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Chemical Structure : I-BET762
CAS No.: 1260907-17-2
Catalog No.: PC-43340Not For Human Use, Lab Use Only.
I-BET762 (GSK-525762A, Molibresib) is a highly potent, selective inhibitor of BET family proteins BRD2, BRD3 and BRD4 with IC50 of 32.5-42.5 nM, does not interact with other bromodomain-containing proteins (BAZ2B, ATAD2, CREBBP and PCAF).
| Packing | Price | Stock | Quantity |
|---|---|---|---|
| 25 mg | $198 | In stock | |
| 50 mg | $298 | In stock | |
| 100 mg | $488 | In stock | |
| 200 mg | Get quote | ||
| 1 g | Get quote |
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I-BET762 (GSK-525762A, Molibresib) is a highly potent, selective inhibitor of BET family proteins BRD2, BRD3 and BRD4 with IC50 of 32.5-42.5 nM, does not interact with other bromodomain-containing proteins (BAZ2B, ATAD2, CREBBP and PCAF).
I-BET762 inhibits binding of BET proteins to acetylated histones, disrupts chromatin complexes responsible for the expression of key inflammatory genes in activated macrophages, suppresses TNF-inducible key proinflammatory cytokine (il1b, il1a) and chemokine genes (ccl5, cxcl10, cxcl2/3) in BMDMs.
I-BET762 inhibits the ability of Th1-differentiated 2D2 T cells to induce neuroinflammation in vivo in mouse model of EAE.
I-BET762 inhibits myeloma cell proliferation both in vitro and myeloma xenograft models.
| M.Wt | 423.8954 | |
| Formula | C22H22ClN5O2 | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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| Chemical Name/SMILES |
4H-[1,2,4]Triazolo[4,3-a][1,4]benzodiazepine-4-acetamide, 6-(4-chlorophenyl)-N-ethyl-8-methoxy-1-methyl-, (4S)- |
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1. Nicodeme E, et al. Nature. 2010 Dec 23;468(7327):1119-23.
2. Bandukwala HS, et al. Proc Natl Acad Sci U S A. 2012 Sep 4;109(36):14532-7.
3. Mirguet O, et al. J Med Chem. 2013 Oct 10;56(19):7501-15.
4. Chaidos A, et al. Blood. 2014 Jan 30;123(5):697-705.
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