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GSK046 (iBET-BD2)

  Cat. No.:  DC39702   Featured
Chemical Structure
2474876-09-8
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More than 5000 active chemicals with high quality for research!
Field of application
GSK046 (iBET-BD2) is a potent, selective and orally active BD2 bromodomain inhibitor 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. GSK046 has immunomodulatory activity.
Chemicals PropertiesBiological activity COA & MSDSRelated productsDatasheet
Cas No.: 2474876-09-8
Chemical Name: GSK046
Synonyms: GSK046;GSK-046;GSK 046
SMILES: O=C(N[C@H]1CC[C@H](O)CC1)C2=CC(O[C@H](C3=CC=CC=C3)C)=C(NC(C)=O)C(F)=C2
Formula: C23H27FN2O4
M.Wt: 414.47
Purity: >98%
Sotrage: 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
Description: GSK046 (iBET-BD2) is a selective and orally active inhibitor of BET, with IC50s of 264 nM (BRD2 BD2), 98 nM (BRD3 BD2), 49 nM (BRD4 BD2) and 214 nM (BRDT BD2), respectively[1].
Target: BRD2 BD2:264 nM (IC50) BRD3 BD2:98 nM (IC50) BRD4 BD2:49 nM (IC50) BRDT BD2:214 nM (IC50)
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).
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.
References: [1]. Omer G, et, al. Selective targeting of BD1 and BD2 of the BET proteins in cancer and immunoinflammation. Science. 2020 Apr 24; 368(6489): 387-394.
MSDS
COA
LOT NO. DOWNLOAD
2018-0101
2018-0101
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