2. PROTAC Immunology/Inflammation NF-κB
  3. PROTACs STING NF-κB IKK
  4. PROTAC STING degrader-4

PROTAC STING degrader-4 是一种不含硝基的共价 STING PROTAC 降解剂，DC50 为 3.23 μM。PROTAC STING degrader-4 可有效抑制 STING 及其下游信号传导，例如 p-TBK1 和 p-NF-κB (p-P65) 以及免疫炎症细胞因子。PROTAC STING degrader-4 可减轻 Cisplatin (HY-17394) 诱发的急性肾损伤 (AKI) 小鼠模型中的肾脏和血液炎症。粉色：STING ligand (HY-176183)；蓝色：CRBN ligase ligand (HY-103596)；黑色：linker (HY-176182)；CRBN ligase ligand + linker：HY-176181

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

PROTAC STING degrader-4 Chemical Structure

PROTAC STING degrader-4 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

PROTAC STING degrader-4 相关抗体

Top Publications Citing Use of Products

查看 PROTACs 亚型特异性产品:

查看所有亚型
von Hippel-Lindau (VHL) Cereblon MDM2 cIAP1

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 IKK 亚型特异性产品:

查看所有亚型
IKK-α IKK-β IKK IKKε TBK1

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

PROTAC STING degrader-4 is a nitro-free covalent STING PROTAC degrader with a DC50 of 3.23 μM. PROTAC STING degrader-4 effectively inhibits STING as well as its downstream signaling, such as p-TBK1 and p-NF-κB (p-P65), and immune-inflammatory cytokines. PROTAC STING degrader-4 mitigates kidney and blood inflammation in Cisplatin (HY-17394)-induced acute kidney injury (AKI) mice model[1]. Pink: STING ligand (HY-176183); Blue: CRBN ligase ligand (HY-103596); Black: linker (HY-176182); CRBN ligase ligand + linker: HY-176181

IC50 & Target[1]

NF-κB

 

TBK1

 

体外研究
(In Vitro)

PROTAC STING degrader-4 (Compound 2h) (0.6-40 μM，2-72 小时) 以剂量和时间依赖性的方式降解 THP-1 dual 细胞中的 STING，持续 72 小时，其 DC50 为 3.23 μM (24小时)[1]。
PROTAC STING degrader-4 (10 μM，48 小时) 通过蛋白酶体途径诱导 STING 降解[1]。
PROTAC STING degrader-4 (0.3-20 μM，2 小时) 以剂量依赖性的方式降低 p-TBK1 和 p-NF-κB (p-P65) 的蛋白水平，从而抑制 STING 下游信号级联，而非直接降解 STING[1]。
PROTAC STING degrader-4 (0.6-20 μM，2 小时) 显著且剂量依赖性地降低 IFN-β 和 CXCL10 的产生，并抑制 THP1-Dual 细胞中 IFNB1、CXCL10 和 ISG15 的 mRNA 表达[1]。
PROTAC STING degrader-4 (0.03-30 μM，24-48 小时) 在 THP1-Dual 和 RAW-Lucia 细胞 (低于 20 μM) 以及人类和小鼠正常细胞 (低于 30 μM) 中均表现出没有或弱细胞毒性[1]。

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

PROTAC STING degrader-4 相关抗体:

Western Blot Analysis[1]

Cell Line: THP-1 dual cells
Concentration: 0.6, 1.2, 2.5, 5, 10, 20, 40 μM
Incubation Time: 2, 4, 8, 12, 24, 48, 72 h
Result: Dose-dependently degraded STING with a DC50 of 3.23 μM (24 h) in THP-1 dual cells.
Continuously reduced the expression level of STING in THP1-dual cells for 72 h in THP-1 dual cells.
Induced potent degradation of STING, and this degradation effect was not inhibited by lysosome inhibitor BAF (Bafilomycin A1) (HY-100558) but was reversed by proteasome inhibitor MG132 (HY-13259) Induced the degradation of STING via the proteasome pathway rather than its warhead molecule or E3 ligase ligand, BAF (a lysosome inhibitor) and MG132 (a proteasome inhibitor).

Western Blot Analysis[1]

Cell Line: THP-1 dual cells
Concentration: 0.3, 0.6, 1.25, 2.5, 5, 10, 20 μM
Incubation Time: 2 h following MSA-2 (10 μM) for 16 h
Result: Dose-dependently reduced protein levels of p-TBK1 and p-NF-κB (p-p65), suppressing the STING downstream signaling cascade beyond direct degradation of STING.

Real Time qPCR[1]

Cell Line: THP-1 dual cells
Concentration: 0.6, 1.25, 2.5, 5, 10, 20 μM
Incubation Time: 2 h following MSA-2 (10 μM) for 24 h
Result: Significantly and dose-dependently inhibited IFNB1, CXCL10 and ISG15 mRNA expression in THP1-Dual cells.

Cell Viability Assay[1]

Cell Line: THP1-Dual, RAW-Lucia cells, human normal cell lines (HEK293T and WI38VA-13) and mouse normal cell lines (HT22 and MEF).
Concentration: 0.03, 0.07, 0.15, 0.31, 0.62, 1.25, 2.5, 5, 10, 20 μM (THP1-Dual and RAW-Lucia cells), 1.1, 3.3, 10, 30 μM (four human and mouse normal cell lines)
Incubation Time: 24, 48 h
Result: Did not exhibit significant inhibition of cellular viability below 20 μM in THP1-Dual and RAW-Lucia cells.
Exhibited no or weak cytotoxicity against four human and mouse cell lines at concentrations below 30 μM.
体内研究
(In Vivo)

PROTAC STING degrader-4 (Compound 2h) (30 mg/kg，腹腔注射，每日一次，持续 3 天) 通过降解 STING 和下游信号通路 (例如 p-IRF3) 显著缓解 Cisplatin 诱发的 AKI 小鼠模型中肾脏炎症[1]。

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

Animal Model: Male C57BL/6 mice (8 weeks old) were given Cisplatin administration (15 mg/kg) 1 h after PROTAC STING degrader-4 to induce AKI mice model[1].
Dosage: 30 mg/kg
Administration: i.p., daily for 3  days and then collected blood and kidney samples after cisplatin induction1.
Result: Potently mitigated ischemic symptoms of kidneys.
Significantly reduced the protein level of STING and p-IRF3 in kidney tissues.
Effectively reduced the mRNA levels of Tnfα, Isg15 and Cxcl10.
Effectively suppressed the production of CXCL10, IFN-β, IL-6 in plasma.
分子量

837.70

Formula

C39H42Cl2N8O9
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

PROTAC STING degrader-4 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:

PROTAC STING degrader-4PROTAC STING degrader4PROTAC STING degrader 4PROTACsSTINGNF-κBIKKStimulator of Interferon GenesTMEM173MITAERISMPYSNuclear factor-κBNuclear factor-kappaBIκB kinaseI kappa B kinasePROTACDegradationInflammatoryAutoimmune diseasesAKI modelInhibitorinhibitorinhibit

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：
PROTAC STING degrader-4
目录号：
HY-176180
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