1. PROTAC Immunology/Inflammation GPCR/G Protein Metabolic Enzyme/Protease
  2. PROTACs CCR E1/E2/E3 Enzyme
  3. PROTAC CCR9 Degrader 1

PROTAC CCR9 Degrader 1 是靶向 CCR9 PROTAC 类降解剂。PROTAC CCR9 Degrader 1 通过招募 VHL E3 连接酶来诱导 CCR9 泛素化、蛋白酶体降解并降低细胞内 CCR9 水平。PROTAC CCR9 Degrader 1 对人源 CCR9Ki 值为 78.0 nM。PROTAC CCR9 Degrader 1 可通过结合 CCR9 的细胞内变构结合位点来调控 GPCR 活性。PROTAC CCR9 Degrader 1 可用于克罗恩病的相关研究

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PROTAC CCR9 Degrader 1

PROTAC CCR9 Degrader 1 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

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Customer Review

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

PROTAC CCR9 Degrader 1 is a PROTAC-based degrader targeting CCR9. PROTAC CCR9 Degrader 1 induces ubiquitination, proteasomal degradation of CCR9 and reduces intracellular CCR9 levels by recruiting the VHL E3 ligase. PROTAC CCR9 Degrader 1 has a Ki value of 78.0 nM against human CCR9. PROTAC CCR9 Degrader 1 modulates GPCR activity by binding to the intracellular allosteric binding site of CCR9. PROTAC CCR9 Degrader 1 can be used in research related to Crohn's disease[1][2].

IC50 & Target

CCR9

78.0 nM (Ki)

VHL

 

体外研究
(In Vitro)

PROTAC CCR9 Degrader 1 (compound 13) 可在活 HEK293T 细胞中结合 CCR9 的细胞内变构结合位点 (IABS),其 Ki 值为 151 nM[1]
PROTAC CCR9 Degrader 1 (0.1-10000 nM) 可在 HEK293T 细胞中诱导细胞表面 CCR9 呈浓度依赖性降解,10 nM 浓度时达到 DCmax,>10 nM 时出现钩状效应[1]
PROTAC CCR9 Degrader 1 对 CCR2CCR7CCR9 具有选择性,无细胞毒性[1]
PROTAC CCR9 Degrader 1 (PROTAC in Figure 8) 在基于细胞的实验中可适度降解 CCR9,相对于 CCR2CCR7 具有极佳的选择性[2]

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

Cell Cytotoxicity Assay[1]

Cell Line: HEK293T cells
Concentration: 0.1, 1, 10, 25, 100, 500, 1000, 2500 nM
Incubation Time: 48 h
Result: Showed no cytotoxicity in cells.
Selectively induced a reduction in CCR9
levels, without affecting the levels of the related chemokine receptors CCR2 and CCR7.
分子量

1144.75

Formula

C55H66ClN9O12S2

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
  • 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.

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产品名称:
PROTAC CCR9 Degrader 1
目录号:
HY-181287
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