Biological activity In vitro In vivo References
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I-BET151 (GSK1210151A)

Biological activity In vitro In vivo References
Product Name
I-BET151 (GSK1210151A)
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
Formula Weight
415.44
MOL File
1300031-49-5.mol
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I-BET151 (GSK1210151A) Property

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
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Safety

Hazard Codes 
T
Risk Statements 
25
Safety Statements 
45
RIDADR 
UN 2811 6.1 / PGIII
WGK Germany 
3
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Hazard and Precautionary Statements (GHS)

Symbol(GHS)
Signal word
Danger
Hazard statements

H301Toxic if swalloed

Precautionary statements

P301+P310IF SWALLOWED: Immediately call a POISON CENTER or doctor/physician.

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N-Bromosuccinimide Price

Sigma-Aldrich
Product number
SML0666
Product name
GSK1210151A
Purity
≥98% (HPLC)
Packaging
5mg
Price
$156
Updated
2024/03/01
Sigma-Aldrich
Product number
SML0666
Product name
GSK1210151A
Purity
≥98% (HPLC)
Packaging
25mg
Price
$620
Updated
2024/03/01
Cayman Chemical
Product number
11181
Product name
I-BET151
Purity
≥98%
Packaging
1mg
Price
$36
Updated
2024/03/01
Cayman Chemical
Product number
11181
Product name
I-BET151
Purity
≥98%
Packaging
5mg
Price
$98
Updated
2024/03/01
Cayman Chemical
Product number
11181
Product name
I-BET151
Purity
≥98%
Packaging
10mg
Price
$179
Updated
2024/03/01
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I-BET151 (GSK1210151A) Chemical Properties,Usage,Production

Biological activity

I-BET151 (GSK1210151A) is a novel selective BET inhibitor for BRD2, BRD3 and BRD4 with IC50 of 0.5 μM, 0.25 μM, and 0.79 μM in cell-free assays, respectively.

In vitro

I-BET151 exhibits potent selectivity over an extensive range of diverse protein types such as COX-2, P450, Aurora B, GSK3β, PI3K-γ, GPCR, ion channels, and transporters. Similar to I-BET762 (GSK525762A), I-BET151 displays potent binding affinity to BRD2, BRD3 and BRD4 with KD of 0.02-0.1 μM, and significantly inhibits lipopolysaccharide-stimulated IL-6 cytokine production in human peripheral blood mononuclear cells (PBMC) and whole blood (WB) as well as rat WB with IC50 of 0.16 μM, 1.26 μM, and 1.26 μM, respectively. I-BET151 (0.5 or 5 μM) inhibits the binding of BETs (BRD2, BRD3, BRD4, and BRD9) but not the binding of 23 other bromodomain proteins in HL60 nuclear extract to acetylated histone peptides. I-BET151 has potent efficacy against cell lines harboring different MLL-fusions such as MV4;11, RS4;11, MOLM13, and NOMO1 cells with IC50 of 15-192 nM. Consistently, I-BET151 completely ablates the colony-forming potential of MLL-fusion-driven leukaemias (MOLM13) but not leukaemias driven by tyrosine kinase activation (K562). I-BET151 also displays potent efficacy in both liquid culture and clonogenic assays using primary murine progenitors transformed with either MLL-ENL or MLL-AF9. I-BET151 treatment significantly induces apoptosis and prominent G0/G1 arrest in MLL-fusion cell lines driven by distinct MLL fusions (MOLM13 and MV4;11 containing MLL-AF9 and MLL-AF4, respectively) but not the K562 cells, probably due to the inhibition of transcription of BCL2, C-MYC and CDK6 by blocking the recruitment of BRD3/4, PAFc and SEC components into transcriptional start site (TSS).

In vivo

Administration of I-BET151 at 30 mg/kg/day significantly inhibits tumor growth of murine MLL-AF9 and human MLL-AF4 leukaemia in mice, and provides marked survival benefit.

References

http://www.selleckchem.com/products/i-bet151-gsk1210151a.html

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

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.

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.

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) Preparation Products And Raw materials

Raw materials

Preparation Products

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I-BET151 (GSK1210151A) Suppliers

Canada 1 China 113 India 2 United States 19 Global 135
AdooQ BioScience, LLC
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+1 (866) 930-6790
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+1 (866) 333-9607
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info@adooq.com
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Target molecule Corp.
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857-239-0968
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857-239-8801
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service1@targetmol.com
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Musechem
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+1-800-259-7612
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TargetMol Chemicals Inc.
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+1-781-999-5354 +1-00000000000
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marketing@targetmol.com
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InvivoChem
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sales@invivochem.cn
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Cckinase, Inc.
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+1 (732)236-3202
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sales@cckinase.com
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BOC Sciences
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+1-631-485-4226
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1-631-614-7828
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inquiry@bocsci.com
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Aladdin Scientific
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View Lastest Price from I-BET151 (GSK1210151A) manufacturers

Career Henan Chemical Co
Product
I-BET151 (GSK1210151A) 1300031-49-5
Price
US $1.00/g
Min. Order
1g
Purity
99%
Supply Ability
200kg
Release date
2020-01-10
Career Henan Chemical Co
Product
7Methyl-5-(1-{[3-(trifluoroMethyl)phenyl]acetyl}-2,3-dihydro1Hindol-5-yl)7Hpyrrolo[2,3d]pyriMidin-4-aMine 1300031-49-5
Price
US $1.00/g
Min. Order
1g
Purity
99%
Supply Ability
200kg
Release date
2020-01-10
Career Henan Chemical Co
Product
7Methyl-5-(1-{[3-(trifluoroMethyl)phenyl]acetyl}-2,3-dihydro1Hindol-5-yl)7Hpyrrolo[2,3d]pyriMidin-4-aMine 1300031-49-5
Price
US $1.00/g
Min. Order
1g
Purity
99%
Supply Ability
200kg
Release date
2020-01-10

1300031-49-5, I-BET151 (GSK1210151A)Related Search:

GSK 525762A Bortezomib (+)-JQ1 CPI-203 OTX015 (1S,4Z,7S,10S,11E,20R)-4-ethylidene-7,20-dipropan-2-yl-9-oxa-15,16-dit hia-3,6,18,21-tetrazabicyclo[8.7.6]tricos-11-ene-2,5,8,19,22-pentone Carfilzomib

  • 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