1. Metabolic Enzyme/Protease
  2. E1/E2/E3 Enzyme
  3. WS-383

WS-383 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 抑制 Cul3/1 的类泛素化修饰,引起 p21,p27 和 NRF2 的积累。

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WS-383 Chemical Structure

WS-383 Chemical Structure

CAS No. : 2247544-02-9

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10 mM * 1 mL in DMSO ¥3400
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1 mg ¥1409
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5 mg ¥3100
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10 mg ¥5300
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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

WS-383 is a potent, selective and reversible inhibitor of DCN1-UBC12 interaction, with an IC50 of 11 nM. WS-383 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 BIBW 2992 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.

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

498.46

Formula

C18H21Cl2N9S2

CAS 号
性状

固体

颜色

White to off-white

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, sealed storage, away from moisture and light

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

溶解性数据
In Vitro: 

DMSO 中的溶解度 : 7.35 mg/mL (14.75 mM; 超声助溶; 吸湿的 DMSO 对产品的溶解度有显著影响,请使用新开封的 DMSO)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.0062 mL 10.0309 mL 20.0618 mL
5 mM 0.4012 mL 2.0062 mL 4.0124 mL
查看完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)。-80°C储存时,请在6个月内使用,-20°C储存时,请在1个月内使用。

  • 摩尔计算器

  • 稀释计算器

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

质量
=
浓度
×
体积
×
分子量 *

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

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start)

C1

×
体积 (start)

V1

=
浓度 (final)

C2

×
体积 (final)

V2

动物溶解方案计算器
请输入动物实验的基本信息:

给药剂量

mg/kg

动物的平均体重

g

每只动物的给药体积

μL

动物数量

由于实验过程有损耗,建议您多配一只动物的量
计算结果
工作液所需浓度 : mg/mL
纯度 & 产品资料
参考文献

完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)。-80°C储存时,请在6个月内使用,-20°C储存时,请在1个月内使用。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.0062 mL 10.0309 mL 20.0618 mL 50.1545 mL
5 mM 0.4012 mL 2.0062 mL 4.0124 mL 10.0309 mL
10 mM 0.2006 mL 1.0031 mL 2.0062 mL 5.0154 mL
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.

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产品名称:
WS-383
目录号:
HY-126075A
需求量: