairs DNA methylation by eukaryotic DNA methyltransferase Dnmt3a.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (39)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's0 (0.00)29.6817
2010's13 (33.33)24.3611
2020's26 (66.67)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 11.05

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.

MetricThis Compound (vs All)
Research Demand Index11.05 (24.57)
Research Supply Index3.69 (2.92)
Research Growth Index4.74 (4.65)
Search Engine Demand Index0.00 (26.88)
Search Engine Supply Index0.00 (0.95)

This Compound (11.05)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials0 (0.00%)5.53%
Reviews0 (0.00%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other39 (100.00%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]