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SML0666

GSK1210151A

≥98% (HPLC)

Synonym(s):

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

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About This Item

Empirical Formula (Hill Notation):
C23H21N5O3
CAS Number:
1300031-49-5
Molecular Weight:
415.44
UNSPSC Code:
12352200
NACRES:
NA.77
Assay:
≥98% (HPLC)
Form:
powder
Quality level:
100
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Quality Level

100

assay

≥98% (HPLC)

form

powder

color

white to beige

solubility

DMSO: 20 mg/mL, clear

originator

GlaxoSmithKline

relevant disease(s)

cancer

storage temp.

2-8°C

SMILES string

[n]2(c3c([nH][c]2=O)cnc4c3cc(c(c4)c5c(n[o]c5C)C)OC)[C@H](C)c1ncccc1

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

InChI key

VUVUVNZRUGEAHB-CYBMUJFWSA-N

Application

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.

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 (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.

Other Notes

GSK1210151A has been expertly reviewed and recommended by the Chemical Probes Portal. For more information, please visit the GSK1210151A probe summary on the Chemical Probes Portal website.

pictograms

Skull and crossbones
GHS06

signalword

Danger

hcodes

H301

Hazard Classifications

Acute Tox. 3 Oral

Storage Class

6.1C - Combustible acute toxic Cat.3 / toxic compounds or compounds which causing chronic effects

wgk

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable

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Certificates of Analysis (COA)

Lot/Batch Number
0000383612
0000383612
0000238598
0000234586
0000238598

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Replication Study: Inhibition of BET recruitment to chromatin as an effective treatment for MLL-fusion leukaemia.
Shan X, et al.
eLife, 6, e25306-e25306 (2017)
Zhongyuan Gao et al.
Cancer biology & therapy, 19(5), 407-415 (2018-01-16)
Lung cancer is the leading cause of cancer-related death worldwide. Bromodomain and extraterminal domain (BET) proteins act as epigenome readers for gene transcriptional regulation. Among BET family members, BRD4 was well studied, but for its mechanism in non-small cell lung
Lisa-Maria Winter et al.
Scientific reports, 13(1), 12061-12061 (2023-07-27)
GDF15 has recently emerged as a key driver of the development of various disease conditions including cancer cachexia. Not only the tumor itself but also adverse effects of chemotherapy have been reported to contribute to increased GDF15. Although regulation of
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