PLK4-IN-3

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。

PLK4-IN-3 

PLK4-IN-3 是PLK4-IN-1 的绝对构型。PLK4-IN-1 (Example A6) 是PLK4 的抑制剂,其IC50 值为 ≤0.1 μM。

PLK4-IN-3

PLK4-IN-3 Chemical Structure

CAS No. : 1247001-86-0

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

PLK4-IN-3 is a less active absolute stereochemistry of PLK4-IN-1. PLK4-IN-1 is a PLK4 inhibitor, with an IC50 of 0.65 μM[1].

IC50 & Target[1]

PLK4

≤ 0.1 μM (IC50)

分子量

431.23

Formula

C18H14IN3O2

CAS 号

1247001-86-0

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]. Peter Brent Sampson, et al. KINASE INHIBITORS AND METHOD OF TREATING CANCER WITH SAME. Patent. WO2011123946A1.

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

PLK4-IN-1

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。

PLK4-IN-1 

PLK4-IN-1 (Example A6) 是 PLK4 的抑制剂,其 IC50 值为 ≤ 0.1 μM。

PLK4-IN-1

PLK4-IN-1 Chemical Structure

CAS No. : 1247001-12-2

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

PLK4-IN-1 (Example A6) is a PLK4 inhibitor, with an IC50 of ≤ 0.1 μM[1].

IC50 & Target

IC50: ≤ 0.1 μM (PLK4)[1].

分子量

431.23

Formula

C18H14IN3O2

CAS 号

1247001-12-2

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]. Peter Brent Sampson, et al. KINASE INHIBITORS AND METHOD OF TREATING CANCER WITH SAME. Patent. WO2011123946A1.

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

PLK4-IN-3

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。

PLK4-IN-3 

PLK4-IN-3 是PLK4-IN-1 的绝对构型。PLK4-IN-1 (Example A6) 是PLK4 的抑制剂,其IC50 值为 ≤0.1 μM。

PLK4-IN-3

PLK4-IN-3 Chemical Structure

CAS No. : 1247001-86-0

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

PLK4-IN-3 is a less active absolute stereochemistry of PLK4-IN-1. PLK4-IN-1 is a PLK4 inhibitor, with an IC50 of 0.65 μM[1].

IC50 & Target[1]

PLK4

≤ 0.1 μM (IC50)

分子量

431.23

Formula

C18H14IN3O2

CAS 号

1247001-86-0

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]. Peter Brent Sampson, et al. KINASE INHIBITORS AND METHOD OF TREATING CANCER WITH SAME. Patent. WO2011123946A1.

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

PLK4-IN-1

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。

PLK4-IN-1 

PLK4-IN-1 (Example A6) 是 PLK4 的抑制剂,其 IC50 值为 ≤ 0.1 μM。

PLK4-IN-1

PLK4-IN-1 Chemical Structure

CAS No. : 1247001-12-2

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

PLK4-IN-1 (Example A6) is a PLK4 inhibitor, with an IC50 of ≤ 0.1 μM[1].

IC50 & Target

IC50: ≤ 0.1 μM (PLK4)[1].

分子量

431.23

Formula

C18H14IN3O2

CAS 号

1247001-12-2

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]. Peter Brent Sampson, et al. KINASE INHIBITORS AND METHOD OF TREATING CANCER WITH SAME. Patent. WO2011123946A1.

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

PLK4-IN-3

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。

PLK4-IN-3 

PLK4-IN-3 是PLK4-IN-1 的绝对构型。PLK4-IN-1 (Example A6) 是PLK4 的抑制剂,其IC50 值为 ≤0.1 μM。

PLK4-IN-3

PLK4-IN-3 Chemical Structure

CAS No. : 1247001-86-0

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

PLK4-IN-3 is a less active absolute stereochemistry of PLK4-IN-1. PLK4-IN-1 is a PLK4 inhibitor, with an IC50 of 0.65 μM[1].

IC50 & Target[1]

PLK4

≤ 0.1 μM (IC50)

分子量

431.23

Formula

C18H14IN3O2

CAS 号

1247001-86-0

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]. Peter Brent Sampson, et al. KINASE INHIBITORS AND METHOD OF TREATING CANCER WITH SAME. Patent. WO2011123946A1.

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

PLK4-IN-1

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。

PLK4-IN-1 

PLK4-IN-1 (Example A6) 是 PLK4 的抑制剂,其 IC50 值为 ≤ 0.1 μM。

PLK4-IN-1

PLK4-IN-1 Chemical Structure

CAS No. : 1247001-12-2

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

PLK4-IN-1 (Example A6) is a PLK4 inhibitor, with an IC50 of ≤ 0.1 μM[1].

IC50 & Target

IC50: ≤ 0.1 μM (PLK4)[1].

分子量

431.23

Formula

C18H14IN3O2

CAS 号

1247001-12-2

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]. Peter Brent Sampson, et al. KINASE INHIBITORS AND METHOD OF TREATING CANCER WITH SAME. Patent. WO2011123946A1.

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

AZD4625

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。

AZD4625 

AZD4625 (Compound 21) 是一种高度有效的、选择性的、共价和变构的突变 GTPase KRASG12C 抑制剂。AZD4625 具有高口服生物利用度。

AZD4625

AZD4625 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

AZD4625 (Compound 21) is a highly potent, selective, covalent and allosteric inhibitor of the mutant GTPase KRASG12C. AZD4625 has high oral bioavailability[1].

IC50 & Target

KRAS(G12C)

 

分子量

486.90

Formula

C24H21ClF2N4O3

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]. Kettle JG, et al. Discovery of AZD4625, a Covalent Allosteric Inhibitor of the Mutant GTPase KRASG12C. J Med Chem. 2022 May 12;65(9):6940-6952.

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

(Z)-Semaxanib(Synonyms: (Z)-SU5416)

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。

(Z)-Semaxanib (Synonyms: (Z)-SU5416)

Z)-Semaxanib (compound (z)-1) 是一种有效的酪氨酸激酶抑制剂。(Z)-Semaxanib 对 TAMH 和 HepG2 细胞具有细胞毒性,IC50s 分别为 6.28 µM 和 8.17 µM。

(Z)-Semaxanib(Synonyms: (Z)-SU5416)

(Z)-Semaxanib Chemical Structure

CAS No. : 194413-58-6

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

(Z)-Semaxanib (compound (z)-1) is a potent tyrosine kinase inhibitor. (Z)-Semaxanib shows cytotoxicity for TAMH and HepG2 cells with IC50s of 6.28 µM and 8.17 µM, respectively[1].

分子量

238.28

Formula

C15H14N2O

CAS 号

194413-58-6

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]. Ngai MH, So CL, Sullivan MB, Ho HK, Chai CL. Photoinduced Isomerization and Hepatoxicities of Semaxanib, Sunitinib and Related 3-Substituted Indolin-2-ones. ChemMedChem. 2016 Jan 5;11(1):72-80.

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

BOLD-100

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。

BOLD-100 

BOLD-100 是一种基于钌元素的抗癌剂。BOLD-10 也是应激诱导的 GRP78 上调的抑制剂,从而破坏内质网 (ER) 稳态并诱导 ER 应激和未折叠蛋白反应 (UPR)。BOLD-100 干扰了内质网应激反应、溶酶体动力和细胞自噬 (autophagy) 之间复杂的相互作用。

BOLD-100

BOLD-100 Chemical Structure

CAS No. : 783324-98-1

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

BOLD-100 is a ruthenium-based anticancer agent. BOLD-100 also is an inhibitor of stress-induced GRP78 upregulation, disrupting endoplasmic reticulum (ER) homeostasis and inducing ER stress and unfolded protein response (UPR). BOLD-100 interferes with the complex interplay between ER-stress response, lysosome dynamics, and autophagy execution[1].

IC50 & Target

GRP78, Autophagy[1]

分子量

479.15

Formula

C14H12Cl4N4Ru

CAS 号

783324-98-1

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]. Baier D, et al. The Anticancer Ruthenium Compound BOLD-100 Targets Glycolysis and Generates a Metabolic Vulnerability towards Glucose Deprivation. Pharmaceutics. 2022;14(2):238. Published 2022 Jan 20.

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

4′-Demethyldehydropodophyllotoxin

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。

4′-Demethyldehydropodophyllotoxin 

4′-Demethyldehydropodophyllotoxin 是一种芳基四氢萘类木质素,可以从 Podophyllum hexandrum 的叶片中分子得到。4′-Demethyldehydropodophyllotoxin 具有细胞毒性和抗肿瘤活性。

4

4′-Demethyldehydropodophyllotoxin Chemical Structure

CAS No. : 117669-31-5

规格 是否有货
5 mg 询价
10 mg 询价
25 mg 询价

* Please select Quantity before adding items.

生物活性

4′-Demethyldehydropodophyllotoxin is an aryltetralin lignan that can be isolated from leaves of Podophyllum hexandrum. 4′-Demethyldehydropodophyllotoxin exhibits some cytotoxic and antitumour activity[1].

分子量

396.35

Formula

C21H16O8

CAS 号

117669-31-5

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]. Atta-ur-Rahman, et al. Antifungal aryltetralin lignans from leaves of Podophyllum hexandrum. Phytochemistry (1995), 40(2), 427-31.

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

Indophagolin

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。

Indophagolin  纯度: 98.05%

Indophagolin 是一种有效的含 indoline 的自噬 (autophagy) 抑制剂 (IC50=140 nM)。Indophagolin 拮抗嘌呤能受体P2X4、P2X1 和 P2X3,IC50 分别为 2.71、2.40 和 3.49 μM。Indophagolin 还拮抗 Gq 蛋白偶联的 P2Y4、P2Y6 和 P2Y11 受体(IC50s =3.4~15.4 μM)。Indophagolin 五羟色胺受体5-HT6 有较强的拮抗作用 (IC50=1.0 μM),对 5-HT1B、5-HT2B、5-HT4e 和 5-HT7 有中度拮抗作用。

Indophagolin

Indophagolin Chemical Structure

CAS No. : 1207660-00-1

规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ¥2881 In-stock
5 mg ¥2500 In-stock
10 mg ¥3750 In-stock
25 mg ¥7500 In-stock
50 mg ¥12000 In-stock
100 mg 询价

* Please select Quantity before adding items.

Indophagolin 相关产品

相关化合物库:

  • Bioactive Compound Library Plus
  • GPCR/G Protein Compound Library
  • Membrane Transporter/Ion Channel Compound Library
  • Neuronal Signaling Compound Library
  • Anti-Cancer Compound Library
  • Autophagy Compound Library
  • Neurotransmitter Receptor Compound Library
  • Anti-Alzheimer’s Disease Compound Library
  • Anti-Parkinson’s Disease Compound Library
  • Neurodegenerative Disease-related Compound Library

生物活性

Indophagolin is a potent, indoline-containing autophagy inhibitor (IC50=140 nM). Indophagolin antagonizes the purinergic receptor P2X4 as well as P2X1 and P2X3 with IC50s of 2.71, 2.40 and 3.49 μM, respectively. Indophagolin also antagonizes the Gq-protein-coupled P2Y4, P2Y6, and P2Y11 receptors (IC50s =3.4~15.4 μM). Indophagolin has a strong antagonistic effect on serotonin receptor 5-HT6 (IC50=1.0 μM) and a moderate effect on receptors 5-HT1B, 5-HT2B, 5-HT4e, and 5-HT7[1].

IC50 & Target[1]

P2X1

2.4 μM (IC50)

P2X4

2.71 μM (IC50)

P2Y11

3.4 μM (IC50)

P2X3

3.49 μM (IC50)

P2Y4

4.89 μM (IC50)

P2Y6

15.4 μM (IC50)

Autophagy

140 nM (IC50)

5-HT6 Receptor

1.0 μM (IC50)

体外研究
(In Vitro)

Indophagolin (10 μM) inhibits autophagosome formation in MCF7 cells[1].

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

分子量

523.75

Formula

C19H15BrClF3N2O3S

CAS 号

1207660-00-1

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

溶解性数据
In Vitro: 

DMSO : 250 mg/mL (477.33 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 1.9093 mL 9.5465 mL 19.0931 mL
5 mM 0.3819 mL 1.9093 mL 3.8186 mL
10 mM 0.1909 mL 0.9547 mL 1.9093 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 (protect from light)。-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 (3.97 mM); Suspended solution; Need ultrasonic

    此方案可获得 2.08 mg/mL (3.97 mM) 的均匀悬浊液,悬浊液可用于口服和腹腔注射。

    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% corn oil

    Solubility: ≥ 2.08 mg/mL (3.97 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (3.97 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 Shanghai Jinpan Biotech Co Ltd 网站选购。
参考文献
  • [1]. Carnero Corrales MA, et al. Thermal proteome profiling identifies the membrane-bound purinergic receptor P2X4 as a target of the autophagy inhibitor indophagolin [published online ahead of print, 2021 Mar 9]. Cell Chem Biol. 2021;S2451-9456(21)00102-1.

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

4′-Demethyldehydropodophyllotoxin

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。

4′-Demethyldehydropodophyllotoxin 

4′-Demethyldehydropodophyllotoxin 是一种芳基四氢萘类木质素,可以从 Podophyllum hexandrum 的叶片中分子得到。4′-Demethyldehydropodophyllotoxin 具有细胞毒性和抗肿瘤活性。

4

4′-Demethyldehydropodophyllotoxin Chemical Structure

CAS No. : 117669-31-5

规格 是否有货
5 mg 询价
10 mg 询价
25 mg 询价

* Please select Quantity before adding items.

生物活性

4′-Demethyldehydropodophyllotoxin is an aryltetralin lignan that can be isolated from leaves of Podophyllum hexandrum. 4′-Demethyldehydropodophyllotoxin exhibits some cytotoxic and antitumour activity[1].

分子量

396.35

Formula

C21H16O8

CAS 号

117669-31-5

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]. Atta-ur-Rahman, et al. Antifungal aryltetralin lignans from leaves of Podophyllum hexandrum. Phytochemistry (1995), 40(2), 427-31.

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

4′-Demethyldehydropodophyllotoxin

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。

4′-Demethyldehydropodophyllotoxin 

4′-Demethyldehydropodophyllotoxin 是一种芳基四氢萘类木质素,可以从 Podophyllum hexandrum 的叶片中分子得到。4′-Demethyldehydropodophyllotoxin 具有细胞毒性和抗肿瘤活性。

4

4′-Demethyldehydropodophyllotoxin Chemical Structure

CAS No. : 117669-31-5

规格 是否有货
5 mg 询价
10 mg 询价
25 mg 询价

* Please select Quantity before adding items.

生物活性

4′-Demethyldehydropodophyllotoxin is an aryltetralin lignan that can be isolated from leaves of Podophyllum hexandrum. 4′-Demethyldehydropodophyllotoxin exhibits some cytotoxic and antitumour activity[1].

分子量

396.35

Formula

C21H16O8

CAS 号

117669-31-5

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]. Atta-ur-Rahman, et al. Antifungal aryltetralin lignans from leaves of Podophyllum hexandrum. Phytochemistry (1995), 40(2), 427-31.

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

Indophagolin

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。

Indophagolin  纯度: 98.05%

Indophagolin 是一种有效的含 indoline 的自噬 (autophagy) 抑制剂 (IC50=140 nM)。Indophagolin 拮抗嘌呤能受体P2X4、P2X1 和 P2X3,IC50 分别为 2.71、2.40 和 3.49 μM。Indophagolin 还拮抗 Gq 蛋白偶联的 P2Y4、P2Y6 和 P2Y11 受体(IC50s =3.4~15.4 μM)。Indophagolin 五羟色胺受体5-HT6 有较强的拮抗作用 (IC50=1.0 μM),对 5-HT1B、5-HT2B、5-HT4e 和 5-HT7 有中度拮抗作用。

Indophagolin

Indophagolin Chemical Structure

CAS No. : 1207660-00-1

规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ¥2881 In-stock
5 mg ¥2500 In-stock
10 mg ¥3750 In-stock
25 mg ¥7500 In-stock
50 mg ¥12000 In-stock
100 mg 询价

* Please select Quantity before adding items.

Indophagolin 相关产品

相关化合物库:

  • Bioactive Compound Library Plus
  • GPCR/G Protein Compound Library
  • Membrane Transporter/Ion Channel Compound Library
  • Neuronal Signaling Compound Library
  • Anti-Cancer Compound Library
  • Autophagy Compound Library
  • Neurotransmitter Receptor Compound Library
  • Anti-Alzheimer’s Disease Compound Library
  • Anti-Parkinson’s Disease Compound Library
  • Neurodegenerative Disease-related Compound Library

生物活性

Indophagolin is a potent, indoline-containing autophagy inhibitor (IC50=140 nM). Indophagolin antagonizes the purinergic receptor P2X4 as well as P2X1 and P2X3 with IC50s of 2.71, 2.40 and 3.49 μM, respectively. Indophagolin also antagonizes the Gq-protein-coupled P2Y4, P2Y6, and P2Y11 receptors (IC50s =3.4~15.4 μM). Indophagolin has a strong antagonistic effect on serotonin receptor 5-HT6 (IC50=1.0 μM) and a moderate effect on receptors 5-HT1B, 5-HT2B, 5-HT4e, and 5-HT7[1].

IC50 & Target[1]

P2X1

2.4 μM (IC50)

P2X4

2.71 μM (IC50)

P2Y11

3.4 μM (IC50)

P2X3

3.49 μM (IC50)

P2Y4

4.89 μM (IC50)

P2Y6

15.4 μM (IC50)

Autophagy

140 nM (IC50)

5-HT6 Receptor

1.0 μM (IC50)

体外研究
(In Vitro)

Indophagolin (10 μM) inhibits autophagosome formation in MCF7 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

523.75

Formula

C19H15BrClF3N2O3S

CAS 号

1207660-00-1

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

溶解性数据
In Vitro: 

DMSO : 250 mg/mL (477.33 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 1.9093 mL 9.5465 mL 19.0931 mL
5 mM 0.3819 mL 1.9093 mL 3.8186 mL
10 mM 0.1909 mL 0.9547 mL 1.9093 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 (protect from light)。-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 (3.97 mM); Suspended solution; Need ultrasonic

    此方案可获得 2.08 mg/mL (3.97 mM) 的均匀悬浊液,悬浊液可用于口服和腹腔注射。

    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% corn oil

    Solubility: ≥ 2.08 mg/mL (3.97 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (3.97 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]. Carnero Corrales MA, et al. Thermal proteome profiling identifies the membrane-bound purinergic receptor P2X4 as a target of the autophagy inhibitor indophagolin [published online ahead of print, 2021 Mar 9]. Cell Chem Biol. 2021;S2451-9456(21)00102-1.

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

Indophagolin

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。

Indophagolin  纯度: 98.05%

Indophagolin 是一种有效的含 indoline 的自噬 (autophagy) 抑制剂 (IC50=140 nM)。Indophagolin 拮抗嘌呤能受体P2X4、P2X1 和 P2X3,IC50 分别为 2.71、2.40 和 3.49 μM。Indophagolin 还拮抗 Gq 蛋白偶联的 P2Y4、P2Y6 和 P2Y11 受体(IC50s =3.4~15.4 μM)。Indophagolin 五羟色胺受体5-HT6 有较强的拮抗作用 (IC50=1.0 μM),对 5-HT1B、5-HT2B、5-HT4e 和 5-HT7 有中度拮抗作用。

Indophagolin

Indophagolin Chemical Structure

CAS No. : 1207660-00-1

规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ¥2881 In-stock
5 mg ¥2500 In-stock
10 mg ¥3750 In-stock
25 mg ¥7500 In-stock
50 mg ¥12000 In-stock
100 mg 询价

* Please select Quantity before adding items.

Indophagolin 相关产品

相关化合物库:

  • Bioactive Compound Library Plus
  • GPCR/G Protein Compound Library
  • Membrane Transporter/Ion Channel Compound Library
  • Neuronal Signaling Compound Library
  • Anti-Cancer Compound Library
  • Autophagy Compound Library
  • Neurotransmitter Receptor Compound Library
  • Anti-Alzheimer’s Disease Compound Library
  • Anti-Parkinson’s Disease Compound Library
  • Neurodegenerative Disease-related Compound Library

生物活性

Indophagolin is a potent, indoline-containing autophagy inhibitor (IC50=140 nM). Indophagolin antagonizes the purinergic receptor P2X4 as well as P2X1 and P2X3 with IC50s of 2.71, 2.40 and 3.49 μM, respectively. Indophagolin also antagonizes the Gq-protein-coupled P2Y4, P2Y6, and P2Y11 receptors (IC50s =3.4~15.4 μM). Indophagolin has a strong antagonistic effect on serotonin receptor 5-HT6 (IC50=1.0 μM) and a moderate effect on receptors 5-HT1B, 5-HT2B, 5-HT4e, and 5-HT7[1].

IC50 & Target[1]

P2X1

2.4 μM (IC50)

P2X4

2.71 μM (IC50)

P2Y11

3.4 μM (IC50)

P2X3

3.49 μM (IC50)

P2Y4

4.89 μM (IC50)

P2Y6

15.4 μM (IC50)

Autophagy

140 nM (IC50)

5-HT6 Receptor

1.0 μM (IC50)

体外研究
(In Vitro)

Indophagolin (10 μM) inhibits autophagosome formation in MCF7 cells[1].

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

分子量

523.75

Formula

C19H15BrClF3N2O3S

CAS 号

1207660-00-1

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

溶解性数据
In Vitro: 

DMSO : 250 mg/mL (477.33 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 1.9093 mL 9.5465 mL 19.0931 mL
5 mM 0.3819 mL 1.9093 mL 3.8186 mL
10 mM 0.1909 mL 0.9547 mL 1.9093 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 (protect from light)。-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 (3.97 mM); Suspended solution; Need ultrasonic

    此方案可获得 2.08 mg/mL (3.97 mM) 的均匀悬浊液,悬浊液可用于口服和腹腔注射。

    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% corn oil

    Solubility: ≥ 2.08 mg/mL (3.97 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (3.97 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 Shanghai Jinpan Biotech Co Ltd 网站选购。
参考文献
  • [1]. Carnero Corrales MA, et al. Thermal proteome profiling identifies the membrane-bound purinergic receptor P2X4 as a target of the autophagy inhibitor indophagolin [published online ahead of print, 2021 Mar 9]. Cell Chem Biol. 2021;S2451-9456(21)00102-1.

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

PD180970

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。

PD180970 

PD180970 是一种高效且具有 ATP 竞争性的 p210Bcr-Abl 激酶抑制剂,可抑制 p210Bcr-Abl 的自磷酸化,IC50 为 5 nM。PD180970 还抑制 SrcKIT 激酶,IC50 分别为 0.8 nM 和 50 nM。PD180970 可诱导 K562 白血病细胞凋亡 (apoptosis),可用于慢性粒细胞白血病的研究。

PD180970

PD180970 Chemical Structure

CAS No. : 287204-45-9

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

PD180970 is a highly potent and ATP-competitive p210Bcr-Abl kinase inhibitor, with an IC50 of 5 nM for inhibiting the autophosphorylation of p210Bcr-Abl. PD180970 also inhibits Src and KIT kinase with IC50s of 0.8 nM and 50 nM, respectively. PD180970 indcues apoptosis of K562 leukemic cells, and can be used for chronic myelogenous leukemia research[1][2][3].

IC50 & Target[1][2]

Bcr-Abl

5 nM (IC50, p210Bcr-Abl kinase)

Src

0.8 nM (IC50)

KIT

50 nM (IC50)

体外研究
(In Vitro)

PD180970 (0.5 μM; 24-96 hours) treatment causes cell death K562 cells[1].
PD180970 (0.5 μM; 24-48 hours) treatment induces apoptosis of K562 cells. The result shows increase in annexin V-PI double-positive cells[1].
PD180970 inhibits tyrosine phosphorylation of p210Bcr-Abl, Gab2, and CrkL in K562 cells with IC50 values of 170 nM, 80 nM, and 80 nM, respectively. In vitro, PD180970 potently inhibits autophosphorylation of p210Bcr-Abl (IC50 of 5 nM) and the kinase activity of purified recombinant Abl tyrosine kinase (IC50 of 2.2 nM)[1].
The blocking Bcr-Abl kinase activity using PD180970 in the human K562 CML cell line resulted in inhibition of Stat5 DNA-binding activity with an IC50 of 5 nM[2].

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

Cell Viability Assay[1]

Cell Line: K562 cells
Concentration: 0.5 μM
Incubation Time: 24 hours, 48 hours, 72 hours, 96 hours
Result: Resulted in cell death.

Apoptosis Analysis[1]

Cell Line: K562 cells
Concentration: 0.5 μM
Incubation Time: 24 hours, 48 hours
Result: Increased annexin V-positive/PI-negative cells.

体内研究
(In Vivo)

PD180970 (5 mg/kg; intraperitonial injection; daily; for 7 days) mitigates MPTP-induced neuronal loss in mice. PD180970 has the neuroprotective ability in a preclinical mouse model of Parkinson’s disease (PD)[4].

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

Animal Model: Male C57BL/6J mice (3-4 months old) injected with MPTP[4]
Dosage: 5 mg/kg
Administration: Intraperitonial injection; daily; for 7 days
Result: Decreased number of activated microglia on activation by MPTP in mice brains. And showed significant reduction in intensity of Iba1 expression in activated microglia.

分子量

429.27

Formula

C21H15Cl2FN4O

CAS 号

287204-45-9

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]. J F Dorsey, et al. The pyrido[2,3-d]pyrimidine derivative PD180970 inhibits p210Bcr-Abl tyrosine kinase and induces apoptosis of K562 leukemic cells. Cancer Res. 2000 Jun 15;60(12):3127-31.

    [2]. Mei Huang, et al. Inhibition of Bcr-Abl kinase activity by PD180970 blocks constitutive activation of Stat5 and growth of CML cells. Oncogene. 2002 Dec 12;21(57):8804-16.

    [3]. Amie S Corbin, et al. Sensitivity of oncogenic KIT mutants to the kinase inhibitors MLN518 and PD180970. Blood. 2004 Dec 1;104(12):3754-7.

    [4]. Suresh Sn, et al. Small molecule modulator of aggrephagy regulates neuroinflammation to curb pathogenesis of neurodegeneration. EBioMedicine. 2019 Dec;50:260-273.

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

Nur77 modulator 1

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。

Nur77 modulator 1  纯度: 98.23%

Nur77 modulator 1 可结合到Nur77 (KD = 3.58 μM)。Nur77 modulator 1 上调 Nur77 表达,介导Nur77亚细胞定位,诱导Nur77 依赖的内质网应激和自噬,可导致细胞凋亡。抗肝癌生物活性。

Nur77 modulator 1

Nur77 modulator 1 Chemical Structure

CAS No. : 2469975-55-9

规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ¥3820 In-stock
5 mg ¥3500 In-stock
10 mg ¥5800 In-stock
25 mg ¥11000 In-stock
50 mg ¥17000 In-stock
100 mg ¥25000 In-stock
200 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

Nur77 modulator 1 相关产品

相关化合物库:

  • Bioactive Compound Library Plus
  • Apoptosis Compound Library
  • Anti-Cancer Compound Library
  • Endoplasmic Reticulum Stress Compound Library
  • Anti-Liver Cancer Compound Library

生物活性

Nur77 modulator 1 is a good Nur77 binder (KD = 3.58 μM). Nur77 modulator 1 up-regulates Nur77 expression, mediates sub-cellular localization of Nur77, induces Nur77-dependent ER stress and autophagy, and results in cell apoptosis. Anti-hepatoma activity[1].

IC50 & Target

KD: 3.58 μM (Nur77) [1].

体外研究
(In Vitro)

Nur77 modulator 1 (10g, 0-20 μM) displays potent and broad-spectrum antiproliferative activity against all tested three hepatoma cell lines (HepG2, QGY-7703, and SMMC-7721), and less cytotoxicity against LO2 cells (human normal liver cell line)[1].
Nur77 modulator 1 (10g, ) could specifically up-regulate the expression of Nur77 in a dose-dependent manner[1].
Nur77 modulator 1 (10g, 2.0 μM) induces Nur77-dependent apoptosis[1].
Nur77 modulator 1 (10g, 2.0 μM) increased LC3-II and Beclin1 protein levels in a dose-dependent manner (10g treatment does not enhance p62 degradation, indicating that autophagy induced by 10g is incomplete)[1].

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

Cell Viability Assay[1].

Cell Line: Liver cancer cell lines (HepG2, QGY-7703, and SMMC-7721).
Concentration: 0-20 μM.
Incubation Time: 12-24 hours.
Result: Exhibited IC50 values of 0.6 µM, 0.89 µM, 1.40 µM and >20 µM in HepG2, QGY-7703, SMMC-7721 and LO2 cells, respectively.
Reduced the viability in a time-dependent manner.
Induced cell morphology alteration, such as cell shrinkage, vesicles accumulated, and reduced cell number.

体内研究
(In Vivo)

Nur77 modulator 1 (10g, 10 and 20 mg/kg/day) exhibits significant anti-tumor activity in mouse hepatoma HepG2 xenograft with good tolerability[1].

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

Animal Model: Nude mouse hepatoma HepG2 xenograft[1].
Dosage: 10 and 20 mg/kg/day.
Administration: IP, once every day for 15 days.
Result: Lead to substantial suppression of tumor growth.
The tumor growth inhibition (TGI) values at doses of 10mg/kg/day and 20 mg/kg/day were 36.74 % and 62.38 %, respectively.
Exhibited almost no influence on the body weight of experimental mice.

分子量

495.60

Formula

C28H25N5O2S

CAS 号

2469975-55-9

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

溶解性数据
In Vitro: 

DMSO : 125 mg/mL (252.22 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.0178 mL 10.0888 mL 20.1776 mL
5 mM 0.4036 mL 2.0178 mL 4.0355 mL
10 mM 0.2018 mL 1.0089 mL 2.0178 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 (protect from light)。-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% (20% SBE-β-CD in saline)

    Solubility: 2.08 mg/mL (4.20 mM); Suspended solution; Need ultrasonic

    此方案可获得 2.08 mg/mL (4.20 mM) 的均匀悬浊液,悬浊液可用于口服和腹腔注射。

    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
  • 2.

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

    Solubility: ≥ 2.08 mg/mL (4.20 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (4.20 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 Shanghai Jinpan Biotech Co Ltd 网站选购。
参考文献
  • [1]. Baicun Li, et al. Design, synthesis, and biological evaluation of 5-((8-methoxy-2-methylquinolin-4-yl)amino)-1H-indole-2-carbohydrazide derivatives as novel Nur77 modulators. Eur J Med Chem. 2020 Oct 15;204:112608.

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

PD180970

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。

PD180970 

PD180970 是一种高效且具有 ATP 竞争性的 p210Bcr-Abl 激酶抑制剂,可抑制 p210Bcr-Abl 的自磷酸化,IC50 为 5 nM。PD180970 还抑制 SrcKIT 激酶,IC50 分别为 0.8 nM 和 50 nM。PD180970 可诱导 K562 白血病细胞凋亡 (apoptosis),可用于慢性粒细胞白血病的研究。

PD180970

PD180970 Chemical Structure

CAS No. : 287204-45-9

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

PD180970 is a highly potent and ATP-competitive p210Bcr-Abl kinase inhibitor, with an IC50 of 5 nM for inhibiting the autophosphorylation of p210Bcr-Abl. PD180970 also inhibits Src and KIT kinase with IC50s of 0.8 nM and 50 nM, respectively. PD180970 indcues apoptosis of K562 leukemic cells, and can be used for chronic myelogenous leukemia research[1][2][3].

IC50 & Target[1][2]

Bcr-Abl

5 nM (IC50, p210Bcr-Abl kinase)

Src

0.8 nM (IC50)

KIT

50 nM (IC50)

体外研究
(In Vitro)

PD180970 (0.5 μM; 24-96 hours) treatment causes cell death K562 cells[1].
PD180970 (0.5 μM; 24-48 hours) treatment induces apoptosis of K562 cells. The result shows increase in annexin V-PI double-positive cells[1].
PD180970 inhibits tyrosine phosphorylation of p210Bcr-Abl, Gab2, and CrkL in K562 cells with IC50 values of 170 nM, 80 nM, and 80 nM, respectively. In vitro, PD180970 potently inhibits autophosphorylation of p210Bcr-Abl (IC50 of 5 nM) and the kinase activity of purified recombinant Abl tyrosine kinase (IC50 of 2.2 nM)[1].
The blocking Bcr-Abl kinase activity using PD180970 in the human K562 CML cell line resulted in inhibition of Stat5 DNA-binding activity with an IC50 of 5 nM[2].

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

Cell Viability Assay[1]

Cell Line: K562 cells
Concentration: 0.5 μM
Incubation Time: 24 hours, 48 hours, 72 hours, 96 hours
Result: Resulted in cell death.

Apoptosis Analysis[1]

Cell Line: K562 cells
Concentration: 0.5 μM
Incubation Time: 24 hours, 48 hours
Result: Increased annexin V-positive/PI-negative cells.

体内研究
(In Vivo)

PD180970 (5 mg/kg; intraperitonial injection; daily; for 7 days) mitigates MPTP-induced neuronal loss in mice. PD180970 has the neuroprotective ability in a preclinical mouse model of Parkinson’s disease (PD)[4].

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

Animal Model: Male C57BL/6J mice (3-4 months old) injected with MPTP[4]
Dosage: 5 mg/kg
Administration: Intraperitonial injection; daily; for 7 days
Result: Decreased number of activated microglia on activation by MPTP in mice brains. And showed significant reduction in intensity of Iba1 expression in activated microglia.

分子量

429.27

Formula

C21H15Cl2FN4O

CAS 号

287204-45-9

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]. J F Dorsey, et al. The pyrido[2,3-d]pyrimidine derivative PD180970 inhibits p210Bcr-Abl tyrosine kinase and induces apoptosis of K562 leukemic cells. Cancer Res. 2000 Jun 15;60(12):3127-31.

    [2]. Mei Huang, et al. Inhibition of Bcr-Abl kinase activity by PD180970 blocks constitutive activation of Stat5 and growth of CML cells. Oncogene. 2002 Dec 12;21(57):8804-16.

    [3]. Amie S Corbin, et al. Sensitivity of oncogenic KIT mutants to the kinase inhibitors MLN518 and PD180970. Blood. 2004 Dec 1;104(12):3754-7.

    [4]. Suresh Sn, et al. Small molecule modulator of aggrephagy regulates neuroinflammation to curb pathogenesis of neurodegeneration. EBioMedicine. 2019 Dec;50:260-273.

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

PD180970

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。

PD180970 

PD180970 是一种高效且具有 ATP 竞争性的 p210Bcr-Abl 激酶抑制剂,可抑制 p210Bcr-Abl 的自磷酸化,IC50 为 5 nM。PD180970 还抑制 SrcKIT 激酶,IC50 分别为 0.8 nM 和 50 nM。PD180970 可诱导 K562 白血病细胞凋亡 (apoptosis),可用于慢性粒细胞白血病的研究。

PD180970

PD180970 Chemical Structure

CAS No. : 287204-45-9

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

PD180970 is a highly potent and ATP-competitive p210Bcr-Abl kinase inhibitor, with an IC50 of 5 nM for inhibiting the autophosphorylation of p210Bcr-Abl. PD180970 also inhibits Src and KIT kinase with IC50s of 0.8 nM and 50 nM, respectively. PD180970 indcues apoptosis of K562 leukemic cells, and can be used for chronic myelogenous leukemia research[1][2][3].

IC50 & Target[1][2]

Bcr-Abl

5 nM (IC50, p210Bcr-Abl kinase)

Src

0.8 nM (IC50)

KIT

50 nM (IC50)

体外研究
(In Vitro)

PD180970 (0.5 μM; 24-96 hours) treatment causes cell death K562 cells[1].
PD180970 (0.5 μM; 24-48 hours) treatment induces apoptosis of K562 cells. The result shows increase in annexin V-PI double-positive cells[1].
PD180970 inhibits tyrosine phosphorylation of p210Bcr-Abl, Gab2, and CrkL in K562 cells with IC50 values of 170 nM, 80 nM, and 80 nM, respectively. In vitro, PD180970 potently inhibits autophosphorylation of p210Bcr-Abl (IC50 of 5 nM) and the kinase activity of purified recombinant Abl tyrosine kinase (IC50 of 2.2 nM)[1].
The blocking Bcr-Abl kinase activity using PD180970 in the human K562 CML cell line resulted in inhibition of Stat5 DNA-binding activity with an IC50 of 5 nM[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.

Cell Viability Assay[1]

Cell Line: K562 cells
Concentration: 0.5 μM
Incubation Time: 24 hours, 48 hours, 72 hours, 96 hours
Result: Resulted in cell death.

Apoptosis Analysis[1]

Cell Line: K562 cells
Concentration: 0.5 μM
Incubation Time: 24 hours, 48 hours
Result: Increased annexin V-positive/PI-negative cells.

体内研究
(In Vivo)

PD180970 (5 mg/kg; intraperitonial injection; daily; for 7 days) mitigates MPTP-induced neuronal loss in mice. PD180970 has the neuroprotective ability in a preclinical mouse model of Parkinson’s disease (PD)[4].

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: Male C57BL/6J mice (3-4 months old) injected with MPTP[4]
Dosage: 5 mg/kg
Administration: Intraperitonial injection; daily; for 7 days
Result: Decreased number of activated microglia on activation by MPTP in mice brains. And showed significant reduction in intensity of Iba1 expression in activated microglia.

分子量

429.27

Formula

C21H15Cl2FN4O

CAS 号

287204-45-9

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]. J F Dorsey, et al. The pyrido[2,3-d]pyrimidine derivative PD180970 inhibits p210Bcr-Abl tyrosine kinase and induces apoptosis of K562 leukemic cells. Cancer Res. 2000 Jun 15;60(12):3127-31.

    [2]. Mei Huang, et al. Inhibition of Bcr-Abl kinase activity by PD180970 blocks constitutive activation of Stat5 and growth of CML cells. Oncogene. 2002 Dec 12;21(57):8804-16.

    [3]. Amie S Corbin, et al. Sensitivity of oncogenic KIT mutants to the kinase inhibitors MLN518 and PD180970. Blood. 2004 Dec 1;104(12):3754-7.

    [4]. Suresh Sn, et al. Small molecule modulator of aggrephagy regulates neuroinflammation to curb pathogenesis of neurodegeneration. EBioMedicine. 2019 Dec;50:260-273.

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

Nur77 modulator 1

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。

Nur77 modulator 1  纯度: 98.23%

Nur77 modulator 1 可结合到Nur77 (KD = 3.58 μM)。Nur77 modulator 1 上调 Nur77 表达,介导Nur77亚细胞定位,诱导Nur77 依赖的内质网应激和自噬,可导致细胞凋亡。抗肝癌生物活性。

Nur77 modulator 1

Nur77 modulator 1 Chemical Structure

CAS No. : 2469975-55-9

规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ¥3820 In-stock
5 mg ¥3500 In-stock
10 mg ¥5800 In-stock
25 mg ¥11000 In-stock
50 mg ¥17000 In-stock
100 mg ¥25000 In-stock
200 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

Nur77 modulator 1 相关产品

相关化合物库:

  • Bioactive Compound Library Plus
  • Apoptosis Compound Library
  • Anti-Cancer Compound Library
  • Endoplasmic Reticulum Stress Compound Library
  • Anti-Liver Cancer Compound Library

生物活性

Nur77 modulator 1 is a good Nur77 binder (KD = 3.58 μM). Nur77 modulator 1 up-regulates Nur77 expression, mediates sub-cellular localization of Nur77, induces Nur77-dependent ER stress and autophagy, and results in cell apoptosis. Anti-hepatoma activity[1].

IC50 & Target

KD: 3.58 μM (Nur77) [1].

体外研究
(In Vitro)

Nur77 modulator 1 (10g, 0-20 μM) displays potent and broad-spectrum antiproliferative activity against all tested three hepatoma cell lines (HepG2, QGY-7703, and SMMC-7721), and less cytotoxicity against LO2 cells (human normal liver cell line)[1].
Nur77 modulator 1 (10g, ) could specifically up-regulate the expression of Nur77 in a dose-dependent manner[1].
Nur77 modulator 1 (10g, 2.0 μM) induces Nur77-dependent apoptosis[1].
Nur77 modulator 1 (10g, 2.0 μM) increased LC3-II and Beclin1 protein levels in a dose-dependent manner (10g treatment does not enhance p62 degradation, indicating that autophagy induced by 10g is incomplete)[1].

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

Cell Viability Assay[1].

Cell Line: Liver cancer cell lines (HepG2, QGY-7703, and SMMC-7721).
Concentration: 0-20 μM.
Incubation Time: 12-24 hours.
Result: Exhibited IC50 values of 0.6 µM, 0.89 µM, 1.40 µM and >20 µM in HepG2, QGY-7703, SMMC-7721 and LO2 cells, respectively.
Reduced the viability in a time-dependent manner.
Induced cell morphology alteration, such as cell shrinkage, vesicles accumulated, and reduced cell number.

体内研究
(In Vivo)

Nur77 modulator 1 (10g, 10 and 20 mg/kg/day) exhibits significant anti-tumor activity in mouse hepatoma HepG2 xenograft with good tolerability[1].

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

Animal Model: Nude mouse hepatoma HepG2 xenograft[1].
Dosage: 10 and 20 mg/kg/day.
Administration: IP, once every day for 15 days.
Result: Lead to substantial suppression of tumor growth.
The tumor growth inhibition (TGI) values at doses of 10mg/kg/day and 20 mg/kg/day were 36.74 % and 62.38 %, respectively.
Exhibited almost no influence on the body weight of experimental mice.

分子量

495.60

Formula

C28H25N5O2S

CAS 号

2469975-55-9

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

溶解性数据
In Vitro: 

DMSO : 125 mg/mL (252.22 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.0178 mL 10.0888 mL 20.1776 mL
5 mM 0.4036 mL 2.0178 mL 4.0355 mL
10 mM 0.2018 mL 1.0089 mL 2.0178 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 (protect from light)。-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% (20% SBE-β-CD in saline)

    Solubility: 2.08 mg/mL (4.20 mM); Suspended solution; Need ultrasonic

    此方案可获得 2.08 mg/mL (4.20 mM) 的均匀悬浊液,悬浊液可用于口服和腹腔注射。

    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
  • 2.

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

    Solubility: ≥ 2.08 mg/mL (4.20 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (4.20 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 Shanghai Jinpan Biotech Co Ltd 网站选购。
参考文献
  • [1]. Baicun Li, et al. Design, synthesis, and biological evaluation of 5-((8-methoxy-2-methylquinolin-4-yl)amino)-1H-indole-2-carbohydrazide derivatives as novel Nur77 modulators. Eur J Med Chem. 2020 Oct 15;204:112608.

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