I-BET151 (GSK1210151A)

Bezeichnung:I-BET151 (GSK1210151A)

CAS-Nr1300031-49-5

Englisch Name:I-BET151 (GSK1210151A)

CBNumberCB92554258

SummenformelC23H21N5O3

Molgewicht415.44

MOL-Datei1300031-49-5.mol

I-BET151 (GSK1210151A) physikalisch-chemischer Eigenschaften

Dichte	1.314
storage temp.	2-8°C
Löslichkeit	DMSO: soluble20mg/mL, clear
Aggregatzustand	powder
pka	11.14±0.20(Predicted)
Farbe	white to beige

Sicherheit

Kennzeichnung gefährlicher	T
R-Sätze:	25
S-Sätze:	45
RIDADR	UN 2811 6.1 / PGIII
WGK Germany	3

Gefahreninformationscode (GHS)

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
GSK1210151A or I-BET151 has been used to study its inhibitory effect on BET (bromodomain and extra terminal) recruitment to chromatin in treating MLL (mixed-lineage leukemia)-fusion leukemia.
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.
Definition
ChEBI: 7-(3,5-dimethyl-4-isoxazolyl)-8-methoxy-1-[(1R)-1-(2-pyridinyl)ethyl]-3H-imidazo[4,5-c]quinolin-2-one is an imidazoquinoline.
Biochem/physiol Actions
GSK1210151A (I-BET151) is an inhibitor of the BET (bromodomain and extra terminal domain protein) family of acetyl-lysine recognizing, chromatin ′adaptor′ proteins. GSK1210151A displaces BRD3 and BRD4, PAFc and SEC components from chromatin resulting in inhibition of transcription at key genes (BCL2, C-MYC and CDK6) involved in the initiation of mixed lineage leukemia (MLL). GSK1210151A (I-BET151) showed good efficacy in 2 MLL animal models.
target
BRD2

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

I-BET151 (GSK1210151A) Anbieter Lieferant Produzent Hersteller Vertrieb Händler.

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