product name SGC-CBP30
Description: SGC-CBP30 is a potent and selective CREBBP/EP300 inhibitor with IC50 of 21 nM and 38 nM 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.
References: J Am Chem Soc. 2014 Jul 2;136(26):9308-19.
509.04
Formula
C28H33ClN4O3
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
other peoduct :References PubMed ID：:http://www.ncbi.nlm.nih.gov/pubmed/19419532
| In Vitro |
In vitro activity: 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. |
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| In Vivo | |
| Animal model | |
| Formulation & Dosage | |
| References | J Am Chem Soc. 2014 Jul 2;136(26):9308-19. |
