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I-BET151 (GSK1210151A)

I-BET151 (GSK1210151A) Structure
CAS No.
1300031-49-5
Chemical Name:
I-BET151 (GSK1210151A)
Synonyms
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;IBET151;I-BET-151;I BET 151;IBET-151;IBET 151
CBNumber:
CB92554258
Molecular Formula:
C23H21N5O3
Molecular Weight:
415.44
MOL File:
1300031-49-5.mol
Modify Date:
2023/6/8 9:01:59

I-BET151 (GSK1210151A) Properties

Density 1.314
storage temp. 2-8°C
solubility DMSO: soluble20mg/mL, clear
form powder
pka 11.14±0.20(Predicted)
color white to beige

SAFETY

Risk and Safety Statements

Symbol(GHS) 
GHS06
Signal word  Danger
Hazard statements  H301
Precautionary statements  P301+P310
Hazard Codes  T
Risk Statements  25
Safety Statements  45
RIDADR  UN 2811 6.1 / PGIII
WGK Germany  3
NFPA 704
0
2 0

I-BET151 (GSK1210151A) price More Price(2)

Manufacturer Product number Product description CAS number Packaging Price Updated Buy
Sigma-Aldrich(India) SML0666 GSK1210151A ≥98% (HPLC) 1300031-49-5 5MG ₹15403.98 2022-06-14 Buy
Sigma-Aldrich(India) SML0666 GSK1210151A ≥98% (HPLC) 1300031-49-5 25MG ₹62633.45 2022-06-14 Buy
Product number Packaging Price Buy
SML0666 5MG ₹15403.98 Buy
SML0666 25MG ₹62633.45 Buy

I-BET151 (GSK1210151A) Chemical Properties,Uses,Production

Description

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.

Chemical Properties

Off-White Solid

Uses

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.

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I-BET151 (GSK1210151A) Spectrum

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 1300031-49-5 300031-49-5 Inhibitors