Product Details
| Product Name:
JQAD1 |
CAS No.:
2417097-18-6 |
| Purity:
99.75% |
Supply Ability:
10g |
| Release date:
2024/11/14 |
Product Introduction
Bioactivity
| 名稱 | JQAD1 |
| 描述 | 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. |
| 體外活性 | 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]. |
| 體內(nèi)活性 | JQAD1 (40 mg/kg; i.p.; once daily for 21 days) inhibits tumor growth in NSG mice transplanted with Kelly NB cells [1]. |
| 存儲條件 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| 溶解度 | DMSO : 90.0 mg/mL (96.5 mM), Sonication is recommended.
|
| 關(guān)鍵字 | JQAD-1 | JQAD 1 | JQAD1 |
| 相關(guān)產(chǎn)品 | ABBV-744 | CeMMEC1 | 3-methyl-1,2,3,4-tetrahydroquinazolin-2-one | (+)-JQ-1 | ARV-471 | Curcumin | dBET6 | Naphthol AS-E | Bisdemethoxycurcumin |
| 相關(guān)庫 | 經(jīng)典已知活性庫 | 已知活性化合物庫 | 抗癌活性化合物庫 |
Company Profile Introduction
Target Molecule Corp. (TargetMol) is a global high-tech enterprise, headquartered in Boston, MA, specializing in chemical and biological research product and service to meet the research needs of global customers.
TargetMol has evolved into one of the biggest global compound library and small molecule suppliers and a customer based on 40+ countries. TargetMol offers over 80 types of compound libraries and a wide range of high-quality research chemicals including inhibitors, activator, natural compounds, peptides, inhibitory antibodies, and novel life-science kits, for laboratory and scientific use. Besides, virtual screening service is also available for customers who would like to conduct the computer-aided drug discovery.
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Recommended supplier
| Product name |
Price |
|
Suppliers |
Update time |
|
|
$/ |
|
Anhui Ruihan Technology Co., Ltd
|
2023-08-21 |
United States