iBET-BD1 MedChemExpress (MCE)

Product Name	GSK778
Synonyms	GSK778;FREEBASE;iBET-BD1;iBET-BD1 dihydrochloride;1H-Imidazo[4,5-c]quinoline, 7-(3,5-dimethyl-4-isoxazolyl)-2-(methoxymethyl)-1-[(1R)-1-phenylethyl]-8-[(3S)-3-pyrrolidinylmethoxy]-
CAS	2451862-42-1
EINECS
Chemical Formula	C30H33N5O3
Molecular Weight	511.61
inchi
Package	10 mM * 1 mL;1 mg;5 mg;10 mg
Price	Email to quote
Descriptions	GSK778 GSK778 MedChemExpress (MCE) HY-136570 2451862-42-1 iBET-BD1 98.93% Powder -20°C 3 years 4°C 2 years In solvent -80°C 1 year -20°C 6 months Room temperature in continental US Descriptions GSK778 GSK778 MedChemExpress (MCE) HY-136570 2451862-42-1 iBET-BD1 98.93% Powder -20°C 3 years 4°C 2 years In solvent -80°C 1 year -20°C 6 months Room temperature in continental US may vary elsewhere. GSK778 (iBET-BD1) is a potent and selective BD1 bromodomain inhibitor of the BET proteins, with IC50s of 75 nM (BRD2 BD1), 41 nM (BRD3 BD1), 41 nM (BRD4 BD1), and 143 nM (BRDT BD1), respectively. GSK778 phenocopies the effects of pan-BET inhibitors in cancer models. GSK778 inhibits BRD BD2 with the IC50s of 3950 nM (BRD2 BD2), 1210 nM (BRD3 BD2), 5843 nM (BRD4 BD2), and 17451 nM (BRDT BD2), respectively[1].?GSK778 (0.01-10 μM 72 hours) inhibits the proliferative activity of human primary CD4+ T cells and the production of effector cytokines including IFNγ, IL-17A and IL-22[1].?GSK778 (0.001-10 μM 5 days) has a more pronounced effect on the growth and viability of MDA-453, MOLM-13, K562, MV4-11, THP-1, and MDA-MB-231 cells[1].?GSK778 (1000 nM 72 hours) inhibits proliferation, induces a cell cycle arrest and apoptosis in MV4-11, MOLM13, MDA-MB-231 and MB453 cells[1].?GSK778 (1000 nM 12 days) reduces the clonogenic capacity of primary human AML cells[1]. GSK778 (15?mg/kg/BID i.p. for 30 days) offers a superior survival advantage to iBET-BD2 in the aggressive MLL-AF9 AML model[1].?GSK778 (15?mg/kg/BID s.c. for 14 days) reduces the production of anti-keyhole limpet hemocyanin (KLH) IgM and is well tolerated[1].?GSK778 exhibits Cmax (85 ng/mL), Tmax (1.48 h) and AUC∞ (132 ng.h/mL) following oral administration (10?mg/kg) in mice[1]. BRD2 BD1 75 nM (IC50) BRD3 BD1 41 nM (IC50) BRD4 BD1 41 nM (IC50) BRDT BD1 143 nM (IC50) \| \| \| \| \| \| \| \| \| \| [1]. Omer G, et, al. Selective targeting of BD1 and BD2 of the BET proteins in cancer and immunoinflammation. Science. 2020 Apr 24 368(6489): 387-394. [Content Brief]
Supplier Website	https://www.medchemexpress.com/gsk778.html
Last Update	2025-05-21 16:50:25

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