2. Metabolic Enzyme/Protease
  3. Proteasome
  4. Immunoproteasome-IN-2

Immunoproteasome-IN-2 是一种选择性免疫蛋白酶体抑制剂，其对 LMP7 亚基 IC50 值为 232.3 nM，对 β5 亚基的 IC50 值为 9384.9 nM。Immunoproteasome-IN-2 对 LMP2 和 MECL-1 亚基亦具有附属抑制活性。Immunoproteasome-IN-2 在关节炎小鼠模型中免疫蛋白酶体抑制剂 IN-2 表现出抗炎效果，并在毒理学研究中显示出良好的安全性，肝脏毒性和血液毒性均较低。Immunoproteasome-IN-2 的 LMP7/β5 选择性与较低的系统毒性直接相关。Immunoproteasome-IN-2 可用于关节炎相关研究。

MCE 的所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务

Immunoproteasome-IN-2

Immunoproteasome-IN-2 Chemical Structure

1.  客户无需承担相应的运输费用。

2.  同一机构（单位）同一产品试用装仅限申领一次，同一机构（单位）一年内

     可免费申领三个不同产品的试用装。

3.  试用装只面向终端客户。

规格 是否有货
50 mg   询价  
100 mg   询价  
250 mg   询价  

* Please select Quantity before adding items.

Customer Review

Immunoproteasome-IN-2 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

Immunoproteasome-IN-2 is selective immunoproteasome inhibitor with IC50 = 232.3 nM for LMP7, IC50 = 9384.9 nM for β5. Immunoproteasome-IN-2 exhibits ancillary inhibitory activity against LMP2 and MECL-1 subunits. Immunoproteasome-IN-2 demonstrates anti-inflammatory efficacy in a mouse model of arthritis and shows a favorable safety profile in toxicological studies with reduced hepatotoxicity and hematotoxicity. Immunoproteasome-IN-2 has LMP7/β5 selectivity directly correlated with lower systemic toxicity. Immunoproteasome-IN-2 can be employed for research in arthritis[1].

体外研究
(In Vitro)

Immunoproteasome-IN-2 (compound A33) (1.37-3000 nM) 在 Molt-4 细胞（人白血病 T 细胞）中对各免疫蛋白酶体亚基均具有抑制活性，其对 LMP7 的 IC50 为 12.5 nM，对 β5 的 IC50 为 2022.3 nM，对 LMP2 的 IC50 为 1043.7 nM，对 MECL-1 的 IC50 为 570.2 nM[1]。
Immunoproteasome-IN-2 (1.37-3000 nM) 在小鼠 B 淋巴瘤细胞中与 LMP7 表现出优异的结合效率，且与 LMP7 形成共价键的速度快于与 β5 的结合 (LMP7 的 KI = 1.10 × 100 μM，β5 的 KI = 2.07 × 101 μM）[1]。
Immunoproteasome-IN-2 的心脏毒性风险较低，其在 HEK293 hERG 细胞中对 HERG 通道的 IC50 大于 30 μM；对免疫蛋白酶体亚基具有突出选择性而对 β1 (IC50 > 30μM) 和 β1 (IC50 > 30 μM) 亚基无抑制活性[1]。

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

Immunoproteasome-IN-2 相关抗体:
药代动力学
(Parmacokinetics)
Species Dose Route C0 T1/2 AUC0-t AUC0-inf CL Vdss
Mice 5 mg/kg i.v. 88000 ng/mL 12.2 min 929 ng·h/mL 932 ng·h/mL 90.1 mL/min/kg 0.88 L/kg
体内研究
(In Vivo)

Immunoproteasome-IN-2 (compound A33) (5 mg/kg，静脉注射，每周三次持续两周) 在 BALB/c 小鼠抗胶原抗体诱导性关节炎 (CAIA) 模型中表现出强效的抗炎活性[1]。
Immunoproteasome-IN-2 (20 mg/kg) 未导致任何 SD 大鼠死亡并且在血液学分析中维持淋巴细胞、血小板和网织红细胞的水平处于正常波动范围内[1]。
Immunoproteasome-IN-2 (5 mg/kg，静脉注射) 在 BALB/c 小鼠脾脏中对 LMP7 具有抑制活性 (相对活性为 1.5 %)，对 LMP2 和 MECL-1 具有中等抑制效果 (相对活性分别为 44.5 % 和 49.2 % )，在肾脏中对 β5 亚基的抑制效力较低 (相对活性为 76.9% )[1]。
Immunoproteasome-IN-2 (5-20 mg/kg，静脉注射，每周两次连续四周) 在 SD 大鼠中显示出良好的安全性特征[1]。

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

Animal Model: anticollagen antibody-induced arthritis (CAIA) induced in BALB/c mice[1]
Dosage: 5 mg/kg
Administration: i.v., three times weekly for 2 weeks
Result: Reduce the thickness of the paws, and the final CAIA score was less than 5.
Did not cause death or significant weight loss.
Exerted its efficacy by inhibiting the LMP2 and MECL-1 subunits, but not LMP7.
Animal Model: SD Rats[1]
Dosage: 5 mg/kg, 10 mg/kg, and 20 mg/kg
Administration: i.v., twice weekly for four consecutive weeks
Result: Observed no mortality at any dosage.
Did not induce any significant adverse effects on hematological parameters or liver function across all tested doses.
分子量

612.71

Formula

C32H44N4O8
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

Immunoproteasome-IN-2 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:

Immunoproteasome-IN-2ProteasomeLMP7β5LMP2MECL-1inflammatory efficacyLMP7/β5arthritis.Inhibitorinhibitorinhibit

您最近查看的产品:

Your information is safe with us. * Required Fields.

   产品名称：

  

* 需求量：

* 客户姓名：

 

* Email：

* 电话：

 

* 公司或机构名称：

   留言给我们：

Bulk Inquiry

Inquiry Information

产品名称：
Immunoproteasome-IN-2
目录号：
HY-179394
需求量：

Request for HNMR Report

Please fill out this form to request the QC report. We will send it to your Email address shortly.

Your information is safe with us. * Required Fields.

   产品名称：

  

* Lot #：

* 客户姓名：

 

* Email：

   电话：

 

* 部门：

* 公司或机构名称：

 

   留言给我们：

Request for HNMR Report

We have received your request and will respond to you as soon as possible.

嗨！很高兴为您提供帮助！

尊敬的 MCE 客户您好，
请您选择所在区域，我们将转接对应客服为您服务！

热门区域

A

B

C

F

G

H

J

L

N

Q

S

T

X

Y

Z

热 A B C F G H J L N Q S T X Y Z