Structure
I-BET151, Inhibitor
I-BET151
Purity
>98% (HPLC)
Synonyms
I-BET151; GSK1210151A; I-BET 151; GSK-1210151A; inhibitor
Purity/Purification
>98% (HPLC)
Suitability
10mM in DMSO
Target
Bromodomain
Receptor
BRD2; BRD3; BRD4
Chemical Name
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]
SMILES
O=C(N1[C@@H](C2=NC=CC=C2)C)NC3=C1C4=CC(OC)=C(C5=C(C)ON=C5C)C=C4N=C3
Molecular Formula
C23H21N5O3
CAS Number
1300031-49-5
Preparation and Storage
Store at -20 degree C
Stability: >=2 years
Shipping: Ice Pack
Stability: >=2 years
Shipping: Ice Pack
Structure
Structure
Related Product Information for I-BET151, inhibitor
I-BET151 (GSK1210151A) is a potent, selective BET bromodomain inhibitor with IC50 of 0.5, 0.25 and 0.79uM for BRD2, BRD3 and BRD4 in FP assays, shows no effect on the 23 other bromodomain proteins including MLL; demonstrates potent efficacy against cell lines harbouring different MLL-fusions (MOLM13 cell IC50=120nM, MV4:11 cell IC50=26nM), induices early cell cycle arrest and apoptosis, selectively abrogates BRD3/4 recruitment to chromatin; shows significant therapeutic value and survival benefit in mouse models of murine MLL-AF9 and human MLL-AF4 leukaemia.
Product Categories/Family for I-BET151, inhibitor
References
1. Dawson MA, et al. Nature. 2011 Oct 2; 478 (7370):529-33.
2. Mirguet O, et al. Bioorg Med Chem Lett. 2012 Apr 15; 22 (8):2963-7.
3. Chaidos A, et al. Blood. 2014 Jan 30; 123 (5):697-705.
4. Wyspiańska BS, et al. Leukemia. 2014 Jan; 28 (1):88-97.
2. Mirguet O, et al. Bioorg Med Chem Lett. 2012 Apr 15; 22 (8):2963-7.
3. Chaidos A, et al. Blood. 2014 Jan 30; 123 (5):697-705.
4. Wyspiańska BS, et al. Leukemia. 2014 Jan; 28 (1):88-97.
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Product Notes
The I-BET151 (Catalog #AAA3601204) is an Inhibitor and is intended for research purposes only. The product is available for immediate purchase. It is sometimes possible for the material contained within the vial of "I-BET151, Inhibitor" to become dispersed throughout the inside of the vial, particularly around the seal of said vial, during shipment and storage. We always suggest centrifuging these vials to consolidate all of the liquid away from the lid and to the bottom of the vial prior to opening. Please be advised that certain products may require dry ice for shipping and that, if this is the case, an additional dry ice fee may also be required.Precautions
All products in the AAA Biotech catalog are strictly for research-use only, and are absolutely not suitable for use in any sort of medical, therapeutic, prophylactic, in-vivo, or diagnostic capacity. By purchasing a product from AAA Biotech, you are explicitly certifying that said products will be properly tested and used in line with industry standard. AAA Biotech and its authorized distribution partners reserve the right to refuse to fulfill any order if we have any indication that a purchaser may be intending to use a product outside of our accepted criteria.Disclaimer
Though we do strive to guarantee the information represented in this datasheet, AAA Biotech cannot be held responsible for any oversights or imprecisions. AAA Biotech reserves the right to adjust any aspect of this datasheet at any time and without notice. It is the responsibility of the customer to inform AAA Biotech of any product performance issues observed or experienced within 30 days of receipt of said product. To see additional details on this or any of our other policies, please see our Terms & Conditions page.Item has been added to Shopping Cart
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