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I-BET151 (GSK1210151A)

I-BET151 (GSK1210151A) Struktur
1300031-49-5
CAS-Nr.
1300031-49-5
Englisch Name:
I-BET151 (GSK1210151A)
Synonyma:
CS-358;CS-1920;I-BET 151;GSK 1210151A;I-BET151, >=98%;GSK1210151A ISOMER;GSK1210151A (I-BET151);I-BET 151/GSK 1210151A;I-BET151 (GSK1210151A) USP/EP/BP;I-BET151, pan-BET family inhibitor
CBNumber:
CB92554258
Summenformel:
C23H21N5O3
Molgewicht:
415.44
MOL-Datei:
1300031-49-5.mol

I-BET151 (GSK1210151A) Eigenschaften

Dichte
1.314
storage temp. 
2-8°C
L?slichkeit
DMSO: soluble20mg/mL, clear
Aggregatzustand
powder
pka
11.14±0.20(Predicted)
Farbe
white to beige
Sicherheit
  • Risiko- und Sicherheitserkl?rung
  • Gefahreninformationscode (GHS)
Kennzeichnung gef?hrlicher T
R-S?tze: 25
S-S?tze: 45
RIDADR  UN 2811 6.1 / PGIII
WGK Germany  3
Bildanzeige (GHS) GHS hazard pictograms
Alarmwort Achtung
Gefahrenhinweise
Code Gefahrenhinweise Gefahrenklasse Abteilung Alarmwort Symbol P-Code
H301 Giftig bei Verschlucken. Akute Toxizit?t oral Kategorie 3 Achtung GHS hazard pictogramssrc="/GHS06.jpg" width="20" height="20" /> P264, P270, P301+P310, P321, P330,P405, P501
Sicherheit
P301+P310 BEI VERSCHLUCKEN: Sofort GIFTINFORMATIONSZENTRUM/Arzt/... (geeignete Stelle für medizinische Notfallversorgung vom Hersteller/Lieferanten anzugeben) anrufen.

I-BET151 (GSK1210151A) Chemische Eigenschaften,Einsatz,Produktion Methoden

Beschreibung

The bromodomain and extra terminal domain (BET) family of proteins including BRD2, BRD3, and BRD4 play a key role in many cellular processes, including inflammatory gene expression, mitosis, and viral/host interaction by controlling the assembly of histone acetylation-dependent chromatin complexes. I-BET151 is an isoxazole class pan-BET family inhibitor, blocking BRD2, BRD3, and BRD4 with IC50 values of 0.5, 0.25, and 0.79 μM, respectively. Through this action, it blocks the growth of leukemic cell lines driven by mixed lineage leukemia (MLL) fusions at nanomolar concentrations, whereas tyrosine kinase activated cells were much less sensitive. Specifically, I-BET151 induces apoptosis via reduced expression of BCL2 or triggers G0/G1 cell cycle arrest in MLL-fusion cell lines. I-BET151 is effective in vivo, suppressing MLL leukemia progression in two different mouse models.

Chemische Eigenschaften

Off-White Solid

Verwenden

I-BET 151 is part of a novel series of quinoline isoxazole BET family bromodomain inhibitors, a family of four proteins that selectively bind to aceylated lysine residues in histone. I-BET 151 play ke y roles in many cellular processes, including anti-inflammatory gene expression, mitosis, and viral/host interaction by controlling the conformation of histone acetylation -dependent chromatin complex es. Studies have shown that I-BET 151 increased ApoA1 expression within the nanomolar range in human hepatic cell line HepG2. The upregulation by I-BET 151 suggested potential anti-inflammatory activi ties upon administration.

I-BET151 (GSK1210151A) Upstream-Materialien And Downstream Produkte

Upstream-Materialien

GSK1210151A S isomer 7-(3,5-dimethylisoxazol-4-yl)-8-methoxy-1-(1-(pyridin-2-yl)ethyl)-1H-imidazo[4,5-c]quinolin-2(3H)-one [3-(3,5-diMethyl-4-isoxazolyl)-4-(Methyloxy)phenyl]aMine 3,5-Dimethylisoxazole-4-boronic acid 4-(2-methoxy-5-nitrophenyl)-3,5-dimethylisoxazole diethyl 2-((3-(3,5-dimethylisoxazol-4-yl)-4-methoxyphenylamino)methylene)malonate 4-chloro-7-(3,5-dimethylisoxazol-4-yl)-6-methoxyquinoline-3-carboxamide 3-QuinolinecarboxaMide, 7-(3,5-diMethyl-4-isoxazolyl)-6-Methoxy-4-[[(1R)-1-(2-pyridinyl)ethyl]aMino]- 2-Iodo-4-nitroanisole

Downstream Produkte

I-BET151 (GSK1210151A) Anbieter Lieferant Produzent Hersteller Vertrieb H?ndler.

Global( 136)Lieferanten
Firmenname Telefon E-Mail Land Produktkatalog Edge Rate
ATK CHEMICAL COMPANY LIMITED 		+undefined-21-51877795
ivan@atkchemical.com China 32956 60
Biochempartner 		0086-13720134139
candy@biochempartner.com CHINA 965 58
Hubei Jusheng Technology Co.,Ltd. 		18871490254
linda@hubeijusheng.com CHINA 28172 58
BOC Sciences 		+1-631-485-4226
inquiry@bocsci.com United States 19553 58
CONIER CHEM AND PHARMA LIMITED 		+8618523575427
 sales@conier.com China 49374 58
career henan chemical co 		+86-0371-86658258 +8613203830695
 factory@coreychem.com China 29810 58
TargetMol Chemicals Inc. 		+1-781-999-5354 +1-00000000000
 marketing@targetmol.com United States 32161 58
HANGZHOU CLAP TECHNOLOGY CO.,LTD 		86-571-88216897,88216896 13588875226
 sales@hzclap.com CHINA 6312 58
Dideu Industries Group Limited 		+86-29-89586680 +86-15129568250
 1026@dideu.com China 22787 58
Dayang Chem (Hangzhou) Co.,Ltd. 		571-88938639 +8617705817739
 info@dycnchem.com China 52849 58
  • 7-(3,5-Dimethyl-4-isoxazolyl)-1,3-dihydro-8-methoxy-1-[(1R)-1-(2-pyridinyl)ethyl]-2H-imidazo[4,5-c]quinolin-2-one
  • I-BET 151/GSK 1210151A
  • GSK1210151A (I-BET151)
  • 7-(3,5-diMethylisoxazol-4-yl)-8-Methoxy-1-((R)-1-(pyridin-2-yl)ethyl)-1H-iMidazo[4,5-c]quinolin-2(3H)-one
  • 7-(3,5-Dimethylisoxazol-4-yl)-8-methoxy-1-((R)-1-(pyridin-2-yl)ethyl)-1H-imidazo[4,5-c]quinolin-2
  • GSK 1210151A
  • I-BET 151
  • 7-(3,5-Dimethyl-4-isoxazolyl)-1,3-dihydro-8-methoxy-1-[(1R)-1-(2-pyridinyl)ethyl]-2H-imidazo[4,5-c]quinolin-2-one I-BET151(GSK1210151A)
  • 7-(3,5-Dimethyl-4-isoxazolyl)-8-(methyloxy)-1-[(1R)-1-(2-pyridinyl)ethyl]-1,3-dihydro-2H-imidazo[4,5-c]quinolin-2-one
  • I-BET151, >=98%
  • 7-(3,5-Dimethylisoxazol-4-yl)-8-methoxy-1-((R)-1-(pyridin-2-yl)ethyl)-1H-imidazo[4,5-c]quinoli
  • GSK1210151A ISOMER
  • 7-(3,5-DIMETHYL-1,2-OXAZOL-4-YL)-8-METHOXY-1-[(1R)-1-PYRIDIN-2-YLETHYL]-3H-IMIDAZO[4,5-C]QUINOLIN-2-ONE
  • CS-1920
  • IBET151;I-BET-151;I BET 151;IBET-151;IBET 151
  • CS-358
  • GSK-1210151A;IBET151;I-BET-151;I BET 151;IBET-151;IBET 151;GSK 1210151A
  • 2H-Imidazo[4,5-c]quinolin-2-one, 7-(3,5-dimethyl-4-isoxazolyl)-1,3-dihydro-8-methoxy-1-[(1R)-1-(2-pyridinyl)ethyl]-
  • I-BET151 (GSK1210151A) USP/EP/BP
  • I-BET151, pan-BET family inhibitor
  • 1300031-49-5
  • 300031-49-5
  • Inhibitors
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