2. Immunology/Inflammation NF-κB MAPK/ERK Pathway
  3. Toll-like Receptor (TLR) NF-κB p38 MAPK
  4. SMU-R39

SMU-R39 是一种 TLR7 和 TLR8 拮抗剂，IC50 值分别为 3.22 μM 和 0.24 μM。SMU-R39 可结合重组 mTLR7 蛋白 (KD = 2.36 μM) 及重组 hTLR8 蛋白 (KD = 105 nM)。SMU-R39 可抑制下游 NF-κB 和 MAPK 信号通路，并减少 PBMCs 和 THP-1 细胞中促炎性细胞因子 (TNF-α, IL-1β, IL-6) 的分泌及转录。SMU-R39 在 Imiquimod (IMQ) (HY-B0180) 诱导的银屑病小鼠模型中显示出抗炎活性。SMU-R39 可用于银屑病等自身免疫疾病的研究。

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

SMU-R39

SMU-R39 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

SMU-R39 相关抗体

Top Publications Citing Use of Products

查看 Toll-like Receptor (TLR) 亚型特异性产品:

查看所有亚型
TLR3 TLR8 TLR9 TLR2 TLR4 TLR7 TLR1 TLR6

查看 NF-κB 亚型特异性产品:

查看所有亚型
NF-κB NF-κB1/p50 RelA/p65 RelB c-Rel

查看 p38 MAPK 亚型特异性产品:

查看所有亚型
p38 MAPK p38α p38β MAPK13 p38δ p38γ

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

SMU-R39 is a TLR7 and TLR8 antagonist with IC50 values of 3.22 μM and 0.24 μM, respectively. SMU-R39 binds to recombinant mTLR7 protein (KD = 2.36 μM) and to recombinant hTLR8 protein (KD = 105 nM). SMU-R39 suppresses downstream NF-κB and MAPK signaling, and reduces secretion/transcription of pro-inflammatory cytokines (TNF-α, IL-1β, IL-6) in PBMCs and THP-1 cells. SMU-R39 demonstrates anti-inflammatory efficacy in Imiquimod (IMQ) (HY-B0180)-induced psoriasis mouse model. SMU-R39 can be used for the study of autoimmune diseases such as psoriasis[1].

IC50 & Target[1]

TLR7

2.36 μM (Kd)

TLR8

105 nM (Kd)

TLR7

3.22 μM (IC50)

TLR8

0.24 μM (IC50)

体外研究
(In Vitro)

SMU-R39 (0.1-30 μM, 24 h) 在 HEK-Blue hTLR8 细胞中对 R848 诱导的 SEAP 信号显示出强抑制活性 (IC50 = 0.24 μM)，在 HEK-Blue hTLR7 细胞中显示中等抑制活性 (IC50 = 3.22 μM)[1]。
SMU-R39 (0.01-10 μM, 24 h) 显著阻断 THP1-Dual 细胞中 Resiquimod (R848) (HY-13740) 诱导的 SEAP 信号升高，IC50 为 0.18 μM，显示其通过 TLR7/8 信号抑制 NF-κB 激活的能力[1]。
SMU-R39 (0.046-100 μM, 24 h) 对 HEK-Blue hTLR7/8 和 THP1-Dual 细胞中 R848 激活的 TLR7/8 活性呈剂量依赖性抑制\[1]。
SMU-R39 (5-10 μM, 0.5 h) 下调 R848 刺激的 THP-1 巨噬细胞中磷酸化 IKKα/β、p65 和 p38 蛋白的表达水平，抑制 TLR7/8 下游 NF-κB 和 MAPK 信号通路[1]。
SMU-R39 (0.1-20 μM, 24 h) 显著降低 R848 刺激的 THP-1 巨噬细胞、Raw 264.7 细胞及 PBMCs 中 TNF-α 的分泌，呈浓度依赖性\[1]。
SMU-R39 (0.1-20 μM, 6 h) 有效降低 R848 刺激的 THP-1 巨噬细胞及 PBMCs 中 TNF-α、IL-1β、IL-8、IL-6 和 IFN-β 的基因表达[1]。

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

SMU-R39 相关抗体:

Real Time qPCR[1]

Cell Line: R848-stimulated THP-1 macrophages and PBMCs
Concentration: 0.1, 1, 10, 20 μM
Incubation Time: 6 h
Result: Decreased the gene expression of TNF-α, IL-1β, IL-8, IL-6, and IFN-β in R848-stimulated THP-1 macrophages and PBMCs[1].

Western Blot Analysis[1]

Cell Line: R848-stimulated THP-1 macrophages
Concentration: 5, 10 μM
Incubation Time: 0.5 h
Result: Downregulated the expression levels of phosphorylated IKKα/β, p65, and p38 proteins in R848-stimulated THP-1 macrophages [1].
体内研究
(In Vivo)

SMU-R39 (0.5%-1.0% 软膏，局部给药，每日一次，7 天) 显著缓解雌性 BALB/c 小鼠中 Imiquimod (IMQ) (HY-B0180) 诱导的银屑病皮肤炎症\[1]。

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

Animal Model: IMQ-induced psoriasis mouse model: 5% Imiquimod (IMQ) ointment (62.5 mg) was topically applied to the hairless dorsal skin of 8-12-week-old female BALB/c mice once daily for 7 consecutive days[1]
Dosage: 0.5%, 1.0% ointment
Administration: topical, once daily, 7 days
Result: Achieved a psoriasis area and severity index (PASI) reduction.
Showed no significant changes in body weight.
Reduced the Ki67 expression.
Downregulated the gene expression of skin TNF-α, IFN-α , IL-17 , IL-22 , and IL-23 .
Achieved an epidermal thickness reduction.
分子量

387.48

Formula

C23H25N5O
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

SMU-R39 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:

SMU-R39Toll-like Receptor (TLR)NF-κBp38 MAPKNuclear factor-κBNuclear factor-kappaBpsoriasisTLR7TLR8MAPKPBMCsTHP-1 cellsInhibitorinhibitorinhibit

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：
SMU-R39
目录号：
HY-175782
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