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CCT-367766

  Cat. No.:  DC11679   Featured
Chemical Structure
2229856-58-8
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More than 5000 active chemicals with high quality for research!
Field of application
CCT367766 is a potent and the third generation heterobifunctional and PROTAC-based pirin targeting protein degradation probe (PDP), depletes pirin protein expression at low concentration. CCT367766 exhibits a moderate affinity for the CRBN-DDB1 complex with an IC50 value of 490 nM. CCT367766 reveals a good affinity for the recombinant pirin and CRBN with Kd values of 55 nM and 120 nM, respectively. CCT367766 provides a potential chemical tool to study a largely unexplored protein[1].
Chemicals PropertiesBiological activity COA & MSDSRelated productsDatasheet
Cas No.: 2229856-58-8
Chemical Name: N-(2-Chloro-5-(2,3-dihydrobenzo[b][1,4]dioxine-6-carboxamido)phenyl)-2-((4-(2-(2-(2-((2-(2,6-dioxopiperidin-3-yl)-1,3-dioxoisoindolin-4-yl)oxy)ethoxy)ethoxy)ethyl)piperazin-1-yl)methyl)quinoline-6-carboxamide
Synonyms: CCT367766;CCT 367766
SMILES: N1C2C(=CC(C(NC3=CC(NC(C4=CC=C5C(=C4)OCCO5)=O)=CC=C3Cl)=O)=CC=2)C=CC=1CN1CCN(CCOCCOCCOC2=CC=CC3=C2C(=O)N(C2CCC(=O)NC2=O)C3=O)CC1
Formula: C49H48ClN7O11
M.Wt: 946.41
Purity: >98%
Sotrage: 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
Publication: [1]. Chessum NEA, et al. Demonstrating In-Cell Target Engagement Using a Pirin Protein Degradation Probe (CCT367766).J Med Chem. 2018 Feb 8;61(3):918-933.
Description: CCT-367766 (CCT367766) is a novel heterobifunctional PROTAC that binds and degrades the putative transcription factor regulator Pirin in cells.
Target: CRBN-DDB1:490 nM (IC50)
In Vitro: CCT367766 (50-1500 nM; 24 hours) demonstates the depletion of pirin protein as a the time-dependent hook-effect in SK-OV-3 human ovarian cancer cells[1]. CCT367766 (0.5-50 nM; 2 hours) demonstrates the concentration-dependent depletion of pirin protein after 2 h exposure in SK-OV-3 cells[1]. Western Blot Analysis[1] Cell Line: SK-OV-3 human ovarian cancer cells Concentration: 50, 150, 250, 500 and 1500 nM Incubation Time: 2 hours, 4 hours, 24 hours Result: Decreased pirin protein expression. Western Blot Analysis[1] Cell Line: SK-OV-3 human ovarian cancer cells Concentration: 0.5, 1, 2.5, 5, 7.5, 10, 25, and 50 nM Incubation Time: 2 hours Result: Completely degraded pirin just at 50 nM treatment.
References: [1]. Chessum NEA, et al. Demonstrating In-Cell Target Engagement Using a Pirin Protein Degradation Probe (CCT367766).J Med Chem. 2018 Feb 8;61(3):918-933.
MSDS
COA
LOT NO. DOWNLOAD
2018-0101
2018-0101
2018-0101
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