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GSK778 hydrochloride

Catalog No. T9703L CAS 2863657-79-6

GSK778 hydrochloride hydrochloride 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 hydrochloride hydrochloride phenocopies the effects of pan-BET inhibitors in cancer models[1].

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GSK778 hydrochloride, CAS 2863657-79-6

Pack Size	Availability	Price/USD
1 mg	In stock	$ 195.00
5 mg	In stock	$ 437.00
10 mg	In stock	$ 646.00
25 mg	In stock	$ 987.00
50 mg	In stock	$ 1,380.00
100 mg	In stock	$ 1,860.00
1 mL * 10 mM (in DMSO)	In stock	$ 561.00

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Biological Description

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Description	GSK778 hydrochloride hydrochloride 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 hydrochloride hydrochloride phenocopies the effects of pan-BET inhibitors in cancer models[1].
In vitro	GSK778 hydrochloride 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 hydrochloride (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 hydrochloride (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 hydrochloride (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 hydrochloride (1000 nM; 12 days) reduces the clonogenic capacity of primary human AML cells[1].
In vivo	GSK778 hydrochloride (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 hydrochloride (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 hydrochloride exhibits Cmax (85 ng/mL), Tmax (1.48 h) and AUC∞ (132 ng.h/mL) following oral administration (10?mg/kg) in mice[1].

Molecular Weight	548.08
Formula	C30H34ClN5O3
CAS No.	2863657-79-6

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 50 mg/mL (91.23 mM)

References and Literature

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.

Related compound libraries

This product is contained In the following compound libraries：

Inhibitor Library Anti-Cancer Active Compound Library Anti-Cancer Compound Library PPI Inhibitor Library Bioactive Compounds Library Max Histone Modification Compound Library Bioactive Compound Library Epigenetics Compound Library

Related Products

Related compounds with same targets

GSK-5959 FHD-286 ZEN-3219 dBET1 IACS-9571 Hydrochloride (1800477-30-8 free base) GNE-064 Diflunisal BETd-260

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Keywords

GSK778 hydrochloride 2863657-79-6 Chromatin/Epigenetic Epigenetic Reader Domain GSK778 Hydrochloride GSK 778 Hydrochloride GSK-778 Hydrochloride inhibitor inhibit

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