2. Cell Cycle/DNA Damage Apoptosis
  3. Deubiquitinase Apoptosis
  4. LLK203

LLK203 是一种有效的 USP2/USP8 双靶点抑制剂，IC50 分别为 0.89 μM 和 0.52 μM。LLK203 导致 ERα 降解并诱导乳腺癌 MCF-7 细胞凋亡。LLK203 对 4T1 肿瘤小鼠模型具有抗肿瘤活性。

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LLK203 Chemical Structure

LLK203 Chemical Structure

CAS No. : 2758090-62-7

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LLK203 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

LLK203 is a potent USP2/USP8 dual-target inhibitor with IC50s of 0.89 μM and 0.52 μM, respectively. LLK203 leads a degradation of ERα and induces apoptosis of breast cancer MCF-7 cells. LLK203 demonstrates antitumor activities against the 4T1 tumor mice model[1].

IC50 & Target[1]

USP2

0.89 μM (IC50)

USP8

0.52 μM (IC50)

体外研究
(In Vitro)

LLK203 (0-100 μM；36小时) 对 MCF-7 细胞具有高抑制活性 (IC50=3.4 μM)，比 ML364 (IC50=9.3 μM) 靶向性更强。与 ML364 (HY-100900) 相比，LLK203 对 USP2 的活性增加了 4 倍，USP8 活性增加了 9 倍[1]。
LLK203 (10-50 μM；24 小时) 可增加 MCF-7 细胞凋亡细胞的比例，并大部分保持在 G1 期[1]。
LLK203 (2-50 μM；24 小时) 可以以剂量依赖性方式降解各种蛋白质 (MDM2、Cyclin D1、Her2、ERα)[1]。
LLK203 (2-50 μM；持续 7 天) 在 10 μM 浓度下表现出强大的抑制克隆形成的能力[1]。

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

LLK203 相关抗体:

Cell Cytotoxicity Assay[1]

Cell Line: MCF-7 and MCF10A cells
Concentration: 0-100 μM
Incubation Time: 36 h
Result: Exhibited lower cytotoxicity towards normal cells (MCF10A; IC50=20.4 μM), while demonstrating higher inhibitory activity on BC cells (MCF-7; IC50=3.4 μM).

Apoptosis Analysis[1]

Cell Line: MCF-7 cells
Concentration: 10, 30, 50 μM
Incubation Time: 24 h
Result: Increased the ratio of apoptotic cells.

Cell Cycle Analysis[1]

Cell Line: MCF-7 cells
Concentration: 10, 30, 50 μM
Incubation Time: 24 h
Result: Remained largely in G1 phase.

Western Blot Analysis[1]

Cell Line: MCF-7 cells
Concentration: 2, 5, 10, 30, 50 μM
Incubation Time: 24 h
Result: Could degrade various proteins (MDM2, Cyclin D1, Her2, ERα) in a dosedependent manner.
体内研究
(In Vivo)

LLK203 (20 mg/kg；腹腔；每天；持续 23 天) 显着减少 4T1 荷瘤小鼠模型中的肿瘤生长[1]。
Pharmacokinetic Parameters of LLK203 in male Sprague-Dawley rats[1].

Intravenously (5 mg/kg) Orally (50 mg/kg)
Tmax (h) 6
Cmax (ng/mL) 36630 1572
AUC0-t (h∗ng/mL) 60824 19144
T1/2 (h) 20 6.14
CL (mL/h/kg) 58
F (%) 2.2%

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

Animal Model: BALB/c mice subcutaneously inoculated with 4T1 cells[1]
Dosage: 20 mg/kg
Administration: Intraperitoneal; every day; for 23 days
Result: Significantly reduced tumor growth in a 4T1 tumor-bearing mice model.
分子量

561.69

Formula

C28H23N3O4S3
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

LLK203 相关分类

  • 摩尔计算器

  • 稀释计算器

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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:

LLK2032758090-62-7LLK 203LLK-203DeubiquitinaseApoptosisDUBsUSP2USP8ERαbreast cancerMCF-74T1 tumorInhibitorinhibitorinhibit

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