Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DB1976 is a selenophene analog of DB270 and a potent and cell-permeable fully efficacious transcription factor PU.1 inhibitor. DB1976 potently 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. DB1976 has Apoptosis-inducing effect.
パッケージサイズ | 在庫状況 | 単価(税別) |
---|---|---|
1 mg | 在庫あり | ¥ 45,500 |
5 mg | 在庫あり | ¥ 91,500 |
10 mg | 在庫あり | ¥ 135,500 |
25 mg | 在庫あり | ¥ 217,000 |
50 mg | 在庫あり | ¥ 294,000 |
100 mg | 在庫あり | ¥ 397,000 |
500 mg | 在庫あり | ¥ 794,000 |
説明 | DB1976 is a selenophene analog of DB270 and a potent and cell-permeable fully efficacious transcription factor PU.1 inhibitor. DB1976 potently 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. DB1976 has Apoptosis-inducing effect. |
ターゲット&IC50 | PU.1:10 nM |
In vitro | 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. |
分子量 | 447.35 |
分子式 | C20H16N8Se |
CAS No. | 1557397-51-9 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: Insoluble
You can also refer to dose conversion for different animals. 詳細
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DB1976 1557397-51-9 Apoptosis Others DB-1976 DB 1976 Inhibitor inhibitor inhibit