标签归档：ri

TGFβRI-IN-1

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TGFβRI-IN-1 

TGFβRI-IN-1 是一种口服有效的、TGFβ 受体I 型激酶 (TGFβRI)的选择性抑制剂，其对TGFβRI 和TGFβRII 的 IC50 值分别为2 nM 和7.6 μM。

TGFβRI-IN-1

TGFβRI-IN-1 Chemical Structure

CAS No. : 1950628-94-0

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生物活性

TGFβRI-IN-1 is an oral active and selective TGFβ receptor type I (TGFβRI) kinase inhibitor, with IC50 values of 2 nM and 7.6 μM for TGFβRI and TGFβRII, respectively[1] .

IC50 & Target

IC50: 2 nM (TGFβRI)[1].
分子量

362.40

Formula

C20H14D3N5O2
CAS 号

1950628-94-0
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.
参考文献

  • [1]. Yong Zhang, et al. Discovery of 4-Azaindole Inhibitors of TGFβRI as Immuno-oncology Agents. ACS Med. Chem. Lett.20189111117-1122.

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RI(dl)-2 TFA

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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。

RI(dl)-2 TFA  纯度: ≥98.0%

RI(dl)-2 TFA 是一种有效的选择性 RAD51 介导的 D 环形成 (RAD51-mediated D-loop formation) 抑制剂，IC50 为 11.1 μM。RI(dl)-2 TFA 不会影响 RAD51 与 ssDNA 的结合，并会抑制人细胞中的同源重组 (HR) 活性 (IC50 为 3.0 μM)。

RI(dl)-2 TFA

RI(dl)-2 TFA Chemical Structure

规格 价格 是否有货 数量
5 mg ￥5500 In-stock
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生物活性

RI(dl)-2 TFA is a potent and selective RAD51-mediated D-loop formation inhibitor with an IC50 of 11.1 μM. RI(dl)-2 TFA does not influence RAD51 binding to ssDNA and inhibits homologous recombination (HR) activity in human cells (IC50 of 3.0 μM)[1].

IC50 & Target

IC50: 11.1 μM (RAD51-mediated D-loop formation)[1]
体外研究
(In Vitro)

RI(dl)-2 stabilizes nucleoprotein filaments in a nonfunctional state, which are incapable of D-loop activity and simultaneously shielded from related (e.g., RAD52-mediated) pathways that promote single-strand annealing (SSA)[1].
RI(dl)-2 does not modulate the affinity of RAD51 to ssDNA or the stability of preformed RAD51-ssDNA complexes when challenged with high concentrations of salt[1].

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

435.59

Formula

C21H18F3N3O2
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

4°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]. Wei Lv, et al. Development of Small Molecules that Specifically Inhibit the D-loop Activity of RAD51. J Med Chem. 2016 May 26;59(10):4511-25.

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RI-1

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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。

RI-1  纯度: 99.83%

RI-1 是一种选择性 RAD51 的抑制剂，IC50 值为 5-30 μM。RI-1 在半胱氨酸 319 处与 RAD51 蛋白表面共价结合。RI-1 通过直接结合到 RAD51 细丝中蛋白质亚基之间的界面的蛋白质表面来灭活 RAD51。RI-1 可以破坏人类细胞中的同源重组。

RI-1

RI-1 Chemical Structure

CAS No. : 415713-60-9

规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ￥825 In-stock
5 mg ￥750 In-stock
10 mg ￥1300 In-stock
50 mg ￥4500 In-stock
100 mg ￥7650 In-stock
200 mg   询价  
500 mg   询价  

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RI-1 相关产品

•相关化合物库:

  • Bioactive Compound Library Plus
  • Cell Cycle/DNA Damage Compound Library
  • Anti-Cancer Compound Library
  • Anti-Aging Compound Library
  • Anti-Breast Cancer Compound Library

生物活性

RI-1 is a RAD51 inhibitor, with IC50s ranging from 5 to 30 μM. RI-1 binds covalently to the surface of RAD51 protein at cysteine 319. RI-1 inactivates RAD51 by directly binding to a protein surface that serves as an interface between protein subunits in RAD51 filaments. RI-1 can disrupt homologous recombination in human cells[1].

IC50 & Target

IC50: 5-30 μM (RAD51)[1]
体外研究
(In Vitro)

RI-1 (1-50 µM; 24 h) specifically inhibits homologous recombination (HR) in U2OS cells and stimulates single-strand annealing (SSA) in HEK293 cells[1].
RI-1 (5-20 µM; 30 min) inhibits HsRAD51 in a concentration-dependent manner[1].
RI-1 (20 µM; 8 h) disrupts the formation of RAD51 foci after DNA damage in immortalized human fibroblasts[1].
RI-1 (15-25 µM; 24 h) sensitizes human cancer cells (HeLa, MCF-7 and U2OS) to cross-linking chemotherapy[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究
(In Vivo)

RI-1 (50 mg/kg; i.p. every 3 d for 30 d) significantly reduces triple negative breast cancer (TNBC) tumor growth in mice[2].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Female BALB/c nude mice (6 weeks) bearing TNBC tumor[2]
Dosage: 50 mg/kg
Administration: I.p. every 3 days for 30 days
Result: Resulted in significant inhibition of tumor growth.
Did not cause body weight loss significantly.

分子量

361.61

Formula

C14H11Cl3N2O3
CAS 号

415713-60-9
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 : 33.33 mg/mL (92.17 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.7654 mL 13.8271 mL 27.6541 mL
5 mM 0.5531 mL 2.7654 mL 5.5308 mL
10 mM 0.2765 mL 1.3827 mL 2.7654 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 (6.91 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (6.91 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 上海金畔生物科技有限公司 网站选购。
参考文献

  • [1]. Budke B, et, al. RI-1: a chemical inhibitor of RAD51 that disrupts homologous recombination in human cells. Nucleic Acids Res. 2012 Aug;40(15):7347-57.

    [2]. Shi Y, et, al. DAXX, as a Tumor Suppressor, Impacts DNA Damage Repair and Sensitizes BRCA-Proficient TNBC Cells to PARP Inhibitors. Neoplasia. 2019 Jun;21(6):533-544.

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RI-2

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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。

RI-2  纯度: 99.64%

RI-2 是一种可逆的 RAD51 抑制剂，IC50 值为 44.17 μM，能够特异性地抑制人体细胞中的同源重组修复。

RI-2

RI-2 Chemical Structure

CAS No. : 1417162-36-7

规格 价格 是否有货 数量
Free Sample (0.1-0.5 mg)   Apply now  
10 mM * 1 mL in DMSO ￥2585 In-stock
5 mg ￥2350 In-stock
10 mg ￥4000 In-stock
50 mg ￥12000 In-stock
100 mg 询价

* Please select Quantity before adding items.

RI-2 相关产品

•相关化合物库:

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

生物活性

RI-2 is a reversible RAD51 inhibitor, with an IC50 of 44.17 μM, and specifically inhibits homologous recombination repair in human cells.

IC50 & Target

IC50: 44.17 μM (RAD51)[1]
体外研究
(In Vitro)

RI-2 (7a) is a reversible RAD51 inhibitor, with an IC50 of 44.17 μM. RI-2 specifically inhibits homologous recombination repair in human cells. RI-2 (150 μM) induces a significant sensitization of cells[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
分子量

433.28

Formula

C21H18Cl2N2O4
CAS 号

1417162-36-7
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 : 130 mg/mL (300.04 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.3080 mL 11.5399 mL 23.0798 mL
5 mM 0.4616 mL 2.3080 mL 4.6160 mL
10 mM 0.2308 mL 1.1540 mL 2.3080 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。
参考文献

  • [1]. Budke B, et al. An optimized RAD51 inhibitor that disrupts homologous recombination without requiring Michael acceptor reactivity. J Med Chem. 2013 Jan 10;56(1):254-63.
Cell Assay
[1]

HEK293 cells are plated into 96-well tissue culture plates at a density of 300 cells per well in the presence or absence of 50 nM mitomycin C (MMC) for 24 hours at 37°C, 5% CO2. Media is subsequently replaced with fresh media containing 0.5% DMSO plus RI-2 for an additional 24 hours. RI-2 is then removed, and cultures are allowed to grow to a 50-70% confluence. Average survival from at least three replicates is measured using CellGlo reagentor. RI-2 is deemed successful in sensitizing cells to MMC if they generate significantly greater toxicity in the presence of MMC relative to the absence of MMC. Specifically, sensitization is scored as a “+” when non-overlapping standard errors are observed for at least two pairs of compound doses[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
参考文献

  • [1]. Budke B, et al. An optimized RAD51 inhibitor that disrupts homologous recombination without requiring Michael acceptor reactivity. J Med Chem. 2013 Jan 10;56(1):254-63.

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

5′-O-DMT-2′-O-TBDMS-rI

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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。

5′-O-DMT-2′-O-TBDMS-rI 

5′-O-DMT-2′-O-TBDMS-rI 是一种修饰的核苷酸，可用于脱氧核糖核酸或者核糖核酸的合成。

5

5′-O-DMT-2′-O-TBDMS-rI Chemical Structure

CAS No. : 127212-34-4

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

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生物活性

5′-O-DMT-2′-O-TBDMS-rI is a modified nucleoside. 5′-O-DMT-2′-O-TBDMS-rI can be used in the synthesis of deoxyribonucleic acid or nucleic acid.

分子量

684.85

Formula

C37H44N4O7Si
CAS 号

127212-34-4
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.

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

5′-O-DMT-2′-O-TBDMS-rI

发表于由

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。

5′-O-DMT-2′-O-TBDMS-rI 

5′-O-DMT-2′-O-TBDMS-rI 是一种修饰的核苷酸，可用于脱氧核糖核酸或者核糖核酸的合成。

5

5′-O-DMT-2′-O-TBDMS-rI Chemical Structure

CAS No. : 127212-34-4

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

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生物活性

5′-O-DMT-2′-O-TBDMS-rI is a modified nucleoside. 5′-O-DMT-2′-O-TBDMS-rI can be used in the synthesis of deoxyribonucleic acid or nucleic acid.

分子量

684.85

Formula

C37H44N4O7Si
CAS 号

127212-34-4
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.

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

5′-O-DMT-2′-O-TBDMS-rI

发表于由

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。

5′-O-DMT-2′-O-TBDMS-rI 

5′-O-DMT-2′-O-TBDMS-rI 是一种修饰的核苷酸，可用于脱氧核糖核酸或者核糖核酸的合成。

5

5′-O-DMT-2′-O-TBDMS-rI Chemical Structure

CAS No. : 127212-34-4

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

* Please select Quantity before adding items.

生物活性

5′-O-DMT-2′-O-TBDMS-rI is a modified nucleoside. 5′-O-DMT-2′-O-TBDMS-rI can be used in the synthesis of deoxyribonucleic acid or nucleic acid.

分子量

684.85

Formula

C37H44N4O7Si
CAS 号

127212-34-4
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.

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