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SGC-CBP30
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
SGC-CBP30图片
CAS NO:1613695-14-9
规格:98%
分子量:509.04
包装与价格:
包装价格(元)
10mg电议
50mg电议

产品介绍
Inhibitor of CREBBP/EP300 bromodomain,potent
CAS:1613695-14-9
分子式:C28H33ClN4O3
分子量:509.04
纯度:98%
存储:Store at -20°C

Background:

SGC-CBP30 is a potent and highly selective CBP/p300 bromodomain (Kds of 21 nM and 32 nM for CBP and p300, respectively) inhibitor, displaying 40-fold selectivity over the first bromodomain of BRD4 [BRD4(1)] bound. SGC-CBP30 strongly reduces secretion of IL-17A in Th17 cells and has anti-inflammatory effects[1][2][3].


In ankylosing spondylitis and psoriatic arthritis condition, SGC-CBP30 inhibits IL-17A secretion by Th17 cells. Transcriptional profiling of human T cells after SGC-CBP30 treatment shows a much more restricted effect on gene expression than that observed with the pan-BET (bromo and extraterminal domain protein family) bromodomain inhibitor JQ1[1].


SGC-CBP30 treatment slightly alleviates alveolar bronchial fibrosis induced by NSC-125066. SGC-CBP30 plus CQ-061 dramatically reduces alveolar bronchial fibrosis. The ELISA of cytokines IL-4 and IFN-γ in BALF demonstrates that combination of SGC-CBP300 and CQ-061 suppresses the activation of IL-4 as well as IFN-γ in NSC-125066 induced IPF murine models to nearly normal levels[2].


参考文献:
[1]. Hammitzsch A, et al. CBP30, a selective CBP/p300 bromodomain inhibitor, suppresses human Th17 responses. Proc Natl Acad Sci U S A. 2015 Aug 25;112(34):10768-73.
[2]. Tao J, Inhibition of EP300 and DDR1 synergistically alleviates pulmonary fibrosis in vitro and in vivo. Biomed Pharmacother. 2018 Oct;106:1727-1733.
[3]. Hay DA, et al. Discovery and optimization of small-molecule ligands for the CBP/p300 bromodomains. J Am Chem Soc. 2014 Jul 2;136(26):9308-19.