2. Immunology/Inflammation Apoptosis
  3. PD-1/PD-L1 Bcl-2 Family MDM-2/p53 Caspase
  4. CSN5-IN-3

CSN5-IN-3 (Compound 30) 是一种 CSN5 抑制剂，其 IC50 为 0.58 μM。CSN5-IN-3 可抑制 CSN5 的酶活性，导致 NEDD8-Cul1 积累增加并促进 PD-L1 降解。CSN5-IN-3 可下调 Bcl-2， 上调 P53 和 Cleaved caspase-3。CSN5-IN-3 对三阴性乳腺癌具有抗癌活性。

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CSN5-IN-3

CSN5-IN-3 Chemical Structure

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CSN5-IN-3 相关抗体

Top Publications Citing Use of Products

查看 Bcl-2 Family 亚型特异性产品:

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Bcl-2 Bcl-xL Bcl-W Mcl-1 Bfl-1 Bcl-B Bax Bak Bim BNIP3 Bad

查看 Caspase 亚型特异性产品:

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Caspase 1 Caspase 2 Caspase 3 Caspase 4 Caspase 5 Caspase 6 Caspase 7 Caspase 8 Caspase 9 Caspase 10 Caspase 12 Caspase Caspase 11 Caspase-13

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

CSN5-IN-3 (Compound 30) is a CSN5 inhibitor with an IC50 of 0.58 μM. CSN5-IN-3 inhibits the enzymatic activity of CSN5, leading to increased accumulation of NEDD8-Cul1 and promoting the degradation of PD-L1. CSN5-IN-3 downregulates Bcl-2, and upregulates P53 and Cleaved caspase-3. CSN5-IN-3 exhibits anticancer activity against triple-negative breast cancer[1].

IC50 & Target[1]

Caspase 3

 

Bcl-2

 

CSN5

0.58 μM (IC50)

体外研究
(In Vitro)

CSN5-IN-3 (20 min) 在无细胞荧光偏振实验中可作为强效 CSN5 抑制剂，其 IC50 为 0.58 μM[1]。
CSN5-IN-3 (72 h) 可强效抑制 MDA-MB-231 细胞活力，IC50 为 2.1 μM[1]。

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

CSN5-IN-3 相关抗体:

Western Blot Analysis[1]

Cell Line: MDA-MB-231 human triple-negative breast cancer cells
Concentration: 2.5-20 μM (direct treatment); 10 μM (following 2 h preincubation with MG132 or MLN4924)
Incubation Time: 12 h
Result: Dose-dependently increased NEDD8-Cul1 protein levels while not altering CSN5 expression.
Dose-dependently reduced PD-L1 protein levels.
Dose-dependently upregulated P53, and cleaved caspase-3 protein levels.
Dose-dependently downregulated Bcl-2 protein levels.

Cell Cycle Analysis[1]

Cell Line: MDA-MB-231 human triple-negative breast cancer cells
Concentration: 1-10 μM
Incubation Time: 24 h
Result: Caused no significant change in G0/G1 phase cell percentage at 1 μM.
Increased G0/G1 phase cell percentage by 9.6% compared to control at 5 μM (p < 0.01).
Increased G0/G1 phase cell percentage by 18.3% compared to control at 10 μM (p < 0.001).
体内研究
(In Vivo)

CSN5-IN-3 (8-16 mg/kg；腹腔注射；每 3 天 1 次；共 21 天) 在小鼠中对 MDA-MB-231 异种移植物具有剂量依赖性的强效体内抗肿瘤活性[1]。

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

Animal Model: BALB/c nude (female, 4 weeks old, triple-negative breast cancer subcutaneous xenograft model)[1]
Dosage: 8 mg/kg; 16 mg/kg
Administration: i.p.; every 3 days; 21 days
Result: Achieved 68.3% tumor growth inhibition (TGI) at 8 mg/kg.
Achieved 89.3% tumor growth inhibition (TGI) at 16 mg/kg.
Showed no mortality in either treatment group.
Exhibited no significant body weight changes in the low-dose group; caused a slight temporary body weight decrease but no significant end-of-study weight loss in the high-dose group.
Reduced PD-L1 and Ki67 expression, and increased P21 expression in excised tumors via immunohistochemical analysis.
分子量

441.57

Formula

C27H31N5O
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

CSN5-IN-3 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:

CSN5-IN-3PD-1/PD-L1Bcl-2 FamilyMDM-2/p53CaspasePD-1/Programmed death-ligand 1NEDD8-Cul1Bcl-2CSN5P27P53/Bax-dependent apoptosisPD-L1MDA-MB-231 cellstriple-negative breast cancerG0/G1 cell cycle arrestP21Inhibitorinhibitorinhibit

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