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GSK 525768A (Synonyms: GSK525768A;GSK-525768A)

Catalog No.GC10524

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GSK 525768A Chemical Structure

Cas No.: 1260530-25-3

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5mg
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10mg
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50mg
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Sample solution is provided at 25 µL, 10mM.

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Background

GSK 525768A is the inactive stereoisomer of I-BET-762 which is a selective inhibitor of BET family with IC50 value of 35 nM [1].
BET (bromodomain and extra-terminal domain) has 4 members, BRD2, BDR3, BRD4 and BRDT and plays an important role in regulating transcription. It has been shown that BET involves in the process of suppressing proinflammatory cytokines production by macrophages and has potent anti-proliferative effects on tumor cells [2].
I-BET-762 is a potent BET inhibitor and suppresses macrophage-derived proinflammatory cytokines production [1]. When tested with naïve CD4+ T cells, I-BET-762 treatment for short 2-d up-regulated anti-inflammatory cytokines production (IL-10, Lag 3 and Egr2) and down-regulated proinflammatory cytokines production (GM-CSF and IL-17) constantly [3].
When tested with LPS-treated C57BL/6 mice, administration with I-BET-762 (5 mg per kg, i.p.) significantly suppressed LPS-induced acute inflammation compared with control GSK 525768A treated group [1]. In adoptive transfer of EAE mouse model with 2D2 T cell receptor that producing IL-17, pretreated T cells with I-BET-762 suppressed T cell mediated inflammation and decreased macrophages recruitment compared with GSK 525768A treatment [3].
References:
[1].    Nicodeme, E., et al., Suppression of inflammation by a synthetic histone mimic. Nature, 2010. 468(7327): p. 1119-23.
[2].    Bartholomeeusen, K., et al., Bromodomain and extra-terminal (BET) bromodomain inhibition activate transcription via transient release of positive transcription elongation factor b (P-TEFb) from 7SK small nuclear ribonucleoprotein. J Biol Chem, 2012. 287(43): p. 36609-16.
[3].    Bandukwala, H.S., et al., Selective inhibition of CD4+ T-cell cytokine production and autoimmunity by BET protein and c-Myc inhibitors. Proc Natl Acad Sci U S A, 2012. 109(36): p. 14532-7.

Chemical Properties

Cas No. 1260530-25-3 SDF
Synonyms GSK525768A;GSK-525768A
Chemical Name 2-[(4R)-6-(4-chlorophenyl)-8-methoxy-1-methyl-4H-[1,2,4]triazolo[4,3-a][1,4]benzodiazepin-4-yl]-N-ethylacetamide
Canonical SMILES CCNC(=O)CC1C2=NN=C(N2C3=C(C=C(C=C3)OC)C(=N1)C4=CC=C(C=C4)Cl)C
Formula C22H22ClN5O2 M.Wt 423.9
Solubility Soluble in DMSO Storage Store at -20°C
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table

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1 mg 5 mg 10 mg
1 mM 2.359 mL 11.7952 mL 23.5905 mL
5 mM 0.4718 mL 2.359 mL 4.7181 mL
10 mM 0.2359 mL 1.1795 mL 2.359 mL
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Average Rating: 5 ★★★★★ (Based on Reviews and 30 reference(s) in Google Scholar.)

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