Pom-8PEG

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白,专注于信号通路和疾病研究领域。

Pom-8PEG 

Pom-8PEG,一种 E3 连接酶配体-linker 偶联物,包含一个用于 E3 泛素连接酶的 cereblon (CRBN) 配体和一个 8 单元 PEG 连接子。Pom-8PEG 可用于合成 PROTAC,如 IDO1 PROTAC 降解剂。

Pom-8PEG

Pom-8PEG Chemical Structure

CAS No. : 2488761-03-9

规格 价格 是否有货 数量
50 mg ¥10500 In-stock
100 mg ¥17000 In-stock
200 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

生物活性

Pom-8PEG, an E3 ligase ligand-linker conjugate, incorporates a cereblon (CRBN) ligand for the E3 ubiquitin ligase and an 8-unit PEG linker. Pom-8PEG can be used in the synthesis of PROTAC, such as IDO1 PROTAC degrader[1].

IC50 & Target[1]

Cereblon

 

分子量

625.66

Formula

C29H43N3O12

CAS 号

2488761-03-9

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

-20°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

参考文献
  • [1]. Hu M, et al. Discovery of the first potent proteolysis targeting chimera (PROTAC) degrader of indoleamine 2,3-dioxygenase 1. Acta Pharm Sin B. 2020;10(10):1943-1953.

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

Pom-8PEG

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白,专注于信号通路和疾病研究领域。

Pom-8PEG 

Pom-8PEG,一种 E3 连接酶配体-linker 偶联物,包含一个用于 E3 泛素连接酶的 cereblon (CRBN) 配体和一个 8 单元 PEG 连接子。Pom-8PEG 可用于合成 PROTAC,如 IDO1 PROTAC 降解剂。

Pom-8PEG

Pom-8PEG Chemical Structure

CAS No. : 2488761-03-9

规格 价格 是否有货 数量
50 mg ¥10500 In-stock
100 mg ¥17000 In-stock
200 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

生物活性

Pom-8PEG, an E3 ligase ligand-linker conjugate, incorporates a cereblon (CRBN) ligand for the E3 ubiquitin ligase and an 8-unit PEG linker. Pom-8PEG can be used in the synthesis of PROTAC, such as IDO1 PROTAC degrader[1].

IC50 & Target[1]

Cereblon

 

分子量

625.66

Formula

C29H43N3O12

CAS 号

2488761-03-9

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

-20°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

参考文献
  • [1]. Hu M, et al. Discovery of the first potent proteolysis targeting chimera (PROTAC) degrader of indoleamine 2,3-dioxygenase 1. Acta Pharm Sin B. 2020;10(10):1943-1953.

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

Pom-8PEG

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白,专注于信号通路和疾病研究领域。

Pom-8PEG 

Pom-8PEG,一种 E3 连接酶配体-linker 偶联物,包含一个用于 E3 泛素连接酶的 cereblon (CRBN) 配体和一个 8 单元 PEG 连接子。Pom-8PEG 可用于合成 PROTAC,如 IDO1 PROTAC 降解剂。

Pom-8PEG

Pom-8PEG Chemical Structure

CAS No. : 2488761-03-9

规格 价格 是否有货 数量
50 mg ¥10500 In-stock
100 mg ¥17000 In-stock
200 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

生物活性

Pom-8PEG, an E3 ligase ligand-linker conjugate, incorporates a cereblon (CRBN) ligand for the E3 ubiquitin ligase and an 8-unit PEG linker. Pom-8PEG can be used in the synthesis of PROTAC, such as IDO1 PROTAC degrader[1].

IC50 & Target[1]

Cereblon

 

分子量

625.66

Formula

C29H43N3O12

CAS 号

2488761-03-9

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

-20°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

参考文献
  • [1]. Hu M, et al. Discovery of the first potent proteolysis targeting chimera (PROTAC) degrader of indoleamine 2,3-dioxygenase 1. Acta Pharm Sin B. 2020;10(10):1943-1953.

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

SCR130

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白,专注于信号通路和疾病研究领域。

SCR130  纯度: 98.00%

SCR130 是一种基于 SCR7 的 DNA 非同源末端连接 (NHEJ) 抑制剂。SCR130 以依赖连接酶 IV 的方式抑制 DNA 的末端连接。SCR130 对连接酶 IV 具有特异性,对连接酶 III 和连接酶 I 介导的连接的影响很小或没有影响。SCR130 诱导细胞凋亡 (apoptosis),并具有抗癌活性。

SCR130

SCR130 Chemical Structure

CAS No. : 2377858-38-1

规格 价格 是否有货 数量
5 mg ¥8500 In-stock
10 mg ¥13600 In-stock
50 mg   询价  
100 mg   询价  

* Please select Quantity before adding items.

SCR130 相关产品

相关化合物库:

  • Bioactive Compound Library Plus
  • Apoptosis Compound Library
  • Cell Cycle/DNA Damage Compound Library
  • Anti-Cancer Compound Library
  • Anti-Aging Compound Library
  • Targeted Diversity Library

生物活性

SCR130 is a SCR7-based DNA nonhomologous end-joining (NHEJ) inhibitor. SCR130 inhibits the end-joining of DNA in a Ligase IV-dependent manner. SCR130 is specific to Ligase IV, and shows minimal or no effect on Ligase III and Ligase I mediated joining. SCR130 induces cell apoptosis and has anticancer activity[1].

体外研究
(In Vitro)

SCR130 (7-21 μM; 48 hours) increase in the number of late and early apoptotic cells. SCR130 induces apoptosis by both intrinsic and extrinsic pathways. SCR130 increases the expression of p-p53, BCL2 and MCL1, and CYTOCHROME C, BAX, and BAK also increaseed. The activation of caspase 8, increase in expression of FAS and SMAC-DIABLO proteins are also observed[1].
SCR130 (48 hours) exhibits cytotoxicity in Reh, HeLa, CEM, Nalm6, and N114 cells with IC50 values of 14.1 μM, 5.9 μM, 6.5 μM, 2.2 μM, and 11 μM, respectively[1].
SCR130 can potentiate the effect of radiation (0.5 and 1 Gy) by inducing enhanced cell death upon coadministration in Reh and Nalm6 cell lines[1].
SCR130 blocks the endogenous NHEJ leading to accumulation of unrepaired DNA breaks. Treatment with SCR130 leads to inhibition of endogenous NHEJ, resulting in the accumulation of DNA double-strand breaks (DSBs) and cell death by activating apoptotic pathways[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Apoptosis Analysis[1]

Cell Line: Reh cells
Concentration: 7 μM, 14 μM, and 21 μM
Incubation Time: 48 hours
Result: Showed a concentration-dependent increase in the number of late and early apoptotic cells.

Western Blot Analysis[1]

Cell Line: Reh cells
Concentration: 7 μM, 14 μM, and 21 μM
Incubation Time: 48 hours
Result: Revealed a concentration-dependent increase in levels of pATM and activation of p53 through phosphorylation.

分子量

418.30

Formula

C19H13Cl2N3O2S

CAS 号

2377858-38-1

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
In Vitro: 

DMSO : 100 mg/mL (239.06 mM; Need ultrasonic and warming)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.3906 mL 11.9531 mL 23.9063 mL
5 mM 0.4781 mL 2.3906 mL 4.7813 mL
10 mM 0.2391 mL 1.1953 mL 2.3906 mL

*

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。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液,再依次添加助溶剂:

——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用; 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂: 10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (5.98 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (5.98 mM,饱和度未知) 的澄清溶液,此方案不适用于实验周期在半个月以上的实验。

    以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。

*以上所有助溶剂都可在 Shanghai Jinpan Biotech Co Ltd 网站选购。
参考文献
  • [1]. Ujjayinee Ray, et al. Identification and characterization of novel SCR7-based small-molecule inhibitor of DNA end-joining, SCR130 and its relevance in cancer therapeutics. Mol Carcinog. 2020 Jun;59(6):618-628.

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