Powder: -20°C for 3 years | In solvent: -80°C for 1 year
GSK778 is a potent and selective inhibitor of BD1 bromodomain such as BRD2 BD1 (IC50s = 75 nM), BRD3 BD1 (IC50s = 41 nM), BRD4 BD1 (IC50s = 41 nM), and BRDT BD1 (IC50s = 143 nM). GSK778 inhibits proliferation, induces a cell cycle arrest and apoptosis.
Pack Size | Availability | Price/USD | Quantity |
---|---|---|---|
1 mg | In stock | $ 163.00 | |
5 mg | In stock | $ 328.00 | |
10 mg | In stock | $ 529.00 | |
25 mg | In stock | $ 1,060.00 | |
50 mg | In stock | $ 1,680.00 | |
100 mg | In stock | $ 2,330.00 | |
1 mL * 10 mM (in DMSO) | In stock | $ 39.00 |
Description | GSK778 is a potent and selective inhibitor of BD1 bromodomain such as BRD2 BD1 (IC50s = 75 nM), BRD3 BD1 (IC50s = 41 nM), BRD4 BD1 (IC50s = 41 nM), and BRDT BD1 (IC50s = 143 nM). GSK778 inhibits proliferation, induces a cell cycle arrest and apoptosis. |
Targets&IC50 | BRD3 BD1:41 nM, BRD2 BD1:75 nM, BRDT BD1:143 nM, BRD4 BD1:41 nM |
In vitro | GSK778 phenocopies the effects of pan-BET inhibitors in cancer models. GSK778 inhibits BRD BD2 receptors such as BRD2 BD2 (IC50 = 3950 nM), BRD3 BD2 (IC50 = 1210 nM ), BRD4 BD2 (IC50 = 5843 nM), and BRDT BD2 (IC50 = 17451 nM)[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. GSK778 (1000 nM; 12 days) reduces the clonogenic capacity of primary human AML cells. GSK778 (0.01-10 μM; 72 hours) inhibited the production of effector cytokines including IFNγ, IL-17A and IL-22 and the proliferative activity of human primary CD4+ T cells[1]. |
In vivo | 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 (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]. The Cmax, Tmax and AUC∞ values are 85 ng/mL, 1.48 h and 132 ng.h/mL, respectively. |
Molecular Weight | 511.61 |
Formula | C30H33N5O3 |
CAS No. | 2451862-42-1 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 41.67 mg/mL (81.45 mM)
You can also refer to dose conversion for different animals. More
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GSK778 2451862-42-1 Chromatin/Epigenetic Epigenetic Reader Domain iBET-BD1 GSK 778 GSK-778 Apoptosis inhibit Inhibitor inhibitor