标签归档：grp

多肽定制GRP (1-16) (porcine) 编码

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名称 GRP (1-16) (porcine)
编码
别名 GRP (1-16) (porcine)
纯度 80%，90%，95%，98%，99%
重量 1mg,5mg,10mg,50mg,100mg,1g
序列（单字母缩写） APVSVGGGTVLAKMYP-OH
序列（三字母缩写） Ala-Pro-Val-Ser-Val-Gly-Gly-Gly-Thr-Val-Leu-Ala-Lys-Met-Tyr-Pro
基本描述
溶解度
分子量 0
化学式
存储条件 Store at -20°C. Keep tightly closed. Store in a cool dry place.
注释
Documents GRP (1-16) (porcine) 编码
Figures GRP (1-16) (porcine) 编码
Reference
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多肽定制GRP (human)|Gastrin Releasing Peptide, human 编码 [93755-85-2]

发表于由

上海金畔生物科技有限公司可以定制不同序列多肽，可以访问官网了解更多产品信息。

名称 GRP (human)|Gastrin Releasing Peptide, human
编码 [93755-85-2]
别名 GRP (human)|Gastrin Releasing Peptide, human
纯度 80%，90%，95%，98%，99%
重量 1mg,5mg,10mg,50mg,100mg,1g
序列（单字母缩写） VPLPAGGGTVLTKMYPRGNHWAVGHLM-NH2
序列（三字母缩写） H-Val-Pro-Leu-Pro-Ala-Gly-Gly-Gly-Thr-Val-Leu-Thr-Lys-Met-Tyr-Pro-Arg-Gly-Asn-His-Trp-Ala-Val-Gly-His-Leu-Met-NH2?(trifluoroacetate salt)
基本描述
溶解度
分子量 2859.4
化学式 C130H204N38O31S2
存储条件 Store at -20°C. Keep tightly closed. Store in a cool dry place.
注释
Documents GRP (human)|Gastrin Releasing Peptide, human 编码 [93755-85-2]
Figures GRP (human)|Gastrin Releasing Peptide, human 编码 [93755-85-2]
Reference E.R. Spindel et al., PNAS, 81, 5699 (1984)
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GRP78-IN-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。

GRP78-IN-2 

GRP78-IN-2 (Compound FL5) 是一种葡萄糖调节蛋白 78 (GRP78) 抑制剂。GRP78-IN-2 优先靶向细胞表面 GRP78 ，在不影响其他正常细胞的情况下表现出强大的抗血管生成和抗癌活性。

GRP78-IN-2

GRP78-IN-2 Chemical Structure

CAS No. : 1882875-63-9

规格 是否有货
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250 mg   询价  
500 mg   询价  

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生物活性

GRP78-IN-2 (Compound FL5) is a GRP78 (Glucose Regulated Protein 78 kDa) inhibitor. GRP78-IN-2 preferentially targeting cell surface GRP78 and shows potent antiangiogenic and anticancer activities without affecting other normal cells[1].

分子量

487.54

Formula

C29H29NO6
CAS 号

1882875-63-9
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]. Qiao Y, et al. Discovery of small molecules targeting GRP78 for antiangiogenic and anticancer therapy. Eur J Med Chem. 2020 May 1;193:112228.

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GRP78-IN-1

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。

GRP78-IN-1 

GRP78-IN-1 与 GRP78 残基具有多种相互作用，结合能为 -8.07 kcal/mol。GRP78-IN-1 在癌细胞中显示出有效的细胞毒性、抗增殖作用。GRP78-IN-1 在乳腺癌细胞中表现出有前景的凋亡和伤口愈合特性。

GRP78-IN-1

GRP78-IN-1 Chemical Structure

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

GRP78-IN-1 exhibits several interactions with GRP78 residues with binding energy of -8.07 kcal/mol. GRP78-IN-1 shows the potent cytotoxic, anti-proliferative in cancer cells. GRP78-IN-1 exhibits promising apoptosis in breast cancer cells and wound healing properties[1].

IC50 & Target

Grp78

 

体外研究
(In Vitro)

GRP78-IN-1 (compound 3i) (0.01, 0.1, 1, 10, 100 µM; 48 h) shows the most potent cytotoxic effect (IC50s of 2.06, 12.57, 9, 18, 4.9, 2.19, 62.48 µM in MCF-1, PANC-1, HCT-116, PC-3, A549, MDA-MB-231 and FR-2 cells, respectively)[1].
GRP78-IN-1 (1, 2, 4, 6 µM) shows a steady increase in the expression of pro-apoptotic proteins viz. Par-4, apoptotic cascade in BAX and cleaved caspase 9 cells[1].
GRP78-IN-1 (1, 2, 4, 6 µM; 48 h) inhibits the motility of MCF-7 and A549 cells in a dose-dependent manner[1].

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

Cell Cytotoxicity Assay[1]

Cell Line: MCF-1, MDA-MB-231, PANC-1, HCT-116, PC-3, A549, FR-2cells
Concentration: 0.01, 0.1, 1, 10, 100 µM
Incubation Time: 48 h
Result: Showed the most promising cytotoxic effect (IC50s is 2.06, 12.57, 9, 18, 4.9, 2.19, 62.48 µM in MCF-1, PANC-1, HCT-116, PC-3, A549, MDA-MB-231 and FR-2 cells, respectively).

Western Blot Analysis[1]

Cell Line: BCL-2, BAX, cleaved caspase 9, MCF-7, A549 cells
Concentration: 1, 2, 4, 6 µM
Incubation Time:
Result: Showed a steady increase in the expression of pro-apoptotic proteins viz. Par-4, apoptotic cascade in BAX and cleaved caspase 9 cells.

分子量

342.40

Formula

C21H23FO3
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]. Rasool JU, et al. Palladium catalyzed migratory heck coupling of arteannuin B and boronic acids: An approach towards the synthesis of antiproliferative agents in breast and lung cancer cells. Bioorg Chem. 2022, 122:105694.

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

GRP78-IN-1

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。

GRP78-IN-1 

GRP78-IN-1 与 GRP78 残基具有多种相互作用，结合能为 -8.07 kcal/mol。GRP78-IN-1 在癌细胞中显示出有效的细胞毒性、抗增殖作用。GRP78-IN-1 在乳腺癌细胞中表现出有前景的凋亡和伤口愈合特性。

GRP78-IN-1

GRP78-IN-1 Chemical Structure

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

GRP78-IN-1 exhibits several interactions with GRP78 residues with binding energy of -8.07 kcal/mol. GRP78-IN-1 shows the potent cytotoxic, anti-proliferative in cancer cells. GRP78-IN-1 exhibits promising apoptosis in breast cancer cells and wound healing properties[1].

IC50 & Target

Grp78

 

体外研究
(In Vitro)

GRP78-IN-1 (compound 3i) (0.01, 0.1, 1, 10, 100 µM; 48 h) shows the most potent cytotoxic effect (IC50s of 2.06, 12.57, 9, 18, 4.9, 2.19, 62.48 µM in MCF-1, PANC-1, HCT-116, PC-3, A549, MDA-MB-231 and FR-2 cells, respectively)[1].
GRP78-IN-1 (1, 2, 4, 6 µM) shows a steady increase in the expression of pro-apoptotic proteins viz. Par-4, apoptotic cascade in BAX and cleaved caspase 9 cells[1].
GRP78-IN-1 (1, 2, 4, 6 µM; 48 h) inhibits the motility of MCF-7 and A549 cells in a dose-dependent manner[1].

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

Cell Cytotoxicity Assay[1]

Cell Line: MCF-1, MDA-MB-231, PANC-1, HCT-116, PC-3, A549, FR-2cells
Concentration: 0.01, 0.1, 1, 10, 100 µM
Incubation Time: 48 h
Result: Showed the most promising cytotoxic effect (IC50s is 2.06, 12.57, 9, 18, 4.9, 2.19, 62.48 µM in MCF-1, PANC-1, HCT-116, PC-3, A549, MDA-MB-231 and FR-2 cells, respectively).

Western Blot Analysis[1]

Cell Line: BCL-2, BAX, cleaved caspase 9, MCF-7, A549 cells
Concentration: 1, 2, 4, 6 µM
Incubation Time:
Result: Showed a steady increase in the expression of pro-apoptotic proteins viz. Par-4, apoptotic cascade in BAX and cleaved caspase 9 cells.

分子量

342.40

Formula

C21H23FO3
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]. Rasool JU, et al. Palladium catalyzed migratory heck coupling of arteannuin B and boronic acids: An approach towards the synthesis of antiproliferative agents in breast and lung cancer cells. Bioorg Chem. 2022, 122:105694.

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

GRP78-IN-1

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。

GRP78-IN-1 

GRP78-IN-1 与 GRP78 残基具有多种相互作用，结合能为 -8.07 kcal/mol。GRP78-IN-1 在癌细胞中显示出有效的细胞毒性、抗增殖作用。GRP78-IN-1 在乳腺癌细胞中表现出有前景的凋亡和伤口愈合特性。

GRP78-IN-1

GRP78-IN-1 Chemical Structure

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

GRP78-IN-1 exhibits several interactions with GRP78 residues with binding energy of -8.07 kcal/mol. GRP78-IN-1 shows the potent cytotoxic, anti-proliferative in cancer cells. GRP78-IN-1 exhibits promising apoptosis in breast cancer cells and wound healing properties[1].

IC50 & Target

Grp78

 

体外研究
(In Vitro)

GRP78-IN-1 (compound 3i) (0.01, 0.1, 1, 10, 100 µM; 48 h) shows the most potent cytotoxic effect (IC50s of 2.06, 12.57, 9, 18, 4.9, 2.19, 62.48 µM in MCF-1, PANC-1, HCT-116, PC-3, A549, MDA-MB-231 and FR-2 cells, respectively)[1].
GRP78-IN-1 (1, 2, 4, 6 µM) shows a steady increase in the expression of pro-apoptotic proteins viz. Par-4, apoptotic cascade in BAX and cleaved caspase 9 cells[1].
GRP78-IN-1 (1, 2, 4, 6 µM; 48 h) inhibits the motility of MCF-7 and A549 cells in a dose-dependent manner[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.

Cell Cytotoxicity Assay[1]

Cell Line: MCF-1, MDA-MB-231, PANC-1, HCT-116, PC-3, A549, FR-2cells
Concentration: 0.01, 0.1, 1, 10, 100 µM
Incubation Time: 48 h
Result: Showed the most promising cytotoxic effect (IC50s is 2.06, 12.57, 9, 18, 4.9, 2.19, 62.48 µM in MCF-1, PANC-1, HCT-116, PC-3, A549, MDA-MB-231 and FR-2 cells, respectively).

Western Blot Analysis[1]

Cell Line: BCL-2, BAX, cleaved caspase 9, MCF-7, A549 cells
Concentration: 1, 2, 4, 6 µM
Incubation Time:
Result: Showed a steady increase in the expression of pro-apoptotic proteins viz. Par-4, apoptotic cascade in BAX and cleaved caspase 9 cells.

分子量

342.40

Formula

C21H23FO3
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]. Rasool JU, et al. Palladium catalyzed migratory heck coupling of arteannuin B and boronic acids: An approach towards the synthesis of antiproliferative agents in breast and lung cancer cells. Bioorg Chem. 2022, 122:105694.

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

多肽定制Acetyl-GRP (20-26) (human, porcine, canine) 编码 [121432-21-1]

发表于由

上海金畔生物科技有限公司可以定制不同序列多肽，可以访问官网了解更多产品信息。

名称 Acetyl-GRP (20-26) (human, porcine, canine)
编码 [121432-21-1]
别名 Acetyl-GRP (20-26) (human, porcine, canine)
纯度 80%，90%，95%，98%，99%
重量 1mg,5mg,10mg,50mg,100mg,1g
序列（单字母缩写） Ac-HWAVGHL-NH2
序列（三字母缩写） Ac-His-Trp-Ala-Val-Gly-His-Leu-NH2
基本描述
溶解度
分子量 859.99
化学式 C410H57N13O8
存储条件 Store at -20°C. Keep tightly closed. Store in a cool dry place.
注释
Documents Acetyl-GRP (20-26) (human, porcine, canine) 编码 [121432-21-1]
Figures Acetyl-GRP (20-26) (human, porcine, canine) 编码 [121432-21-1]
Reference
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多肽定制Acetyl-GRP (20-27) (human, porcine, canine) 编码 [77714-20-6]

发表于由

上海金畔生物科技有限公司可以定制不同序列多肽，可以访问官网了解更多产品信息。

名称 Acetyl-GRP (20-27) (human, porcine, canine)
编码 [77714-20-6]
别名 Acetyl-GRP (20-27) (human, porcine, canine)
纯度 80%，90%，95%，98%，99%
重量 1mg,5mg,10mg,50mg,100mg,1g
序列（单字母缩写） Ac-HWAVGHLM-NH2
序列（三字母缩写） Ac-His-Trp-Ala-Val-Gly-His-Leu-Met-NH2
基本描述
溶解度
分子量 0
化学式
存储条件 Store at -20°C. Keep tightly closed. Store in a cool dry place.
注释
Documents Acetyl-GRP (20-27) (human, porcine, canine) 编码 [77714-20-6]
Figures Acetyl-GRP (20-27) (human, porcine, canine) 编码 [77714-20-6]
Reference
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Grp94 Inhibitor-1

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。

Grp94 Inhibitor-1  纯度: 98.63%

Grp94 Inhibitor-1 是一种有效的、选择性的 Grp94 抑制剂，IC50 值为 2 nM，对 Grp94 的抑制作用是 Hsp90α 的 1000 倍。

Grp94 Inhibitor-1

Grp94 Inhibitor-1 Chemical Structure

CAS No. : 2234897-35-7

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 ￥550 In-stock
5 mg ￥500 In-stock
10 mg ￥800 In-stock
50 mg ￥2400 In-stock
100 mg ￥4100 In-stock
200 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

Grp94 Inhibitor-1 相关产品

•相关化合物库:

  • Bioactive Compound Library Plus
  • Cell Cycle/DNA Damage Compound Library
  • Immunology/Inflammation Compound Library
  • Metabolism/Protease Compound Library
  • Anti-Cancer Compound Library
  • Anti-Aging Compound Library
  • Endoplasmic Reticulum Stress Compound Library
  • Pyroptosis Compound Library
  • Cytoskeleton Compound Library

生物活性

Grp94 Inhibitor-1 is a potent, selective Grp94 inhibitor with an IC50 value of 2 nM, and over 1000-fold selectivity to Grp94 against Hsp90α[1].

IC50 & Target[1]

GRP94

2 nM (IC50)

体外研究
(In Vitro)

Grp94-specific clients include a subset of integrin subunits such as integrin α2 and integrin αL. Their maturation and trafficking to the cell surface are dependent on the Grp94 chaperone function but have no association with cytoplasmic Hsp90α.
Grp94 Inhibitor-1 (1-5 μM; 36 hours) significantly downregulated the cell surface expression levels of integrin α2 and integrin αL in a dose-dependent manner in panc1 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.

Western Blot Analysis[1]

Cell Line: Panc1 cells
Concentration: 1 μM; 2.5 μM; 5 μM
Incubation Time: 36 hours
Result: Decreased integrin α2 and integrin αL protein expression.

体内研究
(In Vivo)

Grp94 Inhibitor-1 (intraperitoneal injection,qid.; coadminbistration 10 mg/kg or 30 mg/kg; 8 days) does not attenuate the colon shortening, but decreases disease activity index (DAI) scores. It also TNFα and IL-6 levels in the serum and colonic tissues and significantly reduces the p65 expression in colonic tissues, especially those in the 30 mg/kg dose group[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.

Animal Model: C57BL/6 mice (male, 20-22 g)[1]
Dosage: 10 mg/kg or 30 mg/kg
Administration: Intraperitoneal injection,qid.; coadminbistration 10 mg/kg or 30 mg/kg
Result: Decreased disease activity index (DAI) scores in UC mices.

分子量

352.47

Formula

C22H28N2O2
CAS 号

2234897-35-7
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 : 250 mg/mL (709.28 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.8371 mL 14.1856 mL 28.3712 mL
5 mM 0.5674 mL 2.8371 mL 5.6742 mL
10 mM 0.2837 mL 1.4186 mL 2.8371 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    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.08 mg/mL (5.90 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (5.90 mM，饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液

  • 2.

    请依序添加每种溶剂： 10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.08 mg/mL (5.90 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (5.90 mM，饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。

    将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
  • 3.

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

    Solubility: ≥ 2.08 mg/mL (5.90 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (5.90 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 20.8 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]. Jiang F, et al. Discovery of a Potent Grp94 Selective Inhibitor with Anti-Inflammatory Efficacy in a Mouse Model of Ulcerative Colitis. J Med Chem. 2018 Nov 8;61(21):9513-9533.

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