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  2. Apoptosis
  3. Apoptosis
  4. DB1976

DB1976 是一種 DB270 的硒烯類似物，是一種高效且可滲透細(xì)胞的轉(zhuǎn)錄因子 PU.1 的抑制劑。在體外，DB1976 有效抑制 PU.1 結(jié)合 (IC50 為 10 nM)，可強(qiáng)烈抑制 PU.1/DNA 復(fù)合物 (具有高 DB1976-λB 親和力，KD 為 12 nM)。DB1976 具有誘導(dǎo)細(xì)胞凋亡的作用。

該游離形式化合物不穩(wěn)定，推薦具有相同生物學(xué)活性的穩(wěn)定鹽形式 DB1976 dihydrochloride。

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DB1976 Chemical Structure

DB1976 Chemical Structure

CAS No. : 1557397-51-9

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Other Forms of DB1976:

  • 生物活性

  • 純度 & 產(chǎn)品資料

  • 參考文獻(xiàn)

生物活性

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[1][2][3].

IC50 & Target

IC50: 10 nM (Transcription factor PU.1)[1]
體外研究
(In Vitro)

DB1976 is a classic heterocyclic dication (a single heteroatom) with strong affinity and selectivity for AT-rich sequences commonly found in cognate DNA binding sites for PU.1[2].
DB1976 inhibits PU.1-dependent transactivation of the reporter in a dose-dependent manner with an IC50 value of 2.4 μM in PU.1-negative HEK293 cells[3].
DB1976 treatment leads to a profound decrease in the growth of PU.1 URE–/– AML cells (IC50 of 105 μM), while showing little effect on normal hematopoietic cells at similar concentrations (IC50 of 334 μM)[3].
DB1976 treatment leads to a 1.6-fold increase in apoptotic cells in murine PU.1 URE–/– AML cells, and observed similar effects in human MOLM13 cells[3].
DB1976 treatment leads to a significant decrease in the number of viable cells (primary human AML cells) (mean decrease of 81%) and clonogenic capacity (mean decrease of 36%) compared with vehicle-treated cells. The apoptotic cell fraction increased on average by 1.5-fold with DB1976[3].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
分子量

447.35

Formula

C20H16N8Se
CAS 號(hào)
運(yùn)輸條件

Room temperature in continental US; may vary elsewhere.
儲(chǔ)存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
純度 & 產(chǎn)品資料
參考文獻(xiàn)

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The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

質(zhì)量   濃度   體積   分子量 *
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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

濃度 (start) × 體積 (start) = 濃度 (final) × 體積 (final)
× = ×
C1   V1   C2   V2
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產(chǎn)品名稱：
DB1976
目錄號(hào)：
HY-135797
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