标签归档：polymerization

Tubulin polymerization-IN-17

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。

Tubulin polymerization-IN-17 

Tubulin aggregation-IN-17 (compound 23g) 是一种有效的 tubulin 聚合抑制剂。Tubulin aggregation-IN-17 表现出微管蛋白解聚和诱导细胞凋亡 (apoptosis) 并抑制迁移。Tubulin aggregation-IN-17 具有研究癌症疾病的潜力。

Tubulin polymerization-IN-17

Tubulin polymerization-IN-17 Chemical Structure

CAS No. : 2454175-89-2

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生物活性

Tubulin polymerization-IN-17 (compound 23g) is a potent inhibitor of tubulin polymerization. Tubulin polymerization-IN-17 exhibits tubulin depolymerization and induced cell apoptosis and inhibits migration. Tubulin polymerization-IN-17 has the potential for the research of cancer diseases[1].

分子量

429.46

Formula

C26H23NO5
CAS 号

2454175-89-2
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]. Guo Q, et al. Ligand- and structural-based discovery of potential small molecules that target the colchicine site of tubulin for cancer treatment. Eur J Med Chem. 2020;196:112328.

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Tubulin polymerization-IN-15

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。

Tubulin polymerization-IN-15 

Tubulin aggregation-IN-15 (compound 4) 是一种有效的 tubulin 聚合抑制剂。Tubulin aggregation-IN-15 具有研究癌症疾病的潜力。

Tubulin polymerization-IN-15

Tubulin polymerization-IN-15 Chemical Structure

CAS No. : 2055517-66-1

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生物活性

Tubulin polymerization-IN-15 (compound 4) is a potent inhibitor of tubulin polymerization. Tubulin polymerization-IN-15 has the potential for the research of cancer diseases[1].

分子量

339.35

Formula

C18H17N3O4
CAS 号

2055517-66-1
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]. Huang L, et al. Design, synthesis and bio-evaluation of novel 2-aryl-4-(3,4,5-trimethoxy-benzoyl)-5-substituted-1,2,3-triazoles as the tubulin polymerization inhibitors. Eur J Med Chem. 2020;186:111846.

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Tubulin polymerization-IN-19

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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。

Tubulin polymerization-IN-19 

Tubulin aggregation-IN-19 (compound 4) 是一种有效的 tubulin 聚合抑制剂。Tubulin aggregation-IN-19 具有研究乳腺癌和耐药结肠癌的潜力。

Tubulin polymerization-IN-19

Tubulin polymerization-IN-19 Chemical Structure

CAS No. : 2340345-85-7

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生物活性

Tubulin polymerization-IN-19 (compound 4) is a potent inhibitor of tubulin polymerization. Tubulin polymerization-IN-20 has the potential for the research of breast cancers and chemoresistant colon cancers[1].

分子量

419.47

Formula

C25H25NO5
CAS 号

2340345-85-7
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]. Malebari AM, et al. β-Lactams with antiproliferative and antiapoptotic activity in breast and chemoresistant colon cancer cells. Eur J Med Chem. 2020;189:112050.

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Tubulin polymerization-IN-16

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。

Tubulin polymerization-IN-16 

Tubulin aggregation-IN-16 (compound 5g) 是一种有效的tubulin 聚合抑制剂。Tubulin aggregation-IN-16 对癌细胞最有效，IC50 值为 0.084-0.221 μM。Tubulin 聚合-IN-16 可有效破坏微管/微管蛋白动力学，在 SGC-7901 细胞中诱导 G2/M 期细胞周期停滞。

Tubulin polymerization-IN-16

Tubulin polymerization-IN-16 Chemical Structure

CAS No. : 2296731-38-7

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生物活性

Tubulin polymerization-IN-16 (compound 5g) is a potent inhibitor of tubulin polymerization. Tubulin polymerization-IN-16 shows most potent against cancer cells, with IC50 values of 0.084-0.221 μM. Tubulin polymerization-IN-16 potently disrupts microtubule/tubulin dynamics, induces cell cycle arrest at G2/M phase in SGC-7901 cells[1].

分子量

465.50

Formula

C24H27N5O5
CAS 号

2296731-38-7
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]. Huang L, et al. Design, synthesis and bio-evaluation of novel 2-aryl-4-(3,4,5-trimethoxy-benzoyl)-5-substituted-1,2,3-triazoles as the tubulin polymerization inhibitors. Eur J Med Chem. 2020;186:111846.

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

Tubulin polymerization-IN-20

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。

Tubulin polymerization-IN-20 

Tubulin aggregation-IN-20 (compound 11) 是一种有效的 tubulin 聚合抑制剂。Tubulin aggregation-IN-20 具有研究乳腺癌和耐药结肠癌的潜力。

Tubulin polymerization-IN-20

Tubulin polymerization-IN-20 Chemical Structure

CAS No. : 2410619-45-1

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生物活性

Tubulin polymerization-IN-20 (compound 11) is a potent inhibitor of tubulin polymerization. Tubulin polymerization-IN-20 has the potential for the research of breast cancers and chemoresistant colon cancers[1].

分子量

437.46

Formula

C25H24FNO5
CAS 号

2410619-45-1
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]. Malebari AM, et al. β-Lactams with antiproliferative and antiapoptotic activity in breast and chemoresistant colon cancer cells. Eur J Med Chem. 2020;189:112050.

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

Tubulin polymerization-IN-18

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。

Tubulin polymerization-IN-18 

Tubulin aggregation-IN-18 (compound 3) 是一种有效的 tubulin 聚合抑制剂。Tubulin aggregation-IN-18 具有研究乳腺癌和耐药结肠癌的潜力。

Tubulin polymerization-IN-18

Tubulin polymerization-IN-18 Chemical Structure

CAS No. : 1258011-23-2

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生物活性

Tubulin polymerization-IN-18 (compound 8) is a potent inhibitor of tubulin polymerization. Tubulin polymerization-IN-18 has the potential for the research of breast cancers and chemoresistant colon cancers[1].

分子量

435.47

Formula

C25H25NO6
CAS 号

1258011-23-2
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]. Malebari AM, et al. β-Lactams with antiproliferative and antiapoptotic activity in breast and chemoresistant colon cancer cells. Eur J Med Chem. 2020;189:112050.

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

Tubulin polymerization-IN-7

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。

Tubulin polymerization-IN-7 

Tubulin aggregation-IN-7 (compound 5) 是一种有效的tubulin 聚合抑制剂。Tubulin aggregation-IN-7 具有研究癌症疾病的潜力。

Tubulin polymerization-IN-7

Tubulin polymerization-IN-7 Chemical Structure

CAS No. : 1394017-46-9

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生物活性

Tubulin polymerization-IN-7 (compound 5) is a potent inhibitor of tubulin polymerization. Tubulin polymerization-IN-7 has the potential for the research of cancer diseases[1].

分子量

544.58

Formula

C28H24N4O6S
CAS 号

1394017-46-9
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]. Chen L, et al. Concise synthesis and preliminary biological evaluation of new triazolylthioacetone derivatives bearing pyridine, pyrazine, and 3,4,5-trimethoxybenzyl fragment. Bioorg Med Chem Lett. 2022;66:128721.

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Tubulin polymerization-IN-8

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。

Tubulin polymerization-IN-8 

Tubulin aggregation-IN-8 (compound IIc) 是一种有效的tubulin 聚合抑制剂。Tubulin aggregation-IN-8 浓度依赖性地导致 HCT116 肿瘤细胞 G2/M 期细胞周期停滞，并显示显着抑制微管蛋白聚合，IC50 值为 12.7 μM。Tubulin aggregation-IN-8 具有研究癌症疾病的潜力。

Tubulin polymerization-IN-8

Tubulin polymerization-IN-8 Chemical Structure

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生物活性

Tubulin polymerization-IN-8 (compound IIc) is a potent inhibitor of tubulin polymerization. Tubulin polymerization-IN-8 concentration-dependently causes cell cycle arrest at the G2/M phase in HCT116 tumor cells, and displays a significant inhibition of tubulin polymerization with an IC50 value of 12.7 μM. Tubulin polymerization-IN-8 has the potential for the research of cancer diseases[ 1].

分子量

428.50

Formula

C21H24N4O4S
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]. Chen L, et al. Concise synthesis and preliminary biological evaluation of new triazolylthioacetone derivatives bearing pyridine, pyrazine, and 3,4,5-trimethoxybenzyl fragment. Bioorg Med Chem Lett. 2022;66:128721.

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

Tubulin polymerization-IN-9

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。

Tubulin polymerization-IN-9 

Tubulin polymerization-IN-9 是一种有效的微管蛋白 (tubulin) 抑制剂，IC50 为 1.82 μM。Tubulin polymerization-IN-9 能引起细胞周期阻滞在 G2/M 期，诱导 K562 细胞凋亡 (apoptosis) 和线粒体去极化。Tubulin polymerization-IN-9 具有强效的抗血管和抗肿瘤活性。

Tubulin polymerization-IN-9

Tubulin polymerization-IN-9 Chemical Structure

CAS No. : 2485020-93-5

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

Tubulin polymerization-IN-9 is a potent tubulin inhibitor with IC50 of 1.82 μM. Tubulin polymerization-IN-9 causes cell cycle arrest at G2/M phase, and induces cell apoptosis and depolarized mitochondria of K562 cells. Tubulin polymerization-IN-9 has potent anti-vascular and antitumor activities[1].

IC50 & Target

IC50: 1.82 μM (tubulin)[1]
体外研究
(In Vitro)

Tubulin polymerization-IN-9 (compound 11k) (0.1, 1, 10 μM; 72 hours) has potent activity against these three cancer cell lines with IC50 values ranging from 0.287 to 0.621 μM[1].
Tubulin polymerization-IN-9 (0.15, 0.3 and 0.6 μM; 24 hours) induces a dose-dependent collapse of the microtubule networks[1].
Tubulin polymerization-IN-9 (0.15, 0.3 and 0.6 μM; 48 hours) observes a gradual accumulation of cells at G2/M phase in K562 cells[1].
Tubulin polymerization-IN-9 (0.15, 0.3 and 0.6 μM; 72 hours) effectively induces cell apoptosis in K562 cells in a concentration-dependent manner[1].
Tubulin polymerization-IN-9 (0.15, 0.3 and 0.6 μM; 24 hours) causes mitochondrial depolarization of K562 cells in the process of apoptosis[1].

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

Cell Proliferation Assay

Cell Line: K562 HepG2 and HCT-8 cells[1]
Concentration: 0.1, 1, 10 μM
Incubation Time: 72 hours
Result: Showed potent activity against these three cancer cell lines with IC50 values ranging from 0.287 to 0.621 μM.

Immunofluorescence

Cell Line: K562 cells[1]
Concentration: 0.15, 0.3 and 0.6 μM
Incubation Time: 24 hours
Result: Induced a dose-dependent collapse of the microtubule networks.

Cell Cycle Analysis

Cell Line: K562 cells[1]
Concentration: 0.15, 0.3 and 0.6 μM
Incubation Time: 48 hours
Result: Observed a gradual accumulation of cells at G2/M phase in K562 cells.

Apoptosis Analysis

Cell Line: K562 cells[1]
Concentration: 0.15, 0.3 and 0.6 μM
Incubation Time: 72 hours
Result: Effectively induced cell apoptosis in K562 cells in a concentration-dependent manner.

体内研究
(In Vivo)

Tubulin polymerization-IN-9 (15 and 30 mg/kg; IV; once a day, for 21 days) effectively suppresses the tumor volume and reduces tumor weight by 71.1% at a dose of 30 mg/kg[1].

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

Animal Model: Male ICR mice (5 weeks; injected with H22 cells; n=6)[1]
Dosage: 15 and 30 mg/kg
Administration: IV; once a day, for 21 days
Result: Effectively suppressed the tumor volume and reduced tumor weight by 71.1% at a dose of 30 mg/kg.

分子量

420.32

Formula

C19H19NO5Se
CAS 号

2485020-93-5
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]. Zhu H, Sun H, Liu Y, et al. Design, synthesis and biological evaluation of vinyl selenone derivatives as novel microtubule polymerization inhibitors. Eur J Med Chem. 2020;207:112716.

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

Tubulin polymerization-IN-9

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。

Tubulin polymerization-IN-9 

Tubulin polymerization-IN-9 是一种有效的微管蛋白 (tubulin) 抑制剂，IC50 为 1.82 μM。Tubulin polymerization-IN-9 能引起细胞周期阻滞在 G2/M 期，诱导 K562 细胞凋亡 (apoptosis) 和线粒体去极化。Tubulin polymerization-IN-9 具有强效的抗血管和抗肿瘤活性。

Tubulin polymerization-IN-9

Tubulin polymerization-IN-9 Chemical Structure

CAS No. : 2485020-93-5

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

Tubulin polymerization-IN-9 is a potent tubulin inhibitor with IC50 of 1.82 μM. Tubulin polymerization-IN-9 causes cell cycle arrest at G2/M phase, and induces cell apoptosis and depolarized mitochondria of K562 cells. Tubulin polymerization-IN-9 has potent anti-vascular and antitumor activities[1].

IC50 & Target

IC50: 1.82 μM (tubulin)[1]
体外研究
(In Vitro)

Tubulin polymerization-IN-9 (compound 11k) (0.1, 1, 10 μM; 72 hours) has potent activity against these three cancer cell lines with IC50 values ranging from 0.287 to 0.621 μM[1].
Tubulin polymerization-IN-9 (0.15, 0.3 and 0.6 μM; 24 hours) induces a dose-dependent collapse of the microtubule networks[1].
Tubulin polymerization-IN-9 (0.15, 0.3 and 0.6 μM; 48 hours) observes a gradual accumulation of cells at G2/M phase in K562 cells[1].
Tubulin polymerization-IN-9 (0.15, 0.3 and 0.6 μM; 72 hours) effectively induces cell apoptosis in K562 cells in a concentration-dependent manner[1].
Tubulin polymerization-IN-9 (0.15, 0.3 and 0.6 μM; 24 hours) causes mitochondrial depolarization of K562 cells in the process of apoptosis[1].

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

Cell Proliferation Assay

Cell Line: K562 HepG2 and HCT-8 cells[1]
Concentration: 0.1, 1, 10 μM
Incubation Time: 72 hours
Result: Showed potent activity against these three cancer cell lines with IC50 values ranging from 0.287 to 0.621 μM.

Immunofluorescence

Cell Line: K562 cells[1]
Concentration: 0.15, 0.3 and 0.6 μM
Incubation Time: 24 hours
Result: Induced a dose-dependent collapse of the microtubule networks.

Cell Cycle Analysis

Cell Line: K562 cells[1]
Concentration: 0.15, 0.3 and 0.6 μM
Incubation Time: 48 hours
Result: Observed a gradual accumulation of cells at G2/M phase in K562 cells.

Apoptosis Analysis

Cell Line: K562 cells[1]
Concentration: 0.15, 0.3 and 0.6 μM
Incubation Time: 72 hours
Result: Effectively induced cell apoptosis in K562 cells in a concentration-dependent manner.

体内研究
(In Vivo)

Tubulin polymerization-IN-9 (15 and 30 mg/kg; IV; once a day, for 21 days) effectively suppresses the tumor volume and reduces tumor weight by 71.1% at a dose of 30 mg/kg[1].

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

Animal Model: Male ICR mice (5 weeks; injected with H22 cells; n=6)[1]
Dosage: 15 and 30 mg/kg
Administration: IV; once a day, for 21 days
Result: Effectively suppressed the tumor volume and reduced tumor weight by 71.1% at a dose of 30 mg/kg.

分子量

420.32

Formula

C19H19NO5Se
CAS 号

2485020-93-5
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]. Zhu H, Sun H, Liu Y, et al. Design, synthesis and biological evaluation of vinyl selenone derivatives as novel microtubule polymerization inhibitors. Eur J Med Chem. 2020;207:112716.

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

Tubulin polymerization-IN-9

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。

Tubulin polymerization-IN-9 

Tubulin polymerization-IN-9 是一种有效的微管蛋白 (tubulin) 抑制剂，IC50 为 1.82 μM。Tubulin polymerization-IN-9 能引起细胞周期阻滞在 G2/M 期，诱导 K562 细胞凋亡 (apoptosis) 和线粒体去极化。Tubulin polymerization-IN-9 具有强效的抗血管和抗肿瘤活性。

Tubulin polymerization-IN-9

Tubulin polymerization-IN-9 Chemical Structure

CAS No. : 2485020-93-5

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

Tubulin polymerization-IN-9 is a potent tubulin inhibitor with IC50 of 1.82 μM. Tubulin polymerization-IN-9 causes cell cycle arrest at G2/M phase, and induces cell apoptosis and depolarized mitochondria of K562 cells. Tubulin polymerization-IN-9 has potent anti-vascular and antitumor activities[1].

IC50 & Target

IC50: 1.82 μM (tubulin)[1]
体外研究
(In Vitro)

Tubulin polymerization-IN-9 (compound 11k) (0.1, 1, 10 μM; 72 hours) has potent activity against these three cancer cell lines with IC50 values ranging from 0.287 to 0.621 μM[1].
Tubulin polymerization-IN-9 (0.15, 0.3 and 0.6 μM; 24 hours) induces a dose-dependent collapse of the microtubule networks[1].
Tubulin polymerization-IN-9 (0.15, 0.3 and 0.6 μM; 48 hours) observes a gradual accumulation of cells at G2/M phase in K562 cells[1].
Tubulin polymerization-IN-9 (0.15, 0.3 and 0.6 μM; 72 hours) effectively induces cell apoptosis in K562 cells in a concentration-dependent manner[1].
Tubulin polymerization-IN-9 (0.15, 0.3 and 0.6 μM; 24 hours) causes mitochondrial depolarization of K562 cells in the process of apoptosis[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 Proliferation Assay

Cell Line: K562 HepG2 and HCT-8 cells[1]
Concentration: 0.1, 1, 10 μM
Incubation Time: 72 hours
Result: Showed potent activity against these three cancer cell lines with IC50 values ranging from 0.287 to 0.621 μM.

Immunofluorescence

Cell Line: K562 cells[1]
Concentration: 0.15, 0.3 and 0.6 μM
Incubation Time: 24 hours
Result: Induced a dose-dependent collapse of the microtubule networks.

Cell Cycle Analysis

Cell Line: K562 cells[1]
Concentration: 0.15, 0.3 and 0.6 μM
Incubation Time: 48 hours
Result: Observed a gradual accumulation of cells at G2/M phase in K562 cells.

Apoptosis Analysis

Cell Line: K562 cells[1]
Concentration: 0.15, 0.3 and 0.6 μM
Incubation Time: 72 hours
Result: Effectively induced cell apoptosis in K562 cells in a concentration-dependent manner.

体内研究
(In Vivo)

Tubulin polymerization-IN-9 (15 and 30 mg/kg; IV; once a day, for 21 days) effectively suppresses the tumor volume and reduces tumor weight by 71.1% at a dose of 30 mg/kg[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: Male ICR mice (5 weeks; injected with H22 cells; n=6)[1]
Dosage: 15 and 30 mg/kg
Administration: IV; once a day, for 21 days
Result: Effectively suppressed the tumor volume and reduced tumor weight by 71.1% at a dose of 30 mg/kg.

分子量

420.32

Formula

C19H19NO5Se
CAS 号

2485020-93-5
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]. Zhu H, Sun H, Liu Y, et al. Design, synthesis and biological evaluation of vinyl selenone derivatives as novel microtubule polymerization inhibitors. Eur J Med Chem. 2020;207:112716.

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

Tubulin polymerization-IN-4

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。

Tubulin polymerization-IN-4 

Tubulin polymerization-IN-4 是一种有效的微管蛋白聚合体 (tubulin polymerization) 抑制剂，IC50 为 4.6 μM。Tubulin polymerization-IN-4 对HeLa细胞可破坏微管蛋白聚合和血管系统，将细胞周期阻滞在G2/M期，诱导细胞凋亡 (apoptosis)，抑制细胞的克隆发生和迁移。

Tubulin polymerization-IN-4

Tubulin polymerization-IN-4 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

Tubulin polymerization-IN-4 is a potent tubulin polymerization inhibitor with IC50 value of 4.6 μM. Tubulin polymerization-IN-4 can disrupt tubulin polymerization and vasculature, arrest the cell cycle at the G2/M phase, induce apoptosis, and suppress clonogenesis and migration in HeLa cells. Tubulin polymerization-IN-4 can be used for researching cervical cancer[1].

IC50 & Target

IC50: 4.6 μM (tubulin)[1]
体外研究
(In Vitro)

Tubulin polymerization-IN-4 (compound 9j) (0-1 μM; 48 hours) exhibits sub-micromolar inhibitory activities against HeLa, SiHa and MS751[1].
Tubulin polymerization-IN-4 (3, 6 and 12.5 μM; 0-20 min) inhibits tubulin polymerization in a concentration-dependent manner with the inhibition percentages of 39%, 54%, and 77% at 3, 6 and 12.5 μM[1].
Tubulin polymerization-IN-4 (1-100 μM; 2 hours) inhibits the formation of EBI-β-tubulin adduct in a concentration-dependent manner[1].
Tubulin polymerization-IN-4 (0.2 μM; 1 and 2 hours) disrupts the HUVEC-formed vascular tube[1].
Tubulin polymerization-IN-4 (0.1-0.4 μM; 24 hours) increases cell distribution to the G2/M phase in a concentration-dependent manner[1].
Tubulin polymerization-IN-4 (0.1-0.4 μM; 24 hours) induces apoptosis of HeLa cells[1].
Tubulin polymerization-IN-4 (20, 50, 100 nM; 14 days) reduces new colony formation and suppresses HeLa cell growth for 14 days in a dose-dependent manner[1].
Tubulin polymerization-IN-4 (0.1, 0.2 and 0.4 μM; 24 hours) effectively inhibits the migration of HeLa cells in a concentration-dependent manner[1].
Tubulin polymerization-IN-4 (0-200 μM; 24 hours) exhibits good renal safety profile, with IC50 of 188 ± 16 μM in HK-2 cells[1].

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

Cell Proliferation Assay

Cell Line: HeLa, SiHa and MS751[1]
Concentration: 0-1 μM
Incubation Time: 48 hours
Result: Exhibited sub-micromolar inhibitory activities against HeLa, SiHa and MS751 with IC50s of 0.09 ± 0.02 μM, 0.15 ± 0.01 μM, 0.11 ± 0.03 μM.

Cell Cycle Analysis

Cell Line: HeLa cells[1]
Concentration: 0.1, 0.2 and 0.4 μM
Incubation Time: 24 hours
Result: Increased cell distribution to the G2/M phase in a concentration-dependent way, arresting 24.7%, 47.6% and 71.7% of the cells in this phase at 0.1, 0.2 and 0.4 μM, respectively.

Apoptosis Analysis

Cell Line: HeLa cells[1]
Concentration: 0.1, 0.2 and 0.4 μM
Incubation Time: 24 hours
Result: Induced 35.9%, 66.4% and 84.4% of cell population undergoing apoptosis at 0.1 μM, 0.2 μM, 0.4 μM, respectively.

Cell Cytotoxicity Assay

Cell Line: HK-2 cells[1]
Concentration: 0-200 μM
Incubation Time: 24 hours
Result: Exhibited good renal safety profile, with IC50 of 188 ± 16 μM in HK-2 cells.

体内研究
(In Vivo)

Tubulin polymerization-IN-4 (100-1000 mg/kg; IP, single) exhibits extremely low toxicity with LD50 over 1000 mg/kg[1].
Tubulin polymerization-IN-4 (30 and 60 mg/kg; IP; daily for 21 days) inhibits the tumor growth, with TGI of 35% and 58% at dosing 30 and 60 mg/kg[1].
Tubulin polymerization-IN-4 (30 mg/kg; IP; single) presents the modest pharmacokinetic properties[1].
Pharmacokinetic Parameters of Tubulin polymerization-IN-4 in ICR mice[1].

IP (30 mg/kg)
T1/2 (h) 1.56 ± 0.28
Tmax (h) 0.25
Cmax (μg/L) 6215 ± 308
AUC0-t (μg/L·h) 5609 ± 347
AUC0-∞ (μg/L·h) 5940 ± 347
VZ/F (L/kg) 11.35 ± 1.29
CLZ/F (L/h/kg) 5.05 ± 0.91
MRT (h) 1.77 ± 0.43

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

400.86

Formula

C21H21ClN2O4
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]. Huo Z, Liu K, Zhang X, Liang Y, Sun X. Discovery of pyrimidine-bridged CA-4 CBSIs for the treatment of cervical cancer in combination with cisplatin with significantly reduced nephrotoxicity. Eur J Med Chem. 2022;235:114271.

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

Tubulin polymerization-IN-4

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。

Tubulin polymerization-IN-4 

Tubulin polymerization-IN-4 是一种有效的微管蛋白聚合体 (tubulin polymerization) 抑制剂，IC50 为 4.6 μM。Tubulin polymerization-IN-4 对HeLa细胞可破坏微管蛋白聚合和血管系统，将细胞周期阻滞在G2/M期，诱导细胞凋亡 (apoptosis)，抑制细胞的克隆发生和迁移。

Tubulin polymerization-IN-4

Tubulin polymerization-IN-4 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

Tubulin polymerization-IN-4 is a potent tubulin polymerization inhibitor with IC50 value of 4.6 μM. Tubulin polymerization-IN-4 can disrupt tubulin polymerization and vasculature, arrest the cell cycle at the G2/M phase, induce apoptosis, and suppress clonogenesis and migration in HeLa cells. Tubulin polymerization-IN-4 can be used for researching cervical cancer[1].

IC50 & Target

IC50: 4.6 μM (tubulin)[1]
体外研究
(In Vitro)

Tubulin polymerization-IN-4 (compound 9j) (0-1 μM; 48 hours) exhibits sub-micromolar inhibitory activities against HeLa, SiHa and MS751[1].
Tubulin polymerization-IN-4 (3, 6 and 12.5 μM; 0-20 min) inhibits tubulin polymerization in a concentration-dependent manner with the inhibition percentages of 39%, 54%, and 77% at 3, 6 and 12.5 μM[1].
Tubulin polymerization-IN-4 (1-100 μM; 2 hours) inhibits the formation of EBI-β-tubulin adduct in a concentration-dependent manner[1].
Tubulin polymerization-IN-4 (0.2 μM; 1 and 2 hours) disrupts the HUVEC-formed vascular tube[1].
Tubulin polymerization-IN-4 (0.1-0.4 μM; 24 hours) increases cell distribution to the G2/M phase in a concentration-dependent manner[1].
Tubulin polymerization-IN-4 (0.1-0.4 μM; 24 hours) induces apoptosis of HeLa cells[1].
Tubulin polymerization-IN-4 (20, 50, 100 nM; 14 days) reduces new colony formation and suppresses HeLa cell growth for 14 days in a dose-dependent manner[1].
Tubulin polymerization-IN-4 (0.1, 0.2 and 0.4 μM; 24 hours) effectively inhibits the migration of HeLa cells in a concentration-dependent manner[1].
Tubulin polymerization-IN-4 (0-200 μM; 24 hours) exhibits good renal safety profile, with IC50 of 188 ± 16 μM in HK-2 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.

Cell Proliferation Assay

Cell Line: HeLa, SiHa and MS751[1]
Concentration: 0-1 μM
Incubation Time: 48 hours
Result: Exhibited sub-micromolar inhibitory activities against HeLa, SiHa and MS751 with IC50s of 0.09 ± 0.02 μM, 0.15 ± 0.01 μM, 0.11 ± 0.03 μM.

Cell Cycle Analysis

Cell Line: HeLa cells[1]
Concentration: 0.1, 0.2 and 0.4 μM
Incubation Time: 24 hours
Result: Increased cell distribution to the G2/M phase in a concentration-dependent way, arresting 24.7%, 47.6% and 71.7% of the cells in this phase at 0.1, 0.2 and 0.4 μM, respectively.

Apoptosis Analysis

Cell Line: HeLa cells[1]
Concentration: 0.1, 0.2 and 0.4 μM
Incubation Time: 24 hours
Result: Induced 35.9%, 66.4% and 84.4% of cell population undergoing apoptosis at 0.1 μM, 0.2 μM, 0.4 μM, respectively.

Cell Cytotoxicity Assay

Cell Line: HK-2 cells[1]
Concentration: 0-200 μM
Incubation Time: 24 hours
Result: Exhibited good renal safety profile, with IC50 of 188 ± 16 μM in HK-2 cells.

体内研究
(In Vivo)

Tubulin polymerization-IN-4 (100-1000 mg/kg; IP, single) exhibits extremely low toxicity with LD50 over 1000 mg/kg[1].
Tubulin polymerization-IN-4 (30 and 60 mg/kg; IP; daily for 21 days) inhibits the tumor growth, with TGI of 35% and 58% at dosing 30 and 60 mg/kg[1].
Tubulin polymerization-IN-4 (30 mg/kg; IP; single) presents the modest pharmacokinetic properties[1].
Pharmacokinetic Parameters of Tubulin polymerization-IN-4 in ICR mice[1].

IP (30 mg/kg)
T1/2 (h) 1.56 ± 0.28
Tmax (h) 0.25
Cmax (μg/L) 6215 ± 308
AUC0-t (μg/L·h) 5609 ± 347
AUC0-∞ (μg/L·h) 5940 ± 347
VZ/F (L/kg) 11.35 ± 1.29
CLZ/F (L/h/kg) 5.05 ± 0.91
MRT (h) 1.77 ± 0.43

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

400.86

Formula

C21H21ClN2O4
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]. Huo Z, Liu K, Zhang X, Liang Y, Sun X. Discovery of pyrimidine-bridged CA-4 CBSIs for the treatment of cervical cancer in combination with cisplatin with significantly reduced nephrotoxicity. Eur J Med Chem. 2022;235:114271.

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

Tubulin polymerization-IN-4

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。

Tubulin polymerization-IN-4 

Tubulin polymerization-IN-4 是一种有效的微管蛋白聚合体 (tubulin polymerization) 抑制剂，IC50 为 4.6 μM。Tubulin polymerization-IN-4 对HeLa细胞可破坏微管蛋白聚合和血管系统，将细胞周期阻滞在G2/M期，诱导细胞凋亡 (apoptosis)，抑制细胞的克隆发生和迁移。

Tubulin polymerization-IN-4

Tubulin polymerization-IN-4 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

Tubulin polymerization-IN-4 is a potent tubulin polymerization inhibitor with IC50 value of 4.6 μM. Tubulin polymerization-IN-4 can disrupt tubulin polymerization and vasculature, arrest the cell cycle at the G2/M phase, induce apoptosis, and suppress clonogenesis and migration in HeLa cells. Tubulin polymerization-IN-4 can be used for researching cervical cancer[1].

IC50 & Target

IC50: 4.6 μM (tubulin)[1]
体外研究
(In Vitro)

Tubulin polymerization-IN-4 (compound 9j) (0-1 μM; 48 hours) exhibits sub-micromolar inhibitory activities against HeLa, SiHa and MS751[1].
Tubulin polymerization-IN-4 (3, 6 and 12.5 μM; 0-20 min) inhibits tubulin polymerization in a concentration-dependent manner with the inhibition percentages of 39%, 54%, and 77% at 3, 6 and 12.5 μM[1].
Tubulin polymerization-IN-4 (1-100 μM; 2 hours) inhibits the formation of EBI-β-tubulin adduct in a concentration-dependent manner[1].
Tubulin polymerization-IN-4 (0.2 μM; 1 and 2 hours) disrupts the HUVEC-formed vascular tube[1].
Tubulin polymerization-IN-4 (0.1-0.4 μM; 24 hours) increases cell distribution to the G2/M phase in a concentration-dependent manner[1].
Tubulin polymerization-IN-4 (0.1-0.4 μM; 24 hours) induces apoptosis of HeLa cells[1].
Tubulin polymerization-IN-4 (20, 50, 100 nM; 14 days) reduces new colony formation and suppresses HeLa cell growth for 14 days in a dose-dependent manner[1].
Tubulin polymerization-IN-4 (0.1, 0.2 and 0.4 μM; 24 hours) effectively inhibits the migration of HeLa cells in a concentration-dependent manner[1].
Tubulin polymerization-IN-4 (0-200 μM; 24 hours) exhibits good renal safety profile, with IC50 of 188 ± 16 μM in HK-2 cells[1].

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

Cell Proliferation Assay

Cell Line: HeLa, SiHa and MS751[1]
Concentration: 0-1 μM
Incubation Time: 48 hours
Result: Exhibited sub-micromolar inhibitory activities against HeLa, SiHa and MS751 with IC50s of 0.09 ± 0.02 μM, 0.15 ± 0.01 μM, 0.11 ± 0.03 μM.

Cell Cycle Analysis

Cell Line: HeLa cells[1]
Concentration: 0.1, 0.2 and 0.4 μM
Incubation Time: 24 hours
Result: Increased cell distribution to the G2/M phase in a concentration-dependent way, arresting 24.7%, 47.6% and 71.7% of the cells in this phase at 0.1, 0.2 and 0.4 μM, respectively.

Apoptosis Analysis

Cell Line: HeLa cells[1]
Concentration: 0.1, 0.2 and 0.4 μM
Incubation Time: 24 hours
Result: Induced 35.9%, 66.4% and 84.4% of cell population undergoing apoptosis at 0.1 μM, 0.2 μM, 0.4 μM, respectively.

Cell Cytotoxicity Assay

Cell Line: HK-2 cells[1]
Concentration: 0-200 μM
Incubation Time: 24 hours
Result: Exhibited good renal safety profile, with IC50 of 188 ± 16 μM in HK-2 cells.

体内研究
(In Vivo)

Tubulin polymerization-IN-4 (100-1000 mg/kg; IP, single) exhibits extremely low toxicity with LD50 over 1000 mg/kg[1].
Tubulin polymerization-IN-4 (30 and 60 mg/kg; IP; daily for 21 days) inhibits the tumor growth, with TGI of 35% and 58% at dosing 30 and 60 mg/kg[1].
Tubulin polymerization-IN-4 (30 mg/kg; IP; single) presents the modest pharmacokinetic properties[1].
Pharmacokinetic Parameters of Tubulin polymerization-IN-4 in ICR mice[1].

IP (30 mg/kg)
T1/2 (h) 1.56 ± 0.28
Tmax (h) 0.25
Cmax (μg/L) 6215 ± 308
AUC0-t (μg/L·h) 5609 ± 347
AUC0-∞ (μg/L·h) 5940 ± 347
VZ/F (L/kg) 11.35 ± 1.29
CLZ/F (L/h/kg) 5.05 ± 0.91
MRT (h) 1.77 ± 0.43

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

400.86

Formula

C21H21ClN2O4
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]. Huo Z, Liu K, Zhang X, Liang Y, Sun X. Discovery of pyrimidine-bridged CA-4 CBSIs for the treatment of cervical cancer in combination with cisplatin with significantly reduced nephrotoxicity. Eur J Med Chem. 2022;235:114271.

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

Tubulin polymerization-IN-10

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。

Tubulin polymerization-IN-10 

Tubulin polymerization-IN-10 是一种有效的微管蛋白聚合抑制剂，其 IC50 为 4.25±0.75 μM。Tubulin polymerization-IN-10 具有抗肿瘤作用。

Tubulin polymerization-IN-10

Tubulin polymerization-IN-10 Chemical Structure

CAS No. : 2238784-19-3

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

Tubulin polymerization-IN-10 is a potent tubulin polymerization inhibitor with an IC50 of 4.25±0.75 μM. Tubulin polymerization-IN-10 has anti-tumor effects[1].

分子量

379.43

Formula

C18H21NO6S
CAS 号

2238784-19-3
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]. Huajian Zhu, et al. Design, synthesis and biological evaluation of vinyl selenone derivatives as novel microtubule polymerization inhibitors. Eur J Med Chem . 2020 Dec 1;207:112716.

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

Tubulin polymerization-IN-10

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。

Tubulin polymerization-IN-10 

Tubulin polymerization-IN-10 是一种有效的微管蛋白聚合抑制剂，其 IC50 为 4.25±0.75 μM。Tubulin polymerization-IN-10 具有抗肿瘤作用。

Tubulin polymerization-IN-10

Tubulin polymerization-IN-10 Chemical Structure

CAS No. : 2238784-19-3

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

Tubulin polymerization-IN-10 is a potent tubulin polymerization inhibitor with an IC50 of 4.25±0.75 μM. Tubulin polymerization-IN-10 has anti-tumor effects[1].

分子量

379.43

Formula

C18H21NO6S
CAS 号

2238784-19-3
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]. Huajian Zhu, et al. Design, synthesis and biological evaluation of vinyl selenone derivatives as novel microtubule polymerization inhibitors. Eur J Med Chem . 2020 Dec 1;207:112716.

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

Tubulin polymerization-IN-10

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。

Tubulin polymerization-IN-10 

Tubulin polymerization-IN-10 是一种有效的微管蛋白聚合抑制剂，其 IC50 为 4.25±0.75 μM。Tubulin polymerization-IN-10 具有抗肿瘤作用。

Tubulin polymerization-IN-10

Tubulin polymerization-IN-10 Chemical Structure

CAS No. : 2238784-19-3

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

Tubulin polymerization-IN-10 is a potent tubulin polymerization inhibitor with an IC50 of 4.25±0.75 μM. Tubulin polymerization-IN-10 has anti-tumor effects[1].

分子量

379.43

Formula

C18H21NO6S
CAS 号

2238784-19-3
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]. Huajian Zhu, et al. Design, synthesis and biological evaluation of vinyl selenone derivatives as novel microtubule polymerization inhibitors. Eur J Med Chem . 2020 Dec 1;207:112716.

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

Tubulin polymerization-IN-6

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。

Tubulin polymerization-IN-6 

Tubulin polymerization-IN-6 (化合物 5f) 是一种有效的微管蛋白聚合抑制剂，其IC50 为 1.09 μM。Tubulin polymerization-IN-6 抑制细胞迁移和管的形成，并有助于抗血管生成。Tubulin polymerization-IN-6 可显著抑制 HT29 移植 Balb/c 裸鼠肿瘤生长。

Tubulin polymerization-IN-6

Tubulin polymerization-IN-6 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

Tubulin polymerization-IN-6 (compound 5f) is a potent tubulin polymerization inhibitor, with an IC50 of 1.09 μM. Tubulin polymerization-IN-6 inhibits cell migration and tube formation and contributes to the anti-angiogenesis. Tubulin polymerization-IN-6 can greatly inhibit tumor growth on HT29 xenograft Balb/c nude mice[1].

IC50 & Target

IC50: 1.09 μM (Tubulin polymerization)[1]
体外研究
(In Vitro)

Tubulin polymerization-IN-6 (compound 5f) (0-20 μM, 24 h) shows a broad spectrum of anti-proliferation activity against cancer cell lines[1].
Tubulin polymerization-IN-6 (0-100 nM, 24 h) inhibits tumor cells colony formation, up-regulates the expression of Ac-α-tubulin and DeY-α-tubulin [1].
Tubulin polymerization-IN-6 (0-5 μM, 1 h) competes with colchicine and directly binds to the colchicine binding site, thus inhibit tubulin polymerization[1].
Tubulin polymerization-IN-6 (0-250 nM, 24 h) possesses a favorable anti-migration activity against cancer cells[1].
Tubulin polymerization-IN-6 (0-50 nM, 24 h) has the ability to inhibit the angiogenesis of HUVEC cells[1].
Tubulin polymerization-IN-6 (0-100 nM, 24 h) induces cell cycle arrest by regulating associated proteins, induces apoptosis by regulating associated proteins and down-regulating mitochondrial membrane potential, and dose-dependently promotes the production of ROS in HT29 cells[1].

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

Cell Proliferation Assay

Cell Line: HT29, MCF-7, HeLa, MDA-MB-231, A549[1]
Concentration: 0-20 μM
Incubation Time: 24 h
Result: Had a broad spectrum of anti-proliferation activity against cancer cell lines (MCF-7, MDA-MB-231, A549, Hela, and HT29), with IC50 values of 0.14 ± 0.03, 0.10 ± 0.00, 0.24 ± 0.03, 0.035 ± 0.002, and 0.023 ± 0.001 μM, respectively; and showed moderate anti-proliferative activity against drug resistant cancer cells (MCF-7/TxR and A549/TxR), with IC50 values of 0.18 ± 0.02 and 0.31 ± 0.08 μM, and DRI (drug-resistant index) of 1.3 and 1.2, respectively.

Western Blot Analysis

Cell Line: HT29 cells[1]
Concentration: 0, 25, 50, and 100 nM
Incubation Time: 24 h
Result: Up-regulated the expression of Ac-α-tubulin (acetyl-α-tubulin) and DeY-α-tubulin (detyrosinated-α-tubulin); regulated the expressions of the proteins involved in cell cycle such as cdc25c, cdk7, cyclin B1, and cdc2; down-regulated the level of Bim and up-regulated the levels of Bcl-2, p-Bcl-2, and Bax, decreased the expression of p-Histone H3(Ser10) and increased the expression of cleaved-Caspase-9, cleaved-Caspase-3, PARP, and cleaved-PARP.

Immunofluorescence

Cell Line: HT29 cells[1]
Concentration: 0, 25, 50, and 100 nM
Incubation Time: 6 h
Result: Dose-dependently depolymerized the tubulin polymers into oligomers, and caused the microtubule network to collapse in HT29 cells.

Cell Cycle Analysis

Cell Line: HT29 cells[1]
Concentration: 0, 12.5, 25, 50, and 100 nM
Incubation Time: 24 h
Result: Induced a dose dependent G2/M phase arrest, increased the proportion of G2/M phase cells from 20.9% to 87.5% at 100 nM.

Apoptosis Analysis

Cell Line: HT29 cells[1]
Concentration: 0, 25, 50, and 100 nM
Incubation Time: 24 h
Result: Induced apoptosis, increased the percentages of total apoptosis cells, down-regulated mitochondrial membrane potential.

体内研究
(In Vivo)

Tubulin polymerization-IN-6 (compound 5f) (HT29 xenograft Balb/c nude mice, 0-10 mg/kg, IP, once every two days, for three weeks) dose-dependently inhibits the tumor growth[1].
Tubulin polymerization-IN-6 (SD rats, 10 mg/kg, IV, once) shows the better pharmacokinetic properties[1]. Pharmacokinetic Parameters of Tubulin polymerization-IN-6 in SD rats[1].

Parameters 5f
t1/2 (h) 1.73
AUC (μg/L·h) 5.67
MRT (h) 1.92
CL (L/h/kg) 1.76
Tmax (h) 0.14
Cmax (ng/mL) 6.88

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

Animal Model: Immunodeficient Balb/c nude mice (HT29 xenograft, 5-week-old, 36 mice, six groups)[1]
Dosage: 0, 5, 7.5, 10 mg/kg
Administration: IP, once every two days, for three weeks
Result: Dose-dependently inhibited the tumor growth, inhibits the tumor weight growth by 75.5% at 10 mg/kg.
Animal Model: SD rats (5-week-old)[1]
Dosage: 10 mg/kg
Administration: IV, once (Pharmacokinetic Analysis)
Result: Showed the better pharmacokinetic properties, exhibited an eight-fold half-life and a two-fold AUC improvement.

分子量

375.37

Formula

C19H21NO7
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]. Yan XY, Leng JF, Chen TT, Zhao YJ, Kong LY, Yin Y. Design, synthesis, and biological evaluation of novel diphenylamine derivatives as tubulin polymerization inhibitors targeting the colchicine binding site. Eur J Med Chem. 2022;237:114372.

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Tubulin polymerization-IN-5

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。

Tubulin polymerization-IN-5 

Tubulin polymerization-IN-5 (化合物 20q) 是一种有效的具有潜在抗癌活性的微管蛋白抑制剂。Tubulin polymerization-IN-5 可以使 ESCC 细胞停滞在 G2/M 期，并导致细胞凋亡 (apoptosis)。

Tubulin polymerization-IN-5

Tubulin polymerization-IN-5 Chemical Structure

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生物活性

Tubulin polymerization-IN-5 (compound 20q) is a potent tubulin inhibitor with potential anticancer activities. Tubulin polymerization-IN-5 can arrest ESCC cells at G2/M phase and cause cells apoptosis[1].

IC50 & Target

Tubulin
体外研究
(In Vitro)

Tubulin polymerization-IN-5 (compound 20q) (0-100 nM, 48 h) exhibits potent antiproliferative activity against Kyse30, Kyse450, MGC-803, and HCT-116 cells[1].
Tubulin polymerization-IN-5 (0-60 nM, 7 d) obviously inhibits the cellular colony formation ability of the Kyse30 and Kyse450 cells[1].
Tubulin polymerization-IN-5 (0-100 nM, 48 h) inhibits microtubule assembly and disrupts cytoskeleton[1].
Tubulin polymerization-IN-5 (0-300 nM, 24 h) causes a significant weakening of the β-tubulin adduct band in Kyse30 and Kyse450 cells, competitively bind the colchicine binding site of β-tubulin[1].
Tubulin polymerization-IN-5 (0-100 nM, 48 h) effectively arrests cells at the G2/M phase, and induces cell apoptosis in Kyse30 and Kyse450 cells by regulating the expression of related proteins[1].
Tubulin polymerization-IN-5 (0-100 nM, 48 h) induces cell mitochondrial apoptosis in ESCC cells, leads to a significant depolarization of mitochondria membrane potential in Kyse30 and Kyse450 cells[1].

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

Cell Proliferation Assay

Cell Line: Kyse30, Kyse450, MGC-803, and HCT-116 cells[1]
Concentration: 0, 80, 100 nM
Incubation Time: 48 h
Result: Exhibited potent antiproliferative activity against Kyse30, Kyse450, MGC-803, and HCT-116 cells, with IC50 values of 0.069, 0.078, 0.084, and 0.227 μM, respectively.

Cell Cycle Analysis

Cell Line: Kyse30 and Kyse450 cells[1]
Concentration: 0, 80, 100 nM
Incubation Time: 48 h
Result: Effectively arrested 2 ESCC cells at the G2/M phase, significantly increased of percentages of cells at the G2/M phase from 19.38 to 76.9767 in Kyse30 cells, and 7.04333 to 80.8933 in Kyse450 cells.

Apoptosis Analysis

Cell Line: Kyse30 and Kyse450 cells[1]
Concentration: 0, 80, 100 nM
Incubation Time: 48 h
Result: Dose-dependently induced cell apoptosis in Kyse30 and Kyse450 cells, significantly increased the percentages of total apoptotic cells from 8.1667% (0 nM) to 23.8% (80 nM, Kyse30 cells), 34.0333% (80 nM, Kyse450 cells), 38.633% (100 nM, Kyse30 cells), and 57.3667% (100 nM, Kyse450 cells), respectively.

Western Blot Analysis

Cell Line: Kyse30 and Kyse450 cells[1]
Concentration: 0, 80, 100 nM
Incubation Time: 48 h
Result: Dose-dependently down-regulated the expression of the G2 phase related proteins CDK1, CDC25c and p-Wee 1, up-regulated the level of the M phase marker protein p-Histone H3; up-regulated the activity of the executors of apoptosis caspase-3, up-regulated the pro-apoptotic proteins Bax and Noxa, and down-regulated the anti-apoptotic protein Bcl-2, decreased the levels of IAP (Inhibitor of Apoptosis Proteins) family protein XIAP.

分子量

621.77

Formula

C29H39N3O8S2
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]. Sun YX, et al. Design, synthesis and evaluation of novel bis-substituted aromatic amide dithiocarbamate derivatives as colchicine site tubulin polymerization inhibitors with potent anticancer activities. Eur J Med Chem. 2022;229:114069.

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Tubulin polymerization-IN-3

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。

Tubulin polymerization-IN-3 

Tubulin polymerization-IN-3 (化合物 4c) 是一种有效的微管蛋白聚合抑制剂，IC50 值为 3.84 µM。Tubulin polymerization-IN-3 可诱导结肠癌细胞凋亡。

Tubulin polymerization-IN-3

Tubulin polymerization-IN-3 Chemical Structure

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

Tubulin polymerization-IN-3 (compound 4c) is a potent tubulin polymerization inhibitor, with an IC50 of 3.84 µM. Tubulin polymerization-IN-3 can induce apoptosis in colon cancer cells[1].

分子量

413.86

Formula

C20H20ClN5O3
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]. Mohamed HS, et, al. Design, synthesis, biological assessment, and in-Silico studies of 1,2,4-triazolo[1,5-a]pyrimidine derivatives as tubulin polymerization inhibitors. Bioorg Chem. 2022 Apr;121:105687.

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