Thailanstatin D

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。

Thailanstatin D 

Thailanstatin D 是 Thailanstatin A 的类似物,通过干扰 U2AF65 和 SAP155 之间的相互作用,阻止它们与位于分支点和 3′ 剪接位点之间的多嘧啶束结合,能够抑制 AR-V7 基因剪接。Thailanstatin D 对人 CRPC 异种移植瘤具有明显的抑瘤作用,可导致细胞凋亡 (apoptosis)。

Thailanstatin D

Thailanstatin D Chemical Structure

CAS No. : 1609105-89-6

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

Thailanstatin D, an analogue of Thailanstatin A, is able to inhibit AR-V7 gene splicing by interfering the interaction between U2AF65 and SAP155 and preventing them from binding to polypyrimidine tract located between the branch point and the 3′ splice site. Thailanstatin D exhibits a potent tumor inhibitory effect on human CRPC xenografts leading to cell apoptosis[1].

体外研究
(In Vitro)

Thailanstatin D (0-50 nM; 4 hours) significantly decreases the protein levels of AR-V7 and other AR-Vs (AR splice variants)[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: VCaP, 22RV1 and LN95 cells
Concentration: 0-50 nM
Incubation Time: 4 hours
Result: The mRNA levels of both AR-V7 and AR-FL were suppressed by Thailanstatin D in a dose-dependent manner.

体内研究
(In Vivo)

Thailanstatin D (300 µg/kg; ALZET osmotic pumps; daily for 4 days) significantly inhibits the tumor growth[1].

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

Animal Model: NOD-SCID mice ( Mice bearing 22RV1 xenografts)[1]
Dosage: 300 µg/kg
Administration: ALZET osmotic pumps; daily for 4 days
Result: Significantly inhibited the tumor growth.

分子量

519.63

Formula

C28H41NO8

CAS 号

1609105-89-6

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]. Wang B, et al. Developing new targeting strategy for androgen receptor variants in castration resistant prostate cancer. Int J Cancer. 2017;141(10):2121-2130.

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

Thailanstatin D

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。

Thailanstatin D 

Thailanstatin D 是 Thailanstatin A 的类似物,通过干扰 U2AF65 和 SAP155 之间的相互作用,阻止它们与位于分支点和 3′ 剪接位点之间的多嘧啶束结合,能够抑制 AR-V7 基因剪接。Thailanstatin D 对人 CRPC 异种移植瘤具有明显的抑瘤作用,可导致细胞凋亡 (apoptosis)。

Thailanstatin D

Thailanstatin D Chemical Structure

CAS No. : 1609105-89-6

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

Thailanstatin D, an analogue of Thailanstatin A, is able to inhibit AR-V7 gene splicing by interfering the interaction between U2AF65 and SAP155 and preventing them from binding to polypyrimidine tract located between the branch point and the 3′ splice site. Thailanstatin D exhibits a potent tumor inhibitory effect on human CRPC xenografts leading to cell apoptosis[1].

体外研究
(In Vitro)

Thailanstatin D (0-50 nM; 4 hours) significantly decreases the protein levels of AR-V7 and other AR-Vs (AR splice variants)[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: VCaP, 22RV1 and LN95 cells
Concentration: 0-50 nM
Incubation Time: 4 hours
Result: The mRNA levels of both AR-V7 and AR-FL were suppressed by Thailanstatin D in a dose-dependent manner.

体内研究
(In Vivo)

Thailanstatin D (300 µg/kg; ALZET osmotic pumps; daily for 4 days) significantly inhibits the tumor growth[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: NOD-SCID mice ( Mice bearing 22RV1 xenografts)[1]
Dosage: 300 µg/kg
Administration: ALZET osmotic pumps; daily for 4 days
Result: Significantly inhibited the tumor growth.

分子量

519.63

Formula

C28H41NO8

CAS 号

1609105-89-6

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]. Wang B, et al. Developing new targeting strategy for androgen receptor variants in castration resistant prostate cancer. Int J Cancer. 2017;141(10):2121-2130.

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

Thailanstatin D

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。

Thailanstatin D 

Thailanstatin D 是 Thailanstatin A 的类似物,通过干扰 U2AF65 和 SAP155 之间的相互作用,阻止它们与位于分支点和 3′ 剪接位点之间的多嘧啶束结合,能够抑制 AR-V7 基因剪接。Thailanstatin D 对人 CRPC 异种移植瘤具有明显的抑瘤作用,可导致细胞凋亡 (apoptosis)。

Thailanstatin D

Thailanstatin D Chemical Structure

CAS No. : 1609105-89-6

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

Thailanstatin D, an analogue of Thailanstatin A, is able to inhibit AR-V7 gene splicing by interfering the interaction between U2AF65 and SAP155 and preventing them from binding to polypyrimidine tract located between the branch point and the 3′ splice site. Thailanstatin D exhibits a potent tumor inhibitory effect on human CRPC xenografts leading to cell apoptosis[1].

体外研究
(In Vitro)

Thailanstatin D (0-50 nM; 4 hours) significantly decreases the protein levels of AR-V7 and other AR-Vs (AR splice variants)[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: VCaP, 22RV1 and LN95 cells
Concentration: 0-50 nM
Incubation Time: 4 hours
Result: The mRNA levels of both AR-V7 and AR-FL were suppressed by Thailanstatin D in a dose-dependent manner.

体内研究
(In Vivo)

Thailanstatin D (300 µg/kg; ALZET osmotic pumps; daily for 4 days) significantly inhibits the tumor growth[1].

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

Animal Model: NOD-SCID mice ( Mice bearing 22RV1 xenografts)[1]
Dosage: 300 µg/kg
Administration: ALZET osmotic pumps; daily for 4 days
Result: Significantly inhibited the tumor growth.

分子量

519.63

Formula

C28H41NO8

CAS 号

1609105-89-6

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]. Wang B, et al. Developing new targeting strategy for androgen receptor variants in castration resistant prostate cancer. Int J Cancer. 2017;141(10):2121-2130.

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

Madrasin(Synonyms: DDD00107587)

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。

Madrasin (Synonyms: DDD00107587) 纯度: 99.90%

Madrasin (DDD00107587) 是一种剪接抑制剂,可在体外阻止剪接中间体和产物的形成,并干扰剪接体组装途径中的一个或多个早期步骤。Madrasin 还能在体外抑制 pre-mRNA 的剪接,并修饰细胞中内源性 pre-mRNA 的剪接。

Madrasin(Synonyms: DDD00107587)

Madrasin Chemical Structure

CAS No. : 374913-63-0

规格 价格 是否有货 数量
5 mg ¥660 In-stock
10 mg ¥990 In-stock
25 mg ¥1980 In-stock
50 mg ¥3300 In-stock
100 mg ¥5500 In-stock
200 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

Madrasin 相关产品

相关化合物库:

  • Bioactive Compound Library Plus
  • Anti-Cancer Compound Library

生物活性

Madrasin (DDD00107587) is a splicing inhibitor that prevents formation of both splicing intermediates and products in vitro and interferes with one or more early steps in the pathway of spliceosome assembly. Madrasin also can inhibit pre-mRNA splicing in vitro and modify splicing of endogenous pre-mRNA in cells[1].

IC50 & Target

pre-mRNA splicing[1]

体外研究
(In Vitro)

Madrasin (10-30 μM; 4-24 hours; HeLa cells) treatment inhibits the splicing of each of the RIOK3, BRD2, and Hsp40, MCL1, CCNA2, AURKA and p27 pre-mRNAs in both HeLa and HEK293 cells[1].
Madrasin (10-30 μM; 4-24 hours; HeLa and HEK293 cells) treatment shows a dose- and time-dependent inhibitory effect on cell cycle progression[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.

RT-PCR[1]

Cell Line: HeLa cells
Concentration: 10 μM, 20 μM, or 30 μM
Incubation Time: 4 hours, 8 hours, or 24 hours
Result: Increased in inhibition of pre-mRNA splicing.

Cell Cycle Analysis[1]

Cell Line: HeLa and HEK293 cells
Concentration: 10 μM, 20 μM, or 30 μM
Incubation Time: 4 hours, 8 hours, or 24 hours
Result: In the presence of 10 μM 8 hours after treatment, the proportion of cells in G2, M, and S phases increased, with a concomitant decrease in the number of G1 phase cells. This effect increased over time, with >40% of cells in G2 and M phase and >50% in S phase 24 hours.

分子量

311.34

Formula

C16H17N5O2

CAS 号

374913-63-0

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 : 2 mg/mL (6.42 mM; Need ultrasonic)

H2O : < 0.1 mg/mL (insoluble)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 3.2119 mL 16.0596 mL 32.1192 mL
5 mM 0.6424 mL 3.2119 mL 6.4238 mL
10 mM

*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month。-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。

参考文献
  • [1]. Andrea Pawellek et al. Identification of Small Molecule Inhibitors of Pre-mRNA Splicing. J Biol Chem, 2014 Dec 12, 289(50): 34683-34698.

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