S81370 |
SGC-CBP30 |
源叶(MedMol) | 99% |
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- 产品描述: 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
- 靶点: CBP/p300 bromodomain;EpigeneticReaderDomain; HistoneAcetyltransferase
- 体内研究:
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
- 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.
- 溶解性: DMSO : ≥ 31 mg/mL (60.90 mM)
- 保存条件: 2-8℃
- 配置溶液浓度参考:
1mg 5mg 10mg 1 mM 1.964 ml 9.822 ml 19.645 ml 5 mM 0.393 ml 1.964 ml 3.929 ml 10 mM 0.196 ml 0.982 ml 1.964 ml 50 mM 0.039 ml 0.196 ml 0.393 ml
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质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子摩尔量 (g/mol)