2. Epigenetics Metabolic Enzyme/Protease Cell Cycle/DNA Damage Apoptosis
  3. Histone Demethylase E1/E2/E3 Enzyme DNA/RNA Synthesis Caspase Apoptosis
  4. WS-384

WS-384 是一种具有口服活性的双 LSD1 和 DCN1-UBC12 蛋白-蛋白相互作用抑制剂，IC50 值分别为 338.79 nM 和 14.81 nM。WS-384 具有抗癌活性，可以引起细胞周期阻滞、DNA损伤和诱导细胞凋亡 (apoptosis)。WS-38 可以用于非小细胞肺癌 (NSCLC) 的研究。

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WS-384 Chemical Structure

WS-384 Chemical Structure

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     可免费申领三个不同产品的试用装。

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Customer Review

WS-384 相关抗体

Top Publications Citing Use of Products

查看 Histone Demethylase 亚型特异性产品:

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KDM1/LSD1 KDM2 KDM3 KDM4 KDM5 KDM6

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

WS-384 is a dual LSD1 and DCN1-UBC12 protein-protein interaction inhibitor with oral activity, with IC50 values of 338.79 nM and 14.81 nM, respectively. WS-384 possesses anticancer activity and can cause cell cycle arrest, DNA damage, and induce apoptosis. WS-384 can be used in the research of non-small cell lung cancer (NSCLC)[1].

IC50 & Target

IC50: 338.79 nM (LSD1)[1].
IC50: 14.81 nM (DCN1-UBC12 Protein-protein interaction)[1].
体外研究
(In Vitro)

WS-384 (1-32 μM; 24-72 h) 以时间和剂量依赖方式抑制了 A549 和 H1975 细胞的生长，IC50 在 2.15-6.67 μM 之间，具有抗癌活性[1]。
WS-384 (1-8 μM; 48 h) 在 A549 和 H1975 细胞中通过抑制 cullin 1 的类泛素化修饰和减少 CDKN1A 启动子处的 H3K4 去甲基化，来增加 p21 的基因和蛋白的表达水平，从而诱导细胞周期阻滞在 G2/M 期和细胞凋亡。WS-384 (1-8 μM; 48 h)也可以引起 DNA 损伤[1]。

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

WS-384 相关抗体:

Apoptosis Analysis[1]

Cell Line: A549, H1975
Concentration: 1 μM, 2 μM, 4 μM, 8 μM (A549);
0.5 μM, 1 μM, 2 μM, 4 μM (H1975)
Incubation Time: 48 h
Result: Increased the apoptosis rate in a concentration-dependent manner, with the apoptosis rate of A549 cells reaching 44.9% at a concentration of 8 μM and the apoptosis rate of H1975 cells reaching 36.42% at a concentration of 4 μM.

Western Blot Analysis[1]

Cell Line: A549, H1975
Concentration: 2 μM, 4 μM, 8 μM (A549);
1 μM, 2 μM, 4 μM (H1975)
Incubation Time: 48 h
Result: Blocked the neddylation of cullin1 and cullin3 but had no effect on the neddylation of other cullin members (cullin2, cullin4A, and cullin5).
Increased the proteins expression of cleaved caspase 3, cleaved caspase 7, cleaved caspase 9, and cleaved PARP.
Decreased the protein expression of p-CDC2, cyclin B1. CDK4 and CDK6.
Increased the protein expression γ-H2AX (a marker protein of DNA damage).
体内研究
(In Vivo)

WS-384 (25-50 mg/kg; p.o.; Once daily for 36 consecutive days) 在 BALB/c 裸鼠异种移植模型中能有效抑制 NSCLC 肿瘤的生长，且毒性较低[1]。

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

Animal Model: BALB/c nude mice xenograft model[1].
Dosage: 25 mg/kg; 50 mg/kg;
Administration: Oral gavage (p.o.); Once daily for 36 consecutive days
Result: Significantly reduced tumor weight and volume in mice in the 50 mg/kg group.
Had no significant toxic effects on the heart, liver, spleen, lungs, and kidneys.
分子量

542.91

Formula

C18H21BrClN9S2
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-384 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)

质量   浓度   体积   分子量 *
= × ×

The dilution calculator equation

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

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
C1   V1   C2   V2
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-384WS384WS 384Histone DemethylaseE1/E2/E3 EnzymeDNA/RNA SynthesisCaspaseApoptosisE1 activating enzymeE2 conjugating enzymeE3 ligating enzymeUbiquitin activating enzymeUbiquitin conjugating enzymeUbiquitin ligasenon-small cell lung cancer (NSCLC)A549H1975apoptosiscell cycle arrestDNA damageInhibitorinhibitorinhibit

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目录号：
HY-161470
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