MS21

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。

MS21 

MS21 是一种新型的 AKT 降解物,通过选择性地抑制 PI3K/PTEN 途径突变癌症的生长。

MS21

MS21 Chemical Structure

CAS No. : 2376137-05-0

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

MS21, a novel degrader of AKT, selectively inhibits the growth of PI3K/PTEN pathway-mutant cancers with wild-type KRAS and BRAF.

分子量

1107.84

Formula

C58H79ClN12O6S

CAS 号

2376137-05-0

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]. Xu J, et al. AKT Degradation Selectively Inhibits the Growth of PI3K/PTEN Pathway-Mutant Cancers with Wild-Type KRAS and BRAF by Destabilizing Aurora Kinase B. Cancer Discov. 2021 Jul 23.

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

MS83

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。

MS83 

MS83 是一种通过将 KEAP1 配体连接到 BRD4/3/2 配体的 PROTAC 分子。

MS83

MS83 Chemical Structure

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

MS83 is a proof-of-concept PROTAC by linking the KEAP1 ligand to a BRD4/3/2 binder.

分子量

1047.64

Formula

C52H55ClN10O8S2

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]. Wei J, et al. Harnessing the E3 Ligase KEAP1 for Targeted Protein Degradation. J Am Chem Soc. 2021 Sep 22;143(37):15073-15083.

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

MS21

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。

MS21 

MS21 是一种新型的 AKT 降解物,通过选择性地抑制 PI3K/PTEN 途径突变癌症的生长。

MS21

MS21 Chemical Structure

CAS No. : 2376137-05-0

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

MS21, a novel degrader of AKT, selectively inhibits the growth of PI3K/PTEN pathway-mutant cancers with wild-type KRAS and BRAF.

分子量

1107.84

Formula

C58H79ClN12O6S

CAS 号

2376137-05-0

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]. Xu J, et al. AKT Degradation Selectively Inhibits the Growth of PI3K/PTEN Pathway-Mutant Cancers with Wild-Type KRAS and BRAF by Destabilizing Aurora Kinase B. Cancer Discov. 2021 Jul 23.

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

MS83

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。

MS83 

MS83 是一种通过将 KEAP1 配体连接到 BRD4/3/2 配体的 PROTAC 分子。

MS83

MS83 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

MS83 is a proof-of-concept PROTAC by linking the KEAP1 ligand to a BRD4/3/2 binder.

分子量

1047.64

Formula

C52H55ClN10O8S2

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]. Wei J, et al. Harnessing the E3 Ligase KEAP1 for Targeted Protein Degradation. J Am Chem Soc. 2021 Sep 22;143(37):15073-15083.

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

MS21

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。

MS21 

MS21 是一种新型的 AKT 降解物,通过选择性地抑制 PI3K/PTEN 途径突变癌症的生长。

MS21

MS21 Chemical Structure

CAS No. : 2376137-05-0

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

MS21, a novel degrader of AKT, selectively inhibits the growth of PI3K/PTEN pathway-mutant cancers with wild-type KRAS and BRAF.

分子量

1107.84

Formula

C58H79ClN12O6S

CAS 号

2376137-05-0

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]. Xu J, et al. AKT Degradation Selectively Inhibits the Growth of PI3K/PTEN Pathway-Mutant Cancers with Wild-Type KRAS and BRAF by Destabilizing Aurora Kinase B. Cancer Discov. 2021 Jul 23.

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

MS83

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。

MS83 

MS83 是一种通过将 KEAP1 配体连接到 BRD4/3/2 配体的 PROTAC 分子。

MS83

MS83 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

MS83 is a proof-of-concept PROTAC by linking the KEAP1 ligand to a BRD4/3/2 binder.

分子量

1047.64

Formula

C52H55ClN10O8S2

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]. Wei J, et al. Harnessing the E3 Ligase KEAP1 for Targeted Protein Degradation. J Am Chem Soc. 2021 Sep 22;143(37):15073-15083.

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

MS-PPOH

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。

MS-PPOH 

MS-PPOH 是一种有效的选择性细胞色素 P450 (CYP) 环氧化酶抑制剂。MS-PPOH 抑制 CYP2C8CYP2C9IC50 分别为 15 和 11 µM。

MS-PPOH

MS-PPOH Chemical Structure

CAS No. : 206052-02-0

规格 是否有货
5 mg 询价
10 mg 询价

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生物活性

MS-PPOH is a potent and selective cytochrome P450 (CYP) epoxygenase inhibitor[1]. MS-PPOH inhibits CYP2C8 and CYP2C9 with IC50s of 15 and 11 µM, respectively[2].

体外研究
(In Vitro)

MS-PPOH blocks cellular EET synthesis. MS-PPOH inhibits tonic (basal) cell invasion and migration and reduces the 11,12-EET (1.0 μM)-induced cell motility[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: PC-3 cells
Concentration: 2.0 and 10.0 μM
Incubation Time: 24 hours
Result: Inhibited tonic (basal) cell invasion and migration.

体内研究
(In Vivo)

MS-PPOH (20 mg/kg/day, i.v.) for 6 days significantly reduced renal levels of epoxyeicosatrienoic acids (EETs) in Dahl salt-resistant rats on 2% NaCl drinking solution[3].

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

Animal Model: Six-week-old male stroke-prone spontaneously hypertensive rats (SHRSP)[3]
Dosage: 20 mg/kg/day
Administration: Intravenously
Result: Treatment had negligible effects on systolic blood pressure (SBP) in saline-drinking SHRSP after 1 week, 160 vs. 167 mmHg, or 2 weeks of treatment, 171 vs. 175 mmHg, for vehicle vs. MS-PPOH, respectively.

分子量

323.41

Formula

C16H21NO4S

CAS 号

206052-02-0

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]. Kasem Nithipatikom, et al. Inhibition of carcinoma cell motility by epoxyeicosatrienoic acid (EET) antagonists. Cancer Sci. 2010 Dec;101(12):2629-36.

    [2]. Jun Yang, et al. Cytochrome P450 2C24: Expression, Tissue Distribution, High-Throughput Assay, and Pharmacological Inhibition. Acta Pharm Sin B. 2012 Apr;2(2):137-145.

    [3]. Jing Li, et al. Pharmacological manipulation of arachidonic acid-epoxygenase results in divergent effects on renal damage. Front Pharmacol. 2014 Aug 15;5:187.

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

MS-PPOH

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。

MS-PPOH 

MS-PPOH 是一种有效的选择性细胞色素 P450 (CYP) 环氧化酶抑制剂。MS-PPOH 抑制 CYP2C8CYP2C9IC50 分别为 15 和 11 µM。

MS-PPOH

MS-PPOH Chemical Structure

CAS No. : 206052-02-0

规格 是否有货
5 mg 询价
10 mg 询价

* Please select Quantity before adding items.

生物活性

MS-PPOH is a potent and selective cytochrome P450 (CYP) epoxygenase inhibitor[1]. MS-PPOH inhibits CYP2C8 and CYP2C9 with IC50s of 15 and 11 µM, respectively[2].

体外研究
(In Vitro)

MS-PPOH blocks cellular EET synthesis. MS-PPOH inhibits tonic (basal) cell invasion and migration and reduces the 11,12-EET (1.0 μM)-induced cell motility[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: PC-3 cells
Concentration: 2.0 and 10.0 μM
Incubation Time: 24 hours
Result: Inhibited tonic (basal) cell invasion and migration.

体内研究
(In Vivo)

MS-PPOH (20 mg/kg/day, i.v.) for 6 days significantly reduced renal levels of epoxyeicosatrienoic acids (EETs) in Dahl salt-resistant rats on 2% NaCl drinking solution[3].

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

Animal Model: Six-week-old male stroke-prone spontaneously hypertensive rats (SHRSP)[3]
Dosage: 20 mg/kg/day
Administration: Intravenously
Result: Treatment had negligible effects on systolic blood pressure (SBP) in saline-drinking SHRSP after 1 week, 160 vs. 167 mmHg, or 2 weeks of treatment, 171 vs. 175 mmHg, for vehicle vs. MS-PPOH, respectively.

分子量

323.41

Formula

C16H21NO4S

CAS 号

206052-02-0

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]. Kasem Nithipatikom, et al. Inhibition of carcinoma cell motility by epoxyeicosatrienoic acid (EET) antagonists. Cancer Sci. 2010 Dec;101(12):2629-36.

    [2]. Jun Yang, et al. Cytochrome P450 2C24: Expression, Tissue Distribution, High-Throughput Assay, and Pharmacological Inhibition. Acta Pharm Sin B. 2012 Apr;2(2):137-145.

    [3]. Jing Li, et al. Pharmacological manipulation of arachidonic acid-epoxygenase results in divergent effects on renal damage. Front Pharmacol. 2014 Aug 15;5:187.

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

MS-PPOH

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。

MS-PPOH 

MS-PPOH 是一种有效的选择性细胞色素 P450 (CYP) 环氧化酶抑制剂。MS-PPOH 抑制 CYP2C8CYP2C9IC50 分别为 15 和 11 µM。

MS-PPOH

MS-PPOH Chemical Structure

CAS No. : 206052-02-0

规格 是否有货
5 mg 询价
10 mg 询价

* Please select Quantity before adding items.

生物活性

MS-PPOH is a potent and selective cytochrome P450 (CYP) epoxygenase inhibitor[1]. MS-PPOH inhibits CYP2C8 and CYP2C9 with IC50s of 15 and 11 µM, respectively[2].

体外研究
(In Vitro)

MS-PPOH blocks cellular EET synthesis. MS-PPOH inhibits tonic (basal) cell invasion and migration and reduces the 11,12-EET (1.0 μM)-induced cell motility[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 Viability Assay[1]

Cell Line: PC-3 cells
Concentration: 2.0 and 10.0 μM
Incubation Time: 24 hours
Result: Inhibited tonic (basal) cell invasion and migration.

体内研究
(In Vivo)

MS-PPOH (20 mg/kg/day, i.v.) for 6 days significantly reduced renal levels of epoxyeicosatrienoic acids (EETs) in Dahl salt-resistant rats on 2% NaCl drinking solution[3].

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: Six-week-old male stroke-prone spontaneously hypertensive rats (SHRSP)[3]
Dosage: 20 mg/kg/day
Administration: Intravenously
Result: Treatment had negligible effects on systolic blood pressure (SBP) in saline-drinking SHRSP after 1 week, 160 vs. 167 mmHg, or 2 weeks of treatment, 171 vs. 175 mmHg, for vehicle vs. MS-PPOH, respectively.

分子量

323.41

Formula

C16H21NO4S

CAS 号

206052-02-0

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]. Kasem Nithipatikom, et al. Inhibition of carcinoma cell motility by epoxyeicosatrienoic acid (EET) antagonists. Cancer Sci. 2010 Dec;101(12):2629-36.

    [2]. Jun Yang, et al. Cytochrome P450 2C24: Expression, Tissue Distribution, High-Throughput Assay, and Pharmacological Inhibition. Acta Pharm Sin B. 2012 Apr;2(2):137-145.

    [3]. Jing Li, et al. Pharmacological manipulation of arachidonic acid-epoxygenase results in divergent effects on renal damage. Front Pharmacol. 2014 Aug 15;5:187.

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

Folate-MS432

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。

Folate-MS432 

Folate-MS432 是一种 PROTAC,能够在癌细胞中以叶酸受体依赖的方式降解 MEKs

Folate-MS432

Folate-MS432 Chemical Structure

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

Folate-MS432, a PROTAC, is capable of degrading MEKs in a folate receptor-dependent manner in cancer cells.

分子量

1693.67

Formula

C78H96F3IN18O12S

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]. Liu J, et al. Cancer Selective Target Degradation by Folate-Caged PROTACs. J Am Chem Soc. 2021 May 19;143(19):7380-7387.

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

Folate-MS432

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。

Folate-MS432 

Folate-MS432 是一种 PROTAC,能够在癌细胞中以叶酸受体依赖的方式降解 MEKs

Folate-MS432

Folate-MS432 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

Folate-MS432, a PROTAC, is capable of degrading MEKs in a folate receptor-dependent manner in cancer cells.

分子量

1693.67

Formula

C78H96F3IN18O12S

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]. Liu J, et al. Cancer Selective Target Degradation by Folate-Caged PROTACs. J Am Chem Soc. 2021 May 19;143(19):7380-7387.

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

MS33

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。

MS33 

MS33 是一种有效的 WDR5 降解剂,对 VCBWDR5Kd 值分别为 870 nM 和 120 nM。MS33 以 E3 连接酶 VHL 和蛋白酶体依赖性方式诱导 WDR5 降解。MS33 可用于急性髓系白血病的研究。

MS33

MS33 Chemical Structure

CAS No. : 2407449-11-8

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

MS33 is a potent WDR5 degrader, with Kds of 870 nM and 120 nM for VCB and WDR5, respectively. MS33 induces WDR5 degradation in an E3 ligase VHL, and proteasome-dependent manner. MS33 can be used for the research of acute myeloid leukemia[1][2][3].

IC50 & Target[1]

VHL

 

WDR5

120 nM (Kd)

VCB

870 nM (Kd)

体外研究
(In Vitro)

MS33 (0.05-5 μM; 18 h) induces WDR5 degradation in a concentration-dependent manner in MV4;11 cells[1].

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

Western Blot Analysis[1]

Cell Line: MV4;11 cells
Concentration: 0.05, 0.1, 0.5, 1, 5 μM
Incubation Time: 1, 2, 4, 8, 16, 24 hours
Result: Concentration- and time-dependently induced WDR5 degradation.
The DC50 of MS33 was 260 nM, and the maximum degradation of 71%.

分子量

1208.48

Formula

C64H84F3N11O7S

CAS 号

2407449-11-8

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]. Yu X, et, al. A selective WDR5 degrader inhibits acute myeloid leukemia in patient-derived mouse models. Sci Transl Med. 2021 Sep 29;13(613):eabj1578.

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

MS33

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。

MS33 

MS33 是一种有效的 WDR5 降解剂,对 VCBWDR5Kd 值分别为 870 nM 和 120 nM。MS33 以 E3 连接酶 VHL 和蛋白酶体依赖性方式诱导 WDR5 降解。MS33 可用于急性髓系白血病的研究。

MS33

MS33 Chemical Structure

CAS No. : 2407449-11-8

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

MS33 is a potent WDR5 degrader, with Kds of 870 nM and 120 nM for VCB and WDR5, respectively. MS33 induces WDR5 degradation in an E3 ligase VHL, and proteasome-dependent manner. MS33 can be used for the research of acute myeloid leukemia[1][2][3].

IC50 & Target[1]

VHL

 

WDR5

120 nM (Kd)

VCB

870 nM (Kd)

体外研究
(In Vitro)

MS33 (0.05-5 μM; 18 h) induces WDR5 degradation in a concentration-dependent manner in MV4;11 cells[1].

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

Western Blot Analysis[1]

Cell Line: MV4;11 cells
Concentration: 0.05, 0.1, 0.5, 1, 5 μM
Incubation Time: 1, 2, 4, 8, 16, 24 hours
Result: Concentration- and time-dependently induced WDR5 degradation.
The DC50 of MS33 was 260 nM, and the maximum degradation of 71%.

分子量

1208.48

Formula

C64H84F3N11O7S

CAS 号

2407449-11-8

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]. Yu X, et, al. A selective WDR5 degrader inhibits acute myeloid leukemia in patient-derived mouse models. Sci Transl Med. 2021 Sep 29;13(613):eabj1578.

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

Folate-MS432

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。

Folate-MS432 

Folate-MS432 是一种 PROTAC,能够在癌细胞中以叶酸受体依赖的方式降解 MEKs

Folate-MS432

Folate-MS432 Chemical Structure

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

Folate-MS432, a PROTAC, is capable of degrading MEKs in a folate receptor-dependent manner in cancer cells.

分子量

1693.67

Formula

C78H96F3IN18O12S

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]. Liu J, et al. Cancer Selective Target Degradation by Folate-Caged PROTACs. J Am Chem Soc. 2021 May 19;143(19):7380-7387.

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

MS33

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。

MS33 

MS33 是一种有效的 WDR5 降解剂,对 VCBWDR5Kd 值分别为 870 nM 和 120 nM。MS33 以 E3 连接酶 VHL 和蛋白酶体依赖性方式诱导 WDR5 降解。MS33 可用于急性髓系白血病的研究。

MS33

MS33 Chemical Structure

CAS No. : 2407449-11-8

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

MS33 is a potent WDR5 degrader, with Kds of 870 nM and 120 nM for VCB and WDR5, respectively. MS33 induces WDR5 degradation in an E3 ligase VHL, and proteasome-dependent manner. MS33 can be used for the research of acute myeloid leukemia[1][2][3].

IC50 & Target[1]

VHL

 

WDR5

120 nM (Kd)

VCB

870 nM (Kd)

体外研究
(In Vitro)

MS33 (0.05-5 μM; 18 h) induces WDR5 degradation in a concentration-dependent manner in MV4;11 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: MV4;11 cells
Concentration: 0.05, 0.1, 0.5, 1, 5 μM
Incubation Time: 1, 2, 4, 8, 16, 24 hours
Result: Concentration- and time-dependently induced WDR5 degradation.
The DC50 of MS33 was 260 nM, and the maximum degradation of 71%.

分子量

1208.48

Formula

C64H84F3N11O7S

CAS 号

2407449-11-8

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]. Yu X, et, al. A selective WDR5 degrader inhibits acute myeloid leukemia in patient-derived mouse models. Sci Transl Med. 2021 Sep 29;13(613):eabj1578.

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

MS37452

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。

MS37452  纯度: 99.22%

MS37452 是一种有效的 CBX7 chromodomain 与 H3K27me3 结合的抑制剂,Kd 为 27.7 μM。MS37452 可以通过置换 CBX7 与前列腺癌细胞中 INK4A/ARF 基因座的结合来抑制多梳抑制复合物靶基因 p16/CDKN2A 的转录。

MS37452

MS37452 Chemical Structure

CAS No. : 423748-02-1

规格 价格 是否有货 数量
5 mg ¥1500 In-stock
10 mg ¥2400 In-stock
25 mg ¥4800 In-stock
50 mg ¥7650 In-stock
100 mg ¥12200 In-stock
200 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

MS37452 相关产品

相关化合物库:

  • Bioactive Compound Library Plus
  • Epigenetics Compound Library
  • Histone Modification Research Compound Library
  • Anti-Cancer Compound Library
  • Reprogramming Compound Library
  • Anti-Blood Cancer Compound Library

生物活性

MS37452 is a potent inhibitor of CBX7 chromodomain binding to H3K27me3, with a Kd of 27.7 μM. MS37452 can derepress transcription of polycomb repressive complex target gene p16/CDKN2A by displacing CBX7 binding to the INK4A/ARF locus in prostate cancer cells[1].

IC50 & Target

CBX7[1]

体外研究
(In Vitro)

MS37452 (125-500 μM; 12 hours) significantly increases INK4A/ARF transcript levels up to 25% and 60% for 250 μM and 500 μM, respectively, as compared to the DMSO control[1].
MS37452 (250 μM; 2 hours) treats human PC3 prostate cancer cells for 2 hours reducing CBX7 occupancy across the INK4A/ARF locus[1].
MS37452 (200 µM; 5 days) combined with doxorubicin results in consistently decreased cell viability compared to DMSO treated and single drug treatment[2].
MS37452 (200 µM; 5 days), which is a CBX7 chromodomain inhibitor (CBX7i), in combination with doxorubicin is a novel therapeutic strategy[2].

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

RT-PCR[1]

Cell Line: PC3 cells
Concentration: 125-500 μM
Incubation Time: 12 hours
Result: Up-regulated INK4A/ARF expression up to 25% and 60% for 250 μM and 500 μM, respectively.

Cell Viability Assay[2]

Cell Line: Glioblastoma multiforme (GBM) U118MG cells
Concentration: PRT4165 40 µM, PTC209 200 nM, DZnep 25 µM, GSK343 400 nM, MS37452 200 µM, Doxorubicin 200 nM, temozolomide 50 µM, SAHA 1 µM
Incubation Time: 5 days
Result: Identified several combinations that resulted in consistently decreased cell viability compared to DMSO treated and single drug treatment: SAHA/TMZ and MS37452/doxorubicin.

分子量

398.45

Formula

C22H26N2O5

CAS 号

423748-02-1

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO : 100 mg/mL (250.97 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.5097 mL 12.5486 mL 25.0972 mL
5 mM 0.5019 mL 2.5097 mL 5.0195 mL
10 mM 0.2510 mL 1.2549 mL 2.5097 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: ≥ 2.5 mg/mL (6.27 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (6.27 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 25.0 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: ≥ 2.5 mg/mL (6.27 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (6.27 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 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
*以上所有助溶剂都可在 Shanghai Jinpan Biotech Co Ltd 网站选购。
参考文献
  • [1]. Ren C, et al. Small-molecule modulators of methyl-lysine binding for the CBX7 chromodomain. Chem Biol. 2015;22(2):161-168.

    [2]. Connelly KE, et al. CBX Chromodomain Inhibition Enhances Chemotherapy Response in Glioblastoma Multiforme. Yale J Biol Med. 2016;89(4):431-440.

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

MS37452

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。

MS37452  纯度: 99.22%

MS37452 是一种有效的 CBX7 chromodomain 与 H3K27me3 结合的抑制剂,Kd 为 27.7 μM。MS37452 可以通过置换 CBX7 与前列腺癌细胞中 INK4A/ARF 基因座的结合来抑制多梳抑制复合物靶基因 p16/CDKN2A 的转录。

MS37452

MS37452 Chemical Structure

CAS No. : 423748-02-1

规格 价格 是否有货 数量
5 mg ¥1500 In-stock
10 mg ¥2400 In-stock
25 mg ¥4800 In-stock
50 mg ¥7650 In-stock
100 mg ¥12200 In-stock
200 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

MS37452 相关产品

相关化合物库:

  • Bioactive Compound Library Plus
  • Epigenetics Compound Library
  • Histone Modification Research Compound Library
  • Anti-Cancer Compound Library
  • Reprogramming Compound Library
  • Anti-Blood Cancer Compound Library

生物活性

MS37452 is a potent inhibitor of CBX7 chromodomain binding to H3K27me3, with a Kd of 27.7 μM. MS37452 can derepress transcription of polycomb repressive complex target gene p16/CDKN2A by displacing CBX7 binding to the INK4A/ARF locus in prostate cancer cells[1].

IC50 & Target

CBX7[1]

体外研究
(In Vitro)

MS37452 (125-500 μM; 12 hours) significantly increases INK4A/ARF transcript levels up to 25% and 60% for 250 μM and 500 μM, respectively, as compared to the DMSO control[1].
MS37452 (250 μM; 2 hours) treats human PC3 prostate cancer cells for 2 hours reducing CBX7 occupancy across the INK4A/ARF locus[1].
MS37452 (200 µM; 5 days) combined with doxorubicin results in consistently decreased cell viability compared to DMSO treated and single drug treatment[2].
MS37452 (200 µM; 5 days), which is a CBX7 chromodomain inhibitor (CBX7i), in combination with doxorubicin is a novel therapeutic strategy[2].

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

RT-PCR[1]

Cell Line: PC3 cells
Concentration: 125-500 μM
Incubation Time: 12 hours
Result: Up-regulated INK4A/ARF expression up to 25% and 60% for 250 μM and 500 μM, respectively.

Cell Viability Assay[2]

Cell Line: Glioblastoma multiforme (GBM) U118MG cells
Concentration: PRT4165 40 µM, PTC209 200 nM, DZnep 25 µM, GSK343 400 nM, MS37452 200 µM, Doxorubicin 200 nM, temozolomide 50 µM, SAHA 1 µM
Incubation Time: 5 days
Result: Identified several combinations that resulted in consistently decreased cell viability compared to DMSO treated and single drug treatment: SAHA/TMZ and MS37452/doxorubicin.

分子量

398.45

Formula

C22H26N2O5

CAS 号

423748-02-1

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO : 100 mg/mL (250.97 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.5097 mL 12.5486 mL 25.0972 mL
5 mM 0.5019 mL 2.5097 mL 5.0195 mL
10 mM 0.2510 mL 1.2549 mL 2.5097 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: ≥ 2.5 mg/mL (6.27 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (6.27 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 25.0 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: ≥ 2.5 mg/mL (6.27 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (6.27 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 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
*以上所有助溶剂都可在 Shanghai Jinpan Biotech Co Ltd 网站选购。
参考文献
  • [1]. Ren C, et al. Small-molecule modulators of methyl-lysine binding for the CBX7 chromodomain. Chem Biol. 2015;22(2):161-168.

    [2]. Connelly KE, et al. CBX Chromodomain Inhibition Enhances Chemotherapy Response in Glioblastoma Multiforme. Yale J Biol Med. 2016;89(4):431-440.

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

MS37452

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。

MS37452  纯度: 99.22%

MS37452 是一种有效的 CBX7 chromodomain 与 H3K27me3 结合的抑制剂,Kd 为 27.7 μM。MS37452 可以通过置换 CBX7 与前列腺癌细胞中 INK4A/ARF 基因座的结合来抑制多梳抑制复合物靶基因 p16/CDKN2A 的转录。

MS37452

MS37452 Chemical Structure

CAS No. : 423748-02-1

规格 价格 是否有货 数量
5 mg ¥1500 In-stock
10 mg ¥2400 In-stock
25 mg ¥4800 In-stock
50 mg ¥7650 In-stock
100 mg ¥12200 In-stock
200 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

MS37452 相关产品

相关化合物库:

  • Bioactive Compound Library Plus
  • Epigenetics Compound Library
  • Histone Modification Research Compound Library
  • Anti-Cancer Compound Library
  • Reprogramming Compound Library
  • Anti-Blood Cancer Compound Library

生物活性

MS37452 is a potent inhibitor of CBX7 chromodomain binding to H3K27me3, with a Kd of 27.7 μM. MS37452 can derepress transcription of polycomb repressive complex target gene p16/CDKN2A by displacing CBX7 binding to the INK4A/ARF locus in prostate cancer cells[1].

IC50 & Target

CBX7[1]

体外研究
(In Vitro)

MS37452 (125-500 μM; 12 hours) significantly increases INK4A/ARF transcript levels up to 25% and 60% for 250 μM and 500 μM, respectively, as compared to the DMSO control[1].
MS37452 (250 μM; 2 hours) treats human PC3 prostate cancer cells for 2 hours reducing CBX7 occupancy across the INK4A/ARF locus[1].
MS37452 (200 µM; 5 days) combined with doxorubicin results in consistently decreased cell viability compared to DMSO treated and single drug treatment[2].
MS37452 (200 µM; 5 days), which is a CBX7 chromodomain inhibitor (CBX7i), in combination with doxorubicin is a novel therapeutic strategy[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.

RT-PCR[1]

Cell Line: PC3 cells
Concentration: 125-500 μM
Incubation Time: 12 hours
Result: Up-regulated INK4A/ARF expression up to 25% and 60% for 250 μM and 500 μM, respectively.

Cell Viability Assay[2]

Cell Line: Glioblastoma multiforme (GBM) U118MG cells
Concentration: PRT4165 40 µM, PTC209 200 nM, DZnep 25 µM, GSK343 400 nM, MS37452 200 µM, Doxorubicin 200 nM, temozolomide 50 µM, SAHA 1 µM
Incubation Time: 5 days
Result: Identified several combinations that resulted in consistently decreased cell viability compared to DMSO treated and single drug treatment: SAHA/TMZ and MS37452/doxorubicin.

分子量

398.45

Formula

C22H26N2O5

CAS 号

423748-02-1

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO : 100 mg/mL (250.97 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.5097 mL 12.5486 mL 25.0972 mL
5 mM 0.5019 mL 2.5097 mL 5.0195 mL
10 mM 0.2510 mL 1.2549 mL 2.5097 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: ≥ 2.5 mg/mL (6.27 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (6.27 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 25.0 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: ≥ 2.5 mg/mL (6.27 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (6.27 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 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
*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]. Ren C, et al. Small-molecule modulators of methyl-lysine binding for the CBX7 chromodomain. Chem Biol. 2015;22(2):161-168.

    [2]. Connelly KE, et al. CBX Chromodomain Inhibition Enhances Chemotherapy Response in Glioblastoma Multiforme. Yale J Biol Med. 2016;89(4):431-440.

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

MS-PEG4-t-butyl ester

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。

MS-PEG4-t-butyl ester 

MS-PEG4-t-butyl ester 是一种 PROTAC linker,属于 PEG 类。可用于合成 PROTAC 分子。

MS-PEG4-t-butyl ester

MS-PEG4-t-butyl ester Chemical Structure

CAS No. : 1024602-74-1

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

MS-PEG4-t-butyl ester is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].

IC50 & Target

PEGs

 

体外研究
(In Vitro)

PROTACs contain two different ligands connected by a linker; one is a ligand for an E3 ubiquitin ligase and the other is for the target protein. PROTACs exploit the intracellular ubiquitin-proteasome system to selectively degrade target proteins[1].

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

分子量

356.43

Formula

C14H28O8S

CAS 号

1024602-74-1

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]. An S, et al. Small-molecule PROTACs: An emerging and promising approach for the development of targeted therapy drugs. EBioMedicine. 2018 Oct;36:553-562

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

MS-PEG4-t-butyl ester

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。

MS-PEG4-t-butyl ester 

MS-PEG4-t-butyl ester 是一种 PROTAC linker,属于 PEG 类。可用于合成 PROTAC 分子。

MS-PEG4-t-butyl ester

MS-PEG4-t-butyl ester Chemical Structure

CAS No. : 1024602-74-1

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

MS-PEG4-t-butyl ester is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].

IC50 & Target

PEGs

 

体外研究
(In Vitro)

PROTACs contain two different ligands connected by a linker; one is a ligand for an E3 ubiquitin ligase and the other is for the target protein. PROTACs exploit the intracellular ubiquitin-proteasome system to selectively degrade target proteins[1].

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

分子量

356.43

Formula

C14H28O8S

CAS 号

1024602-74-1

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]. An S, et al. Small-molecule PROTACs: An emerging and promising approach for the development of targeted therapy drugs. EBioMedicine. 2018 Oct;36:553-562

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