GSK778 | BRD BD1 inhibitor | Probechem Biochemicals

Chemical Structure : GSK778

CAS No.: 2451862-42-1

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GSK778 (iBET-BD1)

货号: PC-38071Not For Human Use, Lab Use Only.

GSK778 is a potent and selective inhibitor of bromodomain (BRD) BD1 with IC50 of 75 nM (BRD2-BD1), 41 nM (BRD3-BD1), 41 nM (BRD4 BD1), and 143 nM (BRDT BD1), respectively.

规格	价格	库存
5 mg	￥2980	In stock
10 mg	￥4580	In stock
25 mg		Get quote
100 mg		Get quote

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生物&药学活性

GSK778 is a potent and selective inhibitor of bromodomain (BRD) BD1 with IC50 of 75 nM (BRD2-BD1), 41 nM (BRD3-BD1), 41 nM (BRD4 BD1), and 143 nM (BRDT BD1), respectively.
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.
GSK778 inhibits the proliferative activity of human primary CD4+ T cells and the production of effector cytokines including IFNγ, IL-17A and IL-2.
GSK778 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 reduces the clonogenic capacity of primary human AML cells.
GSK778 offers a superior survival advantage to iBET-BD2 in the aggressive MLL-AF9 AML model. GSK778 reduces the production of anti-keyhole limpet hemocyanin (KLH) IgM and is well tolerated.

物理化学性质&存储条件

分子量	511.63
分子式	C30H33N5O3
外观性状	Solid
CAS No.
储存条件	固体粉末 -20 °C 12 个月; 4°C 6 个月	配置液 -80 °C 6 个月; -20°C 6 个月
Shipping
Solubility	10 mM in DMSO
Chemical Name/SMILES	4-(2-(methoxymethyl)-1-((R)-1-phenylethyl)-8-(((S)-pyrrolidin-3-yl)methoxy)-1H-imidazo[4,5-c]quinolin-7-yl)-3,5-dimethylisoxazole

参考文献

1. Chun-Shan Liu, et al. Int J Cancer. 2022 Mar 3. doi: 10.1002/ijc.33989.

GSK778 (iBET-BD1)

生物&药学活性

物理化学性质&存储条件

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GSK778 (iBET-BD1)

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