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 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 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

CAS No. : 2451862-42-1

Size Price Stock
5 mg USD 700 Ask For Quote & Lead Time
10 mg USD 1200 Ask For Quote & Lead Time
25 mg USD 2500 Ask For Quote & Lead Time
50 mg USD 4200 Ask For Quote & Lead Time
100 mg USD 6500 Ask For Quote & Lead Time

* Please select Quantity before adding items.

Top Publications Citing Use of Products
  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

GSK778 (iBET-BD1) 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 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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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

CAS No.

2451862-42-1

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
  • No file chosen (Maximum size is: 1024 Kb)
  • If you have published this work, please enter the PubMed ID.
  • Your name will appear on the site.
  • Molarity Calculator

  • Dilution Calculator

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass   Concentration   Volume   Molecular Weight *
= × ×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
× = ×
C1   V1   C2   V2

Keywords:

GSK778iBET-BD1GSK 778GSK-778Epigenetic Reader DomainApoptosisInhibitorinhibitorinhibit

Your Recently Viewed Products:

Inquiry Online

Your information is safe with us. * Required Fields.

Product Name

 

Salutation

Applicant Name *

 

Email address *

Phone number *

 

Organization name *

Department *

 

Requested quantity *

Country or Region *

     

Remarks

Bulk Inquiry

Inquiry Information

Product Name:
GSK778
Cat. No.:
HY-136570
Quantity:
MCE Japan Authorized Agent: