JQAD1
Tocris Bioscience, part of Bio-Techne | Catalog # 7682
Potent and selective EP300 Degrader (PROTAC®)
Key Product Details
Description
Potent and selective EP300 Degrader (PROTAC®)
Product Description
JQAD1 is a potent and selective histone acetyltransferase EP300 Degrader (PROTAC®; DC50 ≤ 31.6 nM); comprises an EP300 inhibitor, A485 (Cat. No. 6387), joined by a linker to a cereblon E3 ligase ligand. JQAD1 brings about degradation of EP300 in neuroblastoma cell lines in a proteasome-dependent manner. JQAD1 suppresses both H3K27ac and EP300 expression levels and induces apoptosis. JQAD1 suppresses tumor growth in NSG mice xenografted with Kelly cells. CRC and MYCN genes are downregulated in tumors treated with JQAD1. JQAD1 exhibits no significant effect on coactivator CBP at concentrations inducing EP300 degradation.p300 antibody validated for Simple Western™ (automated Western) instruments and Western Blot also available: Catalog # AF3789.
PROTAC® is a registered trademark of Arvinas Operations, Inc., and is used under license.
Licensing Information
Sold under license from Dana-Farber Cancer InstituteProduct Specifications
Molecular Weight
932.97
Formula
C48H52F4N6O9
Storage
Store at -20°C
Purity
≥98% (HPLC)
Chemical Name
12-((2-(2,6-dioxopiperidin-3-yl)-1,3-dioxoisoindolin-5-yl)amino)-N-((R)-3'-(2-((4-fluorobenzyl)((S)-1,1,1-trifluoropropan-2-yl)amino)-2-oxoethyl)-2',4'-dioxo-2,3-dihydrospiro[indene-1,5'-oxazolidin]-5-yl)dodecanamide
CAS Number
2417097-18-6
PubChem ID
162615894
InChI Key
TWCIGBYYSZQAAA-GWWVHQGYSA-N
SMILES
C[C@@H](C(F)(F)F)N(C(CN1C(O[C@]2(C1=O)CCC3=CC(NC(CCCCCCCCCCCNC4=CC=C5C(N(C(C5=C4)=O)C6CCC(NC6=O)=O)=O)=O)=CC=C23)=O)=O)CC7=CC=C(C=C7)F
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Solubility
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 93.3 | 100 |
Preparing Stock Solutions
for JQAD1
The following data is based on the product molecular weight 932.97
Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which all affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 1.07 mL | 5.36 mL | 10.72 mL |
| 5 mM | 0.21 mL | 1.07 mL | 2.14 mL |
| 10 mM | 0.11 mL | 0.54 mL | 1.07 mL |
| 50 mM | 0.02 mL | 0.11 mL | 0.21 mL |
Calculators
Molarity Calculator
Dilution Calculator
Reconstitution Calculator
Background References
References are publications that support the biological activity of the product.
- Durbin EP300 selectively controls the enhancer landscape of MYCN-amplified neuroblastoma. Cancer Discov. 2021 PMID: 34772733
Product Specific Notices for JQAD1
For research use only
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