1. Epigenetics
  2. Epigenetic Reader Domain
  3. GSK046

GSK046 (Synonyms: iBET-BD2)

Cat. No.: HY-136571 Purity: 98.05%
Handling Instructions

GSK046 (iBET-BD2) is a potent, selective and orally active bromodomain inhibitor of BD2 of the BET proteins, with IC50s of 264 nM (BRD2 BD2), 98 nM (BRD3 BD2), 49 nM (BRD4 BD2) and 214 nM (BRDT BD2), respectively.

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

GSK046 Chemical Structure

GSK046 Chemical Structure

CAS No. : 2474876-09-8

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Based on 1 publication(s) in Google Scholar

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Description

GSK046 (iBET-BD2) is a potent, selective and orally active bromodomain inhibitor of BD2 of the BET proteins, with IC50s of 264 nM (BRD2 BD2), 98 nM (BRD3 BD2), 49 nM (BRD4 BD2) and 214 nM (BRDT BD2), respectively[1].

IC50 & Target[1]

BRD2 BD2

264 nM (IC50)

BRD3 BD2

98 nM (IC50)

BRD4 BD2

49 nM (IC50)

BRDT BD2

214 nM (IC50)

In Vitro

GSK046 (1000 nM; refresh every three days) reduces the recruitment of BET proteins to interferon (IFN) target genes following IFN-γ stimulation. GSK046 appears to more prominently affect the recruitment of BRD2 and BRD3 compared to BRD4[1].
GSK046 (0.1-10 μM) displays a more selective phenotypic fingerprint, particularly inhibiting the production of key pro-inflammatory mediators including Th17 cytokines in the B and T cell co-culture system[1].
GSK046 (0.01-10 μM; 72 hours) does not affect the proliferative activity of human primary CD4+ T cells but still inhibits the production of effector cytokines including IFNγ, IL-17A and IL-22[1].
GSK046 (0.005-10 μM; 48 hours) impairs macrophage activation following PMA stimulation, without impacting cellular viability[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: Did not affect the proliferative activity of the cells but still inhibited the production of effector cytokines.
In Vivo

GSK046 (40 mg/kg/QD; s.c. for 14 days) has immunomodulatory activity[1].
GSK046 exhibits Cmax (C57BL6 1589, C57B16 2993 ng/mL) and terminal elimination half-lives (C57BL6 1.8, C57B16 1.9 h) following oral administration (C57BL6 10, C57B16 40 mg/kg)[1].
GSK046 exhibits Cmax (mouse 1589, rat 202 ng/mL) and terminal elimination half-lives (mouse 1.8, rat 1.4 h) following oral administration (mouse 10, rat 10 mg/kg)[1].

Animal Model: Male C57BL/6 mice (8/10-weeks-old) are injected with keyhole limpet hemocyanin (KLH)[1]
Dosage: 40 mg/kg/QD
Administration: S.c. injections for 14 days
Result: Reduced the production of anti-keyhole limpet hemocyanin (KLH) IgM and was well tolerated.
Animal Model: Female C57BL/6 mice[1]
Dosage: 10 mg/kg (Pharmacokinetic Analysis)
Administration: Oral administration
Result: Cmax (1859 ng/mL), T1/2 (1.8 h).
Animal Model: Male C57BL/6 mice[1]
Dosage: 40 mg/kg (Pharmacokinetic Analysis)
Administration: Oral administration
Result: Cmax (2993 ng/mL), T1/2 (1.9 h).
Animal Model: Female Lewis rat[1]
Dosage: 10 mg/kg (Pharmacokinetic Analysis)
Administration: Oral administration
Result: Cmax (202 ng/mL), T1/2 (1.4 h).
Molecular Weight

414.47

Formula

C₂₃H₂₇FN₂O₄

CAS No.

2474876-09-8

SMILES

O=C(N[[email protected]]1CC[[email protected]](O)CC1)C2=CC(O[[email protected]](C3=CC=CC=C3)C)=C(NC(C)=O)C(F)=C2

Shipping

Room temperature in continental US; may vary elsewhere.

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

DMSO : 83.33 mg/mL (201.05 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.4127 mL 12.0636 mL 24.1272 mL
5 mM 0.4825 mL 2.4127 mL 4.8254 mL
10 mM 0.2413 mL 1.2064 mL 2.4127 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 (5.02 mM); Clear solution

  • 2.

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

    Solubility: ≥ 2.08 mg/mL (5.02 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.08 mg/mL (5.02 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
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Keywords:

GSK046iBET-BD2GSK 046GSK-046Epigenetic Reader DomainBD2BRD2BRD3 BRD4BRDT immuno-inflammationInhibitorinhibitorinhibit

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GSK046
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