I-BET151 (GSK1210151A)
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- 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, 10 mM in DMSO;GSK1210151A/1300031-49-5/98%
- CBNumber:
- CB92554258
- Summenformel:
- C23H21N5O3
- Molgewicht:
- 415.44
- MOL-Datei:
- 1300031-49-5.mol
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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
- InChI
- InChI=1S/C23H21N5O3/c1-12-21(14(3)31-27-12)16-9-18-15(10-20(16)30-4)22-19(11-25-18)26-23(29)28(22)13(2)17-7-5-6-8-24-17/h5-11,13H,1-4H3,(H,26,29)/t13-/m1/s1
- InChIKey
- VUVUVNZRUGEAHB-CYBMUJFWSA-N
- SMILES
- N1C2C(=CC(OC)=C(C3=C(C)ON=C3C)C=2)C2N([C@@H](C3=NC=CC=C3)C)C(=O)NC=2C=1
Sicherheit
- Risiko- und Sicherheitserkl?rung
- Gefahreninformationscode (GHS)
| Kennzeichnung gef?hrlicher |
T |
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| R-S?tze: |
25 |
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| S-S?tze: |
45 |
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| RIDADR |
UN 2811 6.1 / PGIII |
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| WGK Germany |
3 |
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| Speicherklasse |
6.1C - Combustible acute toxic Cat.3
toxic compounds or compounds which causing chronic effects |
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| Hazard Classifications |
Acute Tox. 3 Oral |
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| Bildanzeige (GHS) |
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| Alarmwort |
Achtung
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| Gefahrenhinweise |
| Code |
Gefahrenhinweise |
Gefahrenklasse |
Abteilung |
Alarmwort |
Symbol |
P-Code |
| H301 |
Giftig bei Verschlucken. |
Akute Toxizit?t oral |
Kategorie 3 |
Achtung |
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P264, P270, P301+P310, P321, P330,P405, P501 |
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| Sicherheit |
| P301+P310 |
BEI VERSCHLUCKEN: Sofort GIFTINFORMATIONSZENTRUM/Arzt/... (geeignete Stelle für medizinische Notfallversorgung vom Hersteller/Lieferanten anzugeben) anrufen. |
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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 IC
50 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 G
0/G
1 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
Downstream Produkte
I-BET151 (GSK1210151A) Anbieter Lieferant Produzent Hersteller Vertrieb H?ndler.
Global( 164)Lieferanten
- 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
- I-BET151, 10 mM in DMSO
- GSK1210151A/1300031-49-5/98%
- I-BET151 (GSK1210151A) ，S2780
- (r)-7-(3,5-dimethylisoxazol-4-yl)-8-methoxy-1-(1-(pyridin-2-yl)ethyl)-1,3-dihydro-2h-imidazo[4,5-c]quinolin-2-one
- 1300031-49-5
- 300031-49-5
- Inhibitors
