product name CeMMEC1
Description: CeMMEC1, an N-methylisoquinolinone analog, is a novel potent inhibitor of TAF4 that inhibits the second bromodomain of TAF1 (Kd = 1.8 µM; IC50 = 0.9 µM). CeMMEC1 only bound BRD4 very weakly but it shows high affinity for the bromodomains of CREBBP, EP300, BRD9 and the second bromodomain of TAF1. It does not bind to either the first or second bromodomain of BRD4. Pharmacological inhibitors of bromodomain promise therapeutic benefits in a variety of cancers.
References: Nat Chem Biol. 2016 Jul;12(7):504-10.
372.8
Formula
C19H17ClN2O4
CAS No.
440662-09-9(free base)
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: 23 mg/mL (61.7 mM)
Water: <1 mg/mL
Ethanol: <1 mg/mL
Solubility (In vivo)
Synonyms
other peoduct :
| In Vitro |
In vitro activity: CeMMEC1 only bound BRD4 very weakly but it shows high affinity for the bromodomains of CREBBP, EP300, BRD9 and the second bromodomain of TAF1. Kinase Assay: Cell Assay: Bromodomain-containing proteins of the BET family recognize histone lysine acetylation and mediate transcriptional activation of target genes such as the MYC oncogene. Pharmacological inhibitors of BET domains promise therapeutic benefits in a variety of cancers. We performed a high-diversity chemical compound screen for agents capable of modulating BRD4-dependent heterochromatization of a generic reporter in human cells. In addition to known and new compounds targeting BRD4, we identified small molecules that mimic BRD4 inhibition without direct engagement. One such compound was a potent inhibitor of the second bromodomain of TAF1. Using this inhibitor, we discovered that TAF1 synergizes with BRD4 to control proliferation of cancer cells, making TAF1 an attractive epigenetic target in cancers driven by MYC. |
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| Formulation & Dosage | |
| References | Nat Chem Biol. 2016 Jul;12(7):504-10. |
