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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%
包装与价格:
包装价格(元)
5mg电议
25mg电议
50mg电议
100mg电议
250mg电议
500mg电议

产品介绍
理化性质和储存条件
Molecular Weight (MW)509.04
FormulaC28H33ClN4O3
CAS No.1613695-14-9
Storage-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)DMSO: 100 mg/mL (196.4 mM)
Water: <1 mg/mL
Ethanol: 100 mg/mL (196.4 mM)
Solubility (In vivo) 2% DMSO+30% PEG 300+5% Tween 80+ddH2O: 5 mg/mL
Synonyms

SGC-CBP 30; SGC-CBP-30; SGC-CBP30.

Chemical Name: (S)-4-(1-(2-(3-chloro-4-methoxyphenethyl)-5-(3,5-dimethylisoxazol-4-yl)-1H-benzo[d]imidazol-1-yl)propan-2-yl)morpholine

InChi Key: GEPYBHCJBORHCE-SFHVURJKSA-N

InChi Code: InChI=1S/C28H33ClN4O3/c1-18(32-11-13-35-14-12-32)17-33-25-8-7-22(28-19(2)31-36-20(28)3)16-24(25)30-27(33)10-6-21-5-9-26(34-4)23(29)15-21/h5,7-9,15-16,18H,6,10-14,17H2,1-4H3/t18-/m0/s1

SMILES Code: C[C@H](N1CCOCC1)CN2C(CCC3=CC=C(OC)C(Cl)=C3)=NC4=CC(C5=C(C)ON=C5C)=CC=C24

实验参考方法
In Vitro

In vitro activity: SGC-CBP30 is a potent and selective CREBBP/EP300 bromodomain inhibitor with IC50 of 21 nM and 38 nM for CREBBP and EP300 bromodomains in cell-free assays, respectively. CREBBP (CBP) and EP300 are general transcriptional co-activators. CREBBP has also been associated with Amyotrophic Lateral Sclerosis (ALS) or Lou GehrigA’s disease, a neurodegenerative disease with progressive degeneration of motor neurons in the brain and spinal cord, Alzheimer's disease and poly glutamine repeat diseases such as Spinal and Bulbar Muscular Atrophy and HuntingtonA’s disease. As a CREBBP/EP300-selective chemical probe, SGC-CBP30 shows moderate cytotoxicity in U2OS cells and HeLa cells.


Kinase Assay: SGC-CBP30 is a highly potent and selective p300/CBP bromodomain inhibitor (IC50 ~0.021-0.069 uM for CBP and ~0.038 uM for p300). It has 40-fold selectivity for CBP over BRD4. It accelerated FRAP recovery at 1 uM.


Cell Assay: In HeLa cells, treatment of SAHA-treated cells with 0.1 μM SGC-CBP30 reduces FRAP recovery times back to unstimulated levels. In RKO cells, SGC-CBP30 effectively inhibits the Doxorubicin induced p53 activity in a dose-dependent manner.

In VivoSGC-CBP30 treatment slightly alleviates alveolar bronchial fibrosis induced by Bleomycin. 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 bleomycininduced IPF murine models to nearly normal levels
Animal modelRats
Formulation & Dosage25 mg/kg; Oral
ReferencesJ Am Chem Soc. 2014 Jul 2;136(26):9308-19.; Biomed Pharmacother. 2018 Oct;106:1727-1733.