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

GSK778  (Synonyms: iBET-BD1)

Cat. No.: HY-136570 Purity: 98.93%
COA 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 Quantity
Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
USD 450 In-stock
Solution
10 mM * 1 mL in DMSO USD 450 In-stock
Solid
1 mg USD 200 In-stock
5 mg USD 400 In-stock
10 mg USD 640 In-stock
25 mg USD 1280 In-stock
50 mg USD 2050 In-stock
100 mg USD 3300 In-stock
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Customer Review

Based on 1 publication(s) in Google Scholar

Other Forms of GSK778:

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  • Biological Activity

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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].

MedChemExpress (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].

MedChemExpress (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.
Appearance

Solid

Color

White to light yellow

SMILES

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 1 year
-20°C 6 months
Solvent & Solubility
In Vitro: 

DMSO : 41.67 mg/mL (81.45 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.9546 mL 9.7731 mL 19.5461 mL
5 mM 0.3909 mL 1.9546 mL 3.9092 mL
10 mM 0.1955 mL 0.9773 mL 1.9546 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.08 mg/mL (4.07 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: 2.08 mg/mL (4.07 mM); Suspended solution; Need ultrasonic

  • 3.

    Add each solvent one by one:  10% DMSO    90% Corn Oil

    Solubility: ≥ 2.08 mg/mL (4.07 mM); Clear solution

*All of the co-solvents are available by MedChemExpress (MCE).
Purity & Documentation

Purity: 98.93%

References
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GSK778 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Product Name:
GSK778
Cat. No.:
HY-136570
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