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    SGC-CBP30
    SGC-CBP30

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    This product is for research use only, not for human use. We do not sell to patients.
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    InvivoChem Cat #: V0417
    CAS #: 1613695-14-9Purity ≥98%

    Description: SGC-CBP30 is a novel, 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 GehrigÂ’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 HuntingtonÂ’s disease. 

    References: J Am Chem Soc. 2014 Jul 2;136(26):9308-19.

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    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[[email protected]](N1CCOCC1)CN2C(CCC3=CC=C(OC)C(Cl)=C3)=NC4=CC(C5=C(C)ON=C5C)=CC=C24 


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    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 GehrigÂ’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 HuntingtonÂ’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.


    These protocols are for reference only. InvivoChem does not independently validate these methods.

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