GSK778 hydrochloride

SKU: orb1297936

Description

GSK778 hydrochloride is a potent and selective BD1 bromodomain inhibitor of BET proteins, demonstrating low nanomolar IC50 values. It mimics pan-BET inhibitor effects in cancer models, making it a valuable tool for epigenetic research in oncology, applicable in both cellular and in vivo studies of transcriptional regulation and tumor progression.

Research Area

Cell Biology, Epigenetics & Chromatin

Key Properties

• CAS Number: 2863657-79-6
• MW: 548.08
• Purity: 98.35% (May vary between batches)
• Formula: C₃₀H₃₄ClN₅O₃
• SMILES: C[C@@H](N1C(COC)=NC2=C1C3=CC(OC[C@@H]4CNCC4)=C(C5=C(C)ON=C5C)C=C3N=C2)C6=CC=CC=C6.[H]Cl
• Target: Apoptosis,Epigenetic Reader Domain
• Solubility: DMSO:50 mg/mL (91.23 mM)

Bioactivity

• Target IC50:
  BRD3 BD1:41 nM|BRDT BD1:143 nM|BRD2 BD1:75 nM|BRD4 BD1:41 nM
• 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. 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. 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.
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• 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. 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. 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. 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. GSK778 hydrochloride (1000 nM; 12 days) reduces the clonogenic capacity of primary human AML cells.
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Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

BET, EpigeneticReaderDomain, Epigenetic Reader Domain, GSK-778 Hydrochloride, GSK778 Hydrochloride, GSK778 hydrochloride, GSK 778 Hydrochloride

Compound Identifiers

PubChem CID

168013350