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APExBIO

GSK 525768A

In stock
Catalog No.
A3445
inactive stereoisomer of I-BET-762
Grouped product items
SizePriceStock Qty
10mM (in 1mL DMSO)
$601.00
In stock
5mg
$546.00
In stock
10mg
$881.00
In stock
50mg
$2,405.00
In stock
100mg
$3,276.00
In stock

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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

StorageStore at -20°C
M.Wt423.9
Cas No.1260530-25-3
FormulaC22H22ClN5O2
SynonymsGSK525768A;GSK-525768A
SolubilitySoluble in DMSO
Chemical Name2-[(4R)-6-(4-chlorophenyl)-8-methoxy-1-methyl-4H-[1,2,4]triazolo[4,3-a][1,4]benzodiazepin-4-yl]-N-ethylacetamide
SDFDownload SDF
Canonical SMILESCCNC(=O)CC1C2=NN=C(N2C3=C(C=C(C=C3)OC)C(=N1)C4=CC=C(C=C4)Cl)C
Shipping ConditionEvaluation sample solution : ship with blue ice.All other available size: ship with RT , or blue ice upon request
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.

Quality Control

Quality Control & MSDS

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Chemical structure

GSK 525768A