Product Details
| Product Name:
DB1976 |
CAS No.:
1557397-51-9 |
| Purity:
98.94% |
Supply Ability:
10g |
| Release date:
2024/11/12 |
Product Introduction
Bioactivity
| 名稱 | DB1976 |
| 描述 | DB1976 is a selenophene analog of DB270 and a highly potent, cell-permeable, fully efficacious transcription factor PU.1 inhibitor. It effectively inhibits PU.1 binding (IC50 of 10 nM) and strongly inhibits the PU.1/DNA complex (with high DB1976-λB affinity, KD of 12 nM) in vitro. Additionally, DB1976 has an apoptosis-inducing effect. |
| 體外活性 | DB1976 is a heterocyclic dication possessing a strong affinity and selectivity for AT-rich sequences in DNA, which are crucial for the binding of transcription factor PU.1. It effectively inhibits the activation mediated by PU.1 in a dose-dependent manner, displaying an IC50 of 2.4 μM in PU.1-negative HEK293 cells. Importantly, DB1976 significantly reduces the growth of PU.1 URE–/– AML cells, with an IC50 of 105 μM, while minimally affecting normal hematopoietic cells (IC50 of 334 μM). Treatment with DB1976 results in a notable increase in apoptosis, particularly a 1.6-fold rise in murine PU.1 URE–/– AML cells and similar outcomes in human MOLM13 cells. Furthermore, DB1976 dramatically reduces the viability (by 81%) and clonogenic capacity (by 36%) of primary human AML cells compared to those treated with a vehicle, alongside effecting a 1.5-fold increase in the apoptotic cell fraction. |
| 存儲(chǔ)條件 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| 溶解度 | DMSO : Insoluble
|
| 關(guān)鍵字 | DB-1976 | DB1976 | DB 1976 |
| 相關(guān)產(chǎn)品 | Stavudine | 5-Fluorouracil | Acetylcysteine | Kaempferol | Myricetin | Sodium 4-phenylbutyrate | L-Ascorbic acid | Dextran sulfate sodium salt (MW 4500-5500) | Metronidazole | Sorafenib | Tributyrin | Lidocaine hydrochloride |
| 相關(guān)庫(kù) | 經(jīng)典已知活性庫(kù) | 已知活性化合物庫(kù) |
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 |
|
|
$118.00/1mg |
VIP5Y
|
TargetMol Chemicals Inc.
|
2024-11-12 |
United States