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JQAD1
🥰Excellent
Catalog No. T41180Cas No. 2417097-18-6
JQAD1 is a potent and selective histone acetyltransferase EP300 degrader (PROTAC®; DC50≤ 31.6 nM); comprises an EP300 inhibitor, A485, 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 tumors 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.
JQAD1
🥰Excellent
Purity: 99.75%
Catalog No. T41180Cas No. 2417097-18-6
JQAD1 is a potent and selective histone acetyltransferase EP300 degrader (PROTAC®; DC50≤ 31.6 nM); comprises an EP300 inhibitor, A485, 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 tumors 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.
| Pack Size | Price | Availability | Quantity |
|---|---|---|---|
| 1 mg | $131 | In Stock | |
| 5 mg | $328 | In Stock | |
| 10 mg | $498 | In Stock | |
| 25 mg | $812 | In Stock | |
| 50 mg | $1,130 | In Stock | |
| 100 mg | $1,520 | In Stock |
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CitedSelect Batch
Purity:99.75%
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All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.Product Introduction
Bioactivity
Chemical Properties
| Description | JQAD1 is a potent and selective histone acetyltransferase EP300 degrader (PROTAC®; DC50≤ 31.6 nM); comprises an EP300 inhibitor, A485, 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 tumors 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. |
| In vitro | JQAD1 (0.5 or 1 μ M; 6-96 h) treatment led to early time-dependent induction of sub-G1 peak, indicating that apoptosis of Kelly and NGP cells. JQAD1 (1 μ M; 12-36 h) induced apoptosis of Kelly NB cell. JQAD1 (0.5 μ M; 24 h) treated cells showed up-regulation of BH3 effectors BIM, BID and PUMA, pro-apoptotic mediator BAX and its inhibitors BCL2 and MCL1. JQAD1 (0.5 and 1 μ M; 24 h) destroy expression of MYCN. JQAD1 (0.5 μ M; 24 h) lead to H3K27ac deletion on chromatin. JQAD1 (1.2 nM-20 μ M; 5 days) has extensive CRBN-dependent anti-tumor activity across cancer cell lines. JQAD1 induced degradation of EP300 in a time-dependent manner, at the earliest 16 hours [1]. |
| In vivo | JQAD1 (40 mg/kg; i.p.; once daily for 21 days) inhibits tumor growth in NSG mice transplanted with Kelly NB cells [1]. |
| Molecular Weight | 932.95 |
| Formula | C48H52F4N6O9 |
| Cas No. | 2417097-18-6 |
| Smiles | O=C1[C@@]2(C=3C(CC2)=CC(NC(CCCCCCCCCCCNC=4C=C5C(=CC4)C(=O)N(C5=O)C6C(=O)NC(=O)CC6)=O)=CC3)OC(=O)N1CC(N(CC7=CC=C(F)C=C7)[C@H](C(F)(F)F)C)=O |
Storage & Solubility Information
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | ||||||||||||||||||||||||||||||
| Solubility Information | DMSO: 90.0 mg/mL (96.5 mM), Sonication is recommended. | ||||||||||||||||||||||||||||||
Solution Preparation Table | |||||||||||||||||||||||||||||||
DMSO
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In Vivo Formulation Calculator (Clear solution)
Please enter your animal experiment information in the following box and click Calculate to obtain the mother liquor preparation method and in vivo formula preparation method:
For example, your dosage is 10 mg/kg Each animal weighs 20 g, and the dosage volume is 100 μL . A total of 10 animals were administered, and the formula you used is 5% 
DMSO+30% PEG300+5% Tween 80+60% ddH2O. So your working solution concentration is 2 mg/mL。Mother liquor preparation method: 2 mg of drug dissolved in 50 μL DMSO (mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.
(mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.Preparation method for in vivo formula: Take 50 μL DMSO main solution, add 300 μLPEG300 mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O mix well and clarify
main solution, add 300 μLPEG300 mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O mix well and clarifyFor Reference Only. Please develop an appropriate dissolution method based on your laboratory animals and route of administration.
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