ChemicalBook > CAS DataBase List > 1,1'-(9-(2-(isopropylamino)ethyl)-9H-carbazole-3,6-diyl)bis(ethan-1-one)

1,1'-(9-(2-(isopropylamino)ethyl)-9H-carbazole-3,6-diyl)bis(ethan-1-one)

Product Name
1,1'-(9-(2-(isopropylamino)ethyl)-9H-carbazole-3,6-diyl)bis(ethan-1-one)
CAS No.
1197996-80-7
Chemical Name
1,1'-(9-(2-(isopropylamino)ethyl)-9H-carbazole-3,6-diyl)bis(ethan-1-one)
Synonyms
CBL0137;Curaxin;CBLC 137;Curaxin 137;Ep300/CREBBP-IN-8;CBL0137, 10 mM in DMSO;CBL0137; CBL-0137; CBL 0137; CURAXIN;1-[6-acetyl-9-[2-(propan-2-ylamino)ethyl]carbazol-3-yl]ethanone;1,1'-(9-(2-(isopropylamino)ethyl)-9H-carbazole-3,6-diyl)bis(ethan-1-one);Ethanone, 1,1'-[9-[2-[(1-methylethyl)amino]ethyl]-9H-carbazole-3,6-diyl]bis-
CBNumber
CB83133464
Molecular Formula
C21H24N2O2
Formula Weight
336.43
MOL File
1197996-80-7.mol
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1,1'-(9-(2-(isopropylamino)ethyl)-9H-carbazole-3,6-diyl)bis(ethan-1-one) Property

storage temp. 
Store at -20°C
solubility 
≤ 2 mg/mL in ethanol; 5 mg/mL in DMSO; 5mg/mL in dimethyl formamide
form 
crystalline solid
color 
Off-white to light yellow
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Hazard and Precautionary Statements (GHS)

Symbol(GHS)
Signal word
Warning
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N-Bromosuccinimide Price

Cayman Chemical
Product number
19110
Product name
CBL0137
Purity
≥95%
Packaging
1mg
Price
$47
Updated
2024/03/01
Cayman Chemical
Product number
19110
Product name
CBL0137
Purity
≥95%
Packaging
5mg
Price
$160
Updated
2024/03/01
Cayman Chemical
Product number
19110
Product name
CBL0137
Purity
≥95%
Packaging
10mg
Price
$295
Updated
2024/03/01
AK Scientific
Product number
3372DF
Product name
CBL-0137freebase
Packaging
25mg
Price
$455
Updated
2021/12/16
ApexBio Technology
Product number
C3171
Product name
CBL0137
Packaging
1mg
Price
$123
Updated
2021/12/16
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1,1'-(9-(2-(isopropylamino)ethyl)-9H-carbazole-3,6-diyl)bis(ethan-1-one) Chemical Properties,Usage,Production

Uses

Curaxin-137 is an inhibitor of the histone chaperone FACT (facilitates chromatin transcription) that simultaneously suppresses NF-κB and activates p53.

Definition

ChEBI: CBL0137 is 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. It has a role as a NF-kappaB inhibitor, a p53 activator, an antineoplastic agent and an apoptosis inducer. It is a member of carbazoles, a secondary amino compound, a tertiary amino compound, an aromatic ketone and a methyl ketone.

Biological Activity

ec50: 0.37 μm for activating p53; 0.47 μm for inhibiting nf-κbcbl0137 is a curaxin that activates p53 and inhibits nf-κb.the p53 and nuclear factor κb (nf-κb) pathways are dysregulated in almost all tumors, making them attractive targets for therapeutic activation and inhibition, respectively.

in vitro

cbl0137 was identified as a metabolically stable curaxin activating p53 and inhibiting nf-κb. cbl0137 could functionally inactivate chromatin transcription complex, resulting in the effects on p53 and nf-κb and promoting cancer cell death [1]. it was also found that cbl0137 alone was a potent inducer of apoptosis in pancreatic cancer cell lines and was toxic not only for proliferating bulk tumor cells, but also for pancreatic cancer stem cells [2].

in vivo

in mice, cbl0137 was effective against orthotopic gemcitabine resistant panc-1 model and patient derived xenografts, in which cbl0137 anti-tumor effect related with overexpression of fact. moreover, the combination effects of cbl0137 and gemcitabine might be explained by the ability of cbl0137 to inhibit several transcriptional programs induced by gemcitabine, including nf-kappab response and expression of ribonucleotide reductase [2].

References

1. a. v. gasparian, c. a. burkhart, a. a. purmal, et al. curaxins: anticancer compounds that simultaneously suppress nf-κb and activate p53 by targeting fact. sci.transl.med. 3(95), (2011).2. c. burkhart, d. fleyshman, r. kohrn, et al. curaxin cbl0137 eradicates drug resistant cancer stem cells and potentiates efficacy of gemcitabine in preclinical models of pancreatic cancer. oncotarget 5(22), 11038-11053 (2014).

1,1'-(9-(2-(isopropylamino)ethyl)-9H-carbazole-3,6-diyl)bis(ethan-1-one) Preparation Products And Raw materials

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View Lastest Price from 1,1'-(9-(2-(isopropylamino)ethyl)-9H-carbazole-3,6-diyl)bis(ethan-1-one) manufacturers

Henan Aochuang Chemical Co.,Ltd.
Product
1,1'-(9-(2-(isopropylamino)ethyl)-9H-carbazole-3,6-diyl)bis(ethan-1-one) 1197996-80-7
Price
US $0.00-0.00/kg
Min. Order
1kg
Purity
98%
Supply Ability
1Ton
Release date
2022-09-22
Career Henan Chemical Co
Product
1,1'-(9-(2-(isopropylamino)ethyl)-9H-carbazole-3,6-diyl)bis(ethan-1-one) 1197996-80-7
Price
US $1.00/g
Min. Order
1g
Purity
99.99%
Supply Ability
200kg
Release date
2019-12-24

1197996-80-7, 1,1'-(9-(2-(isopropylamino)ethyl)-9H-carbazole-3,6-diyl)bis(ethan-1-one)Related Search:


  • 1,1'-(9-(2-(isopropylamino)ethyl)-9H-carbazole-3,6-diyl)bis(ethan-1-one)
  • CBL0137
  • CBL0137; CBL-0137; CBL 0137; CURAXIN
  • Curaxin
  • CBLC 137
  • Curaxin 137
  • Ethanone, 1,1'-[9-[2-[(1-methylethyl)amino]ethyl]-9H-carbazole-3,6-diyl]bis-
  • 1-[6-acetyl-9-[2-(propan-2-ylamino)ethyl]carbazol-3-yl]ethanone
  • Ep300/CREBBP-IN-8
  • CBL0137, 10 mM in DMSO
  • 1197996-80-7
  • API