2. Metabolic Enzyme/Protease
  3. E1/E2/E3 Enzyme
  4. WS-383 free base

WS-383 free base 是一种有效、选择性、可逆的 DCN1-UBC12 相互作用抑制剂，IC50 值为 11 nM。WS-383 free base 抑制 Cul3/1 的类泛素化修饰，引起 p21，p27 和 NRF2 的积累。

在相同的摩尔浓度下，化合物盐形式与游离形式有相同的生物活性，但盐形式 WS-383 通常具有更好的水溶性和稳定性。

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WS-383 free base Chemical Structure

WS-383 free base Chemical Structure

CAS No. : 2247543-65-1

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WS-383 free base 的其他形式现货产品:

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WS-383 free base 相关抗体

Top Publications Citing Use of Products

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

WS-383 free base is a potent, selective and reversible inhibitor of DCN1-UBC12 interaction, with an IC50 of 11 nM. WS-383 free base inhibits Cul3/1 neddylation, induces accumulation of p21, p27 and NRF2[1].

IC50 & Target

IC50: 11 nM (DCN1–UBC12 interaction)[1]
体外研究
(In Vitro)

WS-383 (10 μM) is against a panel of kinases such as BTK, CDKs, and EGFR [L858R] using staurosporine and afatinib as the positive controls. WS-383 showed weak inhibitory activity at 10.0 μM,it is selective to the DCN1–UBC12 interaction over the selected kinasesr[1].
WS-383 (0.03-3 μM;24 hours) blocks Cul3 neddylation at 3 μM and also has certain inhibition of Cul1 neddylation at 10 μM but was not effective in inhibiting neddylation of other cullin members[1].
WS-383 (0.03-3 μM;24 hours) increases Cul1, Skp1 (adaptor protein), F-box protein, and RBX1/RBX2 RING protein form SCF E3 complex. Cyclin dependent kinase inhibitor 1A (p21) and cyclin dependent kinase inhibitor 1B (p27) expression in a dose-dependent manner in MGC-803 and KYSE70 manner[1].

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

WS-383 free base 相关抗体:

Western Blot Analysis[1]

Cell Line: MGC-803 cells
Concentration: 0.03 μM; 0.3 μM; 3 μM; 10 μM
Incubation Time: 24 hours
Result: Decreased N8-Cul1 and N8-Cul2 protein expression.

Western Blot Analysis[1]

Cell Line: MGC-803 and KYSE70 cells
Concentration: 0.03 μM; 0.3 μM; 3 μM; 10 μM
Incubation Time: 24 hours
Result: Induced accumulation of p21, p27, and NRF2 in MGC-803 cells.
分子量

461.99

Formula

C18H20ClN9S2
CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

WS-383 free base 相关分类

  • 摩尔计算器

  • 稀释计算器

The molarity calculator equation

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

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

WS-3832247543-65-1WS383WS 383E1/E2/E3 EnzymeE1 activating enzymeE2 conjugating enzymeE3 ligating enzymeUbiquitin activating enzymeUbiquitin conjugating enzymeUbiquitin ligaseMGC-803KYSE70cellDCN1-UBC12interactionInhibitorinhibitorinhibit

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