2. Metabolic Enzyme/Protease Apoptosis
  3. Proteasome Apoptosis
  4. UK-101

UK-101 是一种强有力的和有选择性的免疫蛋白酶体 β1i (LMP2) 的抑制剂 (IC50=104 nM)。UK-101 对 LMP2 的选择性是 β1c (IC50=15 μM) 和 β5 (IC50=1 μM) 亚基的 144 倍和 10 倍。UK-101 可以诱导细胞凋亡 (apoptosis)，可用于前列腺癌的相关研究。

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UK-101 Chemical Structure

UK-101 Chemical Structure

CAS No. : 1000313-40-5

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规格 价格 是否有货 数量
1 mg ￥2900
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5 mg ￥5400
In-stock
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Customer Review

UK-101 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

UK-101 is a potent and selective immunoproteasome β1i (LMP2) inhibitor with an IC50 value of 104 nM, displays 144- and 10-fold selectivity over β1c (IC50=15 μM) and β5 subunit (IC50=1 μM), respectivey[1]. UK-101 induces cell apoptosis and can be used for the study of prostate cancer[2].

IC50 & Target

IC50: 104 nM (LMP2)
IC50: 15 μM (immunoproteasome β1c)
IC50: 1 μM (immunoproteasome β5)[1]
细胞效力
(Cellular Effect)
Cell Line Type Value Description References
NCI-H23 IC50
3.37 μM
Compound: UK101
Cytotoxicity against human NCI-H23 cells after 72 hrs by CellTiter 96 AQueous one solution cell proliferation assay
Cytotoxicity against human NCI-H23 cells after 72 hrs by CellTiter 96 AQueous one solution cell proliferation assay
[PMID: 30964987]
NCI-H727 IC50
5.21 μM
Compound: UK101
Cytotoxicity against human NCI-H727 cells after 72 hrs by CellTiter 96 AQueous one solution cell proliferation assay
Cytotoxicity against human NCI-H727 cells after 72 hrs by CellTiter 96 AQueous one solution cell proliferation assay
[PMID: 30964987]
Raji IC50
0.104 μM
Compound: 38
Inhibition of proteasome subunit beta-1i in human Raji cells using BODIPY- epoxomicin by fluorescent densitometry
Inhibition of proteasome subunit beta-1i in human Raji cells using BODIPY- epoxomicin by fluorescent densitometry
[PMID: 25006746]
Raji IC50
15 μM
Compound: 38
Inhibition of 20s proteasome subunit beta-1c in human Raji cells using BODIPY- epoxomicin by fluorescent densitometry
Inhibition of 20s proteasome subunit beta-1c in human Raji cells using BODIPY- epoxomicin by fluorescent densitometry
[PMID: 25006746]
Raji IC50
25 μM
Compound: 38
Inhibition of proteasome subunit beta-2i in human Raji cells using BODIPY- epoxomicin by fluorescent densitometry
Inhibition of proteasome subunit beta-2i in human Raji cells using BODIPY- epoxomicin by fluorescent densitometry
[PMID: 25006746]
RPMI-8226 IC50
2.14 μM
Compound: UK101
Cytotoxicity against human RPMI8226 cells after 72 hrs by CellTiter 96 AQueous one solution cell proliferation assay
Cytotoxicity against human RPMI8226 cells after 72 hrs by CellTiter 96 AQueous one solution cell proliferation assay
[PMID: 30964987]
体外研究
(In Vitro)

UK-101 (2-8 μM; 24 hours) induces cell cycle arrest and increases the number of the PC-3 cells arrest in G1 phase of the cell cycle[2].
UK-101 (2-8 μM; 24 hours) induces cell apoptosis, shows a minimal increase in late apoptosis, but has no significant increase in early apoptosis[2].
UK-101 (1-8 μM; 24 hours) induces cells accumulation in the G1 phase of the cell cycle, it increases p27 accumulation and significantly increases PARP cleavage as a dose-dependent manner[2].

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

UK-101 相关抗体:

Cell Cycle Analysis[1]

Cell Line: PC-3 cells
Concentration: 2 μM; 8 μM
Incubation Time: 24 hours
Result: Induced G1 cell cycle arrest in PC-3 cells.

Apoptosis Analysis[1]

Cell Line: PC-3 cells
Concentration: 2 μM; 8 μM
Incubation Time: 24 hours
Result: Increased cell apoptosis as a dose-dependent manner.

Western Blot Analysis[1]

Cell Line: PC-3 cells
Concentration: 1 μM; 2 μM; 8 μM
Incubation Time: 24 hours
Result: Increased PARP cleavage and p27 accumulation as a dose-dependent manner.
体内研究
(In Vivo)

UK-101 (intraperitoneal injection; 1-3 mg/kg; twice a week; 3 weeks) decreases tumor volume as a dose-dependent manner, it significantly decreases tumor volume at a dose of 3 mg/kg. Additionally, UK-101-treated mice is suffering less systemic toxicity and the weights of mice treated with UK-101 remains steady over the 3-week treatment period[2].

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

Animal Model: Subcutaneously implanted PC-3 cells in 6-week-old male BALB/c athymic nude mice[2]
Dosage: 1 mg/kg; 3 mg/kg
Administration: Intraperitoneal injection; twice a week; 3 weeks
Result: Inhibited tumour growth in the prostate cancer mouse xenograft model.
分子量

484.74

Formula

C25H48N2O5Si
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
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
细胞实验： 

DMSO 中的溶解度 : 7.3 mg/mL (15.06 mM; 超声加热助溶; 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 2.0630 mL 10.3148 mL 20.6296 mL
5 mM 0.4126 mL 2.0630 mL 4.1259 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。-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

只
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

UK-101 相关分类

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。-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 2.0630 mL 10.3148 mL 20.6296 mL 51.5740 mL
5 mM 0.4126 mL 2.0630 mL 4.1259 mL 10.3148 mL
10 mM 0.2063 mL 1.0315 mL 2.0630 mL 5.1574 mL
15 mM 0.1375 mL 0.6877 mL 1.3753 mL 3.4383 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.

Keywords:

UK-1011000313-40-5UK101UK 101ProteasomeApoptosisInhibitorinhibitorinhibit

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