1. Epigenetics
    Apoptosis
  2. Epigenetic Reader Domain
    Apoptosis
  3. GSK778

GSK778 (Synonyms: iBET-BD1)

Cat. No.: HY-136570
Handling Instructions

GSK778 (iBET-BD1) is a potent and selective inhibitor of bromodomain (BRD) BD1, 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.

For research use only. We do not sell to patients.

GSK778 Chemical Structure

GSK778 Chemical Structure

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Description

GSK778 (iBET-BD1) is a potent and selective inhibitor of bromodomain (BRD) BD1, 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[1].

IC50 & Target[1]

BRD2 BD1

75 nM (IC50)

BRD3 BD1

41 nM (IC50)

BRD4 BD1

41 nM (IC50)

BRDT BD1

143 nM (IC50)

In Vitro

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].

Cell Proliferation Assay[1]

Cell Line: Human primary CD4+ T cell
Concentration: 0.001, 0.01, 0.1, 1, 10 μM
Incubation Time: 72 hours
Result: Inhibited the proliferative activity of the cells and the production of effector cytokines.

Cell Viability Assay[1]

Cell Line: MDA-453, MOLM-13, K562, MV4-11, THP-1, and MDA-MB-231 cells
Concentration: 0.001, 0.01, 0.1, 1, 10 μM
Incubation Time: 5 days
Result: Inhibited the growth and viability of human cancer cell lines.

Apoptosis Analysis[1]

Cell Line: MV4-11, MOLM13, MDA-MB-231 and MB453 cells
Concentration: 1000 nM
Incubation Time: 72 hours
Result: Inhibited cell proliferation and induced a cell cycle arrest and apoptosis.
In Vivo

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].

Animal Model: 6-8 weeks female C57BL/6 mice are injected with MLL-AF9 cells[1]
Dosage: 15 mg/kg/BID
Administration: I.p. injections for 30 days
Result: Increased the survival rate of leukemia mice.
Animal Model: Male CD1 mice[1]
Dosage: 10 mg/kg (Pharmacokinetic Analysis)
Administration: P.o. administration
Result: Cmax (85 ng/mL), Tmax (1.48 h); AUC (132 ng.h/mL).
Molecular Weight

511.61

Formula

C₃₀H₃₃N₅O₃

SMILES

CC1=NOC(C)=C1C2=C(OC[[email protected]@H]3CNCC3)C=C4C5=C(N=C(COC)N5[[email protected]](C)C6=CC=CC=C6)C=NC4=C2

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

References
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Keywords:

GSK778iBET-BD1GSK 778GSK-778Epigenetic Reader DomainApoptosisBD1BRD2BRD3BRD4BRDTcancerimmuno-inflammationInhibitorinhibitorinhibit

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