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Purity: ≥98%
SGC-CBP30 is a novel, potent and selective inhibitor of CREBBP (CBP/KAT3A) and its paralogue EP300 (KAT3B) with the potential to be used in neurodegenerative diseases (e.g. Alzheimer's disease). CREBBP/EP300 are the lysine acetyltransferases (KATs) that are essential for human development. It inhibits CREBBP and EP300 bromodomains with IC50s 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, Alzheimer's disease and poly glutamine repeat diseases such as Spinal and Bulbar Muscular Atrophy and HuntingtonÂ's disease.
| ln Vitro |
In ankylosing spondylitis and psoriatic arthritis situations, SGC-CBP30 suppresses IL-17A release by Th17 cells. Transcriptional profiling of human T cells following SGC-CBP30 treatment demonstrated more restricted effects on gene expression than that reported with the pan-BET (bromodomain and ecto-terminal protein family) bromodomain inhibitor JQ1[1] .
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| ln Vivo |
Treatment with SGC-CBP30 somewhat reduced the alveolar bronchial fibrosis caused by NSC-125066. Alveolar bronchial fibrosis is greatly reduced by SGC-CBP30 with CQ-061. The combination of SGC-CBP30 0 and CQ-061 suppressed the activation of IL-4 and IFN-γ in the NSC-125066-induced IPF mouse model to near normal levels, according to an ELISA of the cytokines IL-4 and IFN-γ in BALF [2].
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| Animal Protocol |
Animal/Disease Models: SD (Sprague-Dawley) rats (aged 3-4 weeks) injected with NSC-125066[2]
Doses: 25 mg/kg Route of Administration: Oral administration; daily; for 14 days Experimental Results: Slightly alleviated alveolar bronchial fibrosis induced by NSC-125066. |
| References |
[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. |
| Molecular Formula |
C28H33CLN4O3
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| Molecular Weight |
509.04
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| CAS # |
1613695-14-9
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| Related CAS # |
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| SMILES |
C[C@H](N1CCOCC1)CN2C(CCC3=CC=C(OC)C(Cl)=C3)=NC4=CC(C5=C(C)ON=C5C)=CC=C24
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| InChi Key |
GEPYBHCJBORHCE-SFHVURJKSA-N
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| 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
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| 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
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| Synonyms |
SGC-CBP 30; SGC-CBP-30; SGC-CBP30.
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Solubility (In Vivo) |
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| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.9645 mL | 9.8224 mL | 19.6448 mL | |
| 5 mM | 0.3929 mL | 1.9645 mL | 3.9290 mL | |
| 10 mM | 0.1964 mL | 0.9822 mL | 1.9645 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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