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I-BET151 (GSK1210151A)

I-BET151 (GSK1210151A) Structure
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
MDL Number:
MFCD22124472
MOL File:
1300031-49-5.mol
Last updated:2023-06-08 09:01:59
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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)  GHS hazard pictograms
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(30)

Manufacturer Product number Product description CAS number Packaging Price Updated Buy
Sigma-Aldrich SML0666 GSK1210151A ≥98% (HPLC) 1300031-49-5 5mg $156 2024-03-01 Buy
Sigma-Aldrich SML0666 GSK1210151A ≥98% (HPLC) 1300031-49-5 25mg $620 2024-03-01 Buy
Cayman Chemical 11181 I-BET151 ≥98% 1300031-49-5 1mg $36 2024-03-01 Buy
Cayman Chemical 11181 I-BET151 ≥98% 1300031-49-5 5mg $98 2024-03-01 Buy
Cayman Chemical 11181 I-BET151 ≥98% 1300031-49-5 10mg $179 2024-03-01 Buy
Product number Packaging Price Buy
SML0666 5mg $156 Buy
SML0666 25mg $620 Buy
11181 1mg $36 Buy
11181 5mg $98 Buy
11181 10mg $179 Buy

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

1300737-69-2
1300031-49-5
Synthesis of I-BET151 (GSK1210151A) from 3-QuinolinecarboxaMide, 7-(3,5-diMethyl-4-isoxazolyl)-6-Methoxy-4-[[(1R)-1-(2-pyridinyl)ethyl]aMino]-

I-BET151 (GSK1210151A) Preparation Products And Raw materials

Raw materials

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

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Preparation Products

I-BET151 (GSK1210151A) Suppliers

Global( 135)Suppliers
Supplier Tel Email Country ProdList Advantage
ATK CHEMICAL COMPANY LIMITED 		+undefined-21-51877795 ivan@atkchemical.com China 32480 60
Biochempartner 		0086-13720134139 candy@biochempartner.com CHINA 967 58
Hubei Jusheng Technology Co.,Ltd. 		18871490254 linda@hubeijusheng.com CHINA 28180 58
BOC Sciences 		+1-631-485-4226 inquiry@bocsci.com United States 19553 58
CONIER CHEM AND PHARMA LIMITED 		+8618523575427 sales@conier.com China 47465 58
career henan chemical co 		+86-0371-86658258 15093356674; factory@coreychem.com China 29826 58
TargetMol Chemicals Inc. 		+1-781-999-5354 +1-00000000000 marketing@targetmol.com United States 19892 58
HANGZHOU CLAP TECHNOLOGY CO.,LTD 		86-571-88216897,88216896 13588875226 sales@hzclap.com CHINA 6313 58
Dideu Industries Group Limited 		+86-29-89586680 +86-15129568250 1026@dideu.com China 29271 58
Dayang Chem (Hangzhou) Co.,Ltd. 		571-88938639 +8617705817739 info@dycnchem.com CHINA 52867 58
Supplier Advantage
ATK CHEMICAL COMPANY LIMITED 		60
Biochempartner 		58
Hubei Jusheng Technology Co.,Ltd. 		58
BOC Sciences 		58
CONIER CHEM AND PHARMA LIMITED 		58
career henan chemical co 		58
TargetMol Chemicals Inc. 		58
HANGZHOU CLAP TECHNOLOGY CO.,LTD 		58
Dideu Industries Group Limited 		58
Dayang Chem (Hangzhou) Co.,Ltd. 		58

View Lastest Price from I-BET151 (GSK1210151A) manufacturers

Image Update time Product Price Min. Order Purity Supply Ability Manufacturer
I-BET151 (GSK1210151A) pictures 2020-01-13 I-BET151 (GSK1210151A)
1300031-49-5
 US $1.00 / g 1g 99% 200kg Career Henan Chemical Co
7Methyl-5-(1-{[3-(trifluoroMethyl)phenyl]acetyl}-2,3-dihydro1Hindol-5-yl)7Hpyrrolo[2,3d]pyriMidin-4-aMine pictures 2020-01-13 7Methyl-5-(1-{[3-(trifluoroMethyl)phenyl]acetyl}-2,3-dihydro1Hindol-5-yl)7Hpyrrolo[2,3d]pyriMidin-4-aMine
1300031-49-5
 US $1.00 / g 1g 99% 200kg Career Henan Chemical Co
7Methyl-5-(1-{[3-(trifluoroMethyl)phenyl]acetyl}-2,3-dihydro1Hindol-5-yl)7Hpyrrolo[2,3d]pyriMidin-4-aMine pictures 2020-01-13 7Methyl-5-(1-{[3-(trifluoroMethyl)phenyl]acetyl}-2,3-dihydro1Hindol-5-yl)7Hpyrrolo[2,3d]pyriMidin-4-aMine
1300031-49-5
 US $1.00 / g 1g 99% 200kg Career Henan Chemical Co

I-BET151 (GSK1210151A) Spectrum

I-BET151 (GSK1210151A)(1300031-49-5)1HNMR

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

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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