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Chemical Structure : I-BET151
CAS No.: 1300031-49-5
Catalog No.: PC-43414Not For Human Use, Lab Use Only.
I-BET151 (GSK1210151A) is a potent, selective BET bromodomain inhibitor with IC50 of 0.5, 0.25 and 0.79 uM for BRD2, BRD3 and BRD4 in FP assays, shows no effect on the 23 other bromodomain proteins including MLL.
| Packing | Price | Stock | Quantity |
|---|---|---|---|
| 5 mg | $98 | In stock | |
| 10 mg | $138 | In stock | |
| 25 mg | $238 | In stock | |
| 50 mg | $398 | In stock | |
| 100 mg | Get quote |
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I-BET151 (GSK1210151A) is a potent, selective BET bromodomain inhibitor with IC50 of 0.5, 0.25 and 0.79 uM for BRD2, BRD3 and BRD4 in FP assays, shows no effect on the 23 other bromodomain proteins including MLL.
I-BET151 (GSK1210151A) demonstrates potent efficacy against cell lines harbouring different MLL-fusions (MOLM13 cell IC50=120 nM, MV4:11 cell IC50=26 nM).
I-BET151 (GSK1210151A) induces early cell cycle arrest and apoptosis, selectively abrogates BRD3/4 recruitment to chromatin。
I-BET151 (GSK1210151A) shows significant therapeutic value and survival benefit in mouse models of murine MLL-AF9 and human MLL-AF4 leukaemia.
| M.Wt | 415.4445 | |
| Formula | C23H21N5O3 | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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| Chemical Name/SMILES |
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]- |
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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.
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