SGC-CBP30 is a potent CREBBP/EP300 inhibitor with IC50 of 21 nM and 38 nM in cell-free assays, respectively. It has 40-fold selectivity for CBP over BRD4. SGC-CBP30 shows moderate cytotoxicity in U2OS cells and HeLa cells as a CREBBP/EP300-selective chemical probe.
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.
|Solubility||DMSO: ≥ 30 mg/mL|
Inhibition of EP300 and DDR1 synergistically alleviates pulmonary fibrosis in vitro and in vivo.
Tao J, et al. Biomed Pharmacother. 2018 Oct;106:1727-1733. PMID: 30119248.
Activity of bromodomain protein inhibitors/binders against asexual-stage Plasmodium falciparum parasites.
Chua MJ, et al. Int J Parasitol Drugs Drug Resist. 2018 Aug;8(2):189-193. PMID: 29631126.
Discovery and optimization of 1-(1H-indol-1-yl)ethanone derivatives as CBP/EP300 bromodomain inhibitors for the treatment of castration-resistant prostate cancer.
Xiang Q, et al. Eur J Med Chem. 2018 Mar 10;147:238-252. PMID: 29448139.
|Related Epigenetic Reader Domain Products|
AZD5153 is a potent bivalent triazolopyridazine based Bromodomain and Extraterminal (BET) Inhibitor, with IC50 value of 5 nM.
MS417 (also known as GTPL7512) is a potent and selective BRD4 inhibitor, which binds to BRD4-BD1 and BRD4-BD2 with IC50s of 30 and 46 nM, respectively.
FL-411 is a selective BRD4 inhibitor.
dBET6 is a highly potent, selective and cell-permeable degrader of BET with an IC50 of 14 nM.
dBET1 is a potent BRD4 protein degrader with an EC50 of 430 nM.
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