2. PROTAC Cell Cycle/DNA Damage
  3. PROTACs CDK
  4. BSJ-5-63

BSJ-5-63 是一种有效的 CDK12、CDK7、CDK9 PROTAC 降解剂。BSJ-5-63 降低 CDK12、CDK7、CDK9、RNAPII、Cyclin K 的蛋白表达。BSJ-5-63 降低 BRCA1、BRCA2 的 mRNA 表达。BSJ-5-63 具有抗癌活性，具有用于前列腺癌研究的潜力 (粉色：靶蛋白配体 (HY-150948)；黑色：连接子 (HY-W140827)；蓝色：E3 连接酶配体 (HY-112078))。。

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BSJ-5-63 Chemical Structure

BSJ-5-63 Chemical Structure

CAS No. : 2519823-37-9

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BSJ-5-63 相关抗体

Top Publications Citing Use of Products

查看 PROTACs 亚型特异性产品:

查看所有亚型
von Hippel-Lindau (VHL) Cereblon MDM2 cIAP1

查看 CDK 亚型特异性产品:

查看所有亚型
CDK1 CDK2 CDK3 CDK4 CDK5 CDK6 CDK7 CDK8 CDK9 CDK11 CDK12 CDK13 CDK14 CDK16 CDK19 CDC CLK Pho85

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

BSJ-5-63 is a potent CDK12, CDK7, CDK9 PROTAC degrader. BSJ-5-63 BSJ-5-63 decreases the protein expression of CDK12, CDK7, CDK9, RNAPII, Cyclin K. BSJ-5-63 decreases the mRNA expression of BRCA1, BRCA2. BSJ-5-63 shows anticancer activity and has the potential for the research of prostate cancer (Pink: ligand for target protein (HY-150948); black: linker (HY-W140827); Blue: E3 ligase ligand (HY-112078))[1].

IC50 & Target[1]

CDK12

 

CDK7

 

CDK9

 

体外研究
(In Vitro)

BSJ-5-63 (0-1000 nM; 8 h) 以剂量依赖性方式降低 CDK12、CDK7、CDK9、RNAPII、Cyclin K 的蛋白质表达[1]。
BSJ-5-63 (0-1000 nM; 8, 16, 24 h) 以剂量和时间依赖性方式降低 BRCA1、BRCA2 的 mRNA 表达[1]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

BSJ-5-63 相关抗体:

Western Blot Analysis[1]

Cell Line: LNCaP, C4-2B, 22Rv1 cells
Concentration: 62.5, 125, 250, 500, 1000 nM
Incubation Time: 8 h
Result: Decreased the protein expression of CDK12, CDK7, CDK9, P-RNAPII Ser2, P-RNAPII Ser5, P-RNAPII Ser7, RNAPII, Cyclin K in a dose-dependent manner.

RT-PCR[1]

Cell Line: LNCaP, C4-2B, 22Rv1 cells
Concentration: 62.5, 125, 250, 500, 1000 nM
Incubation Time: 8, 16, 24 h
Result: Decreased the mRNA expression of BRCA1, BRCA2 in a dose and time dependent manner.
体内研究
(In Vivo)

BSJ-5-63 (50 mg/kg; i.p.; daily for 12 days) 在小鼠中显示出抗癌活性[1]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: 4-5 weeks, Male ICR-SCID mice (22Rv1 cells)[1]
Dosage: 50 mg/kg
Administration: I.p.; daily for 12 days
Result: Significantly inhibited the growth of 22Rv1 tumors and tumor weight was significantly reduced and increased in the number of apoptotic cells, daily administration resulted in approximately 10% weight loss in mice.
分子量

1020.78

Formula

C52H74ClN9O6S2
CAS 号
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.
纯度 & 产品资料
参考文献

BSJ-5-63 相关分类

  • 摩尔计算器

  • 稀释计算器

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

BSJ-5-632519823-37-9PROTACsCDKCyclin dependent kinaseRNAPIICyclin Kanticancerprostate cancerLNCaPC4-2B22Rv1 cellsInhibitorinhibitorinhibit

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目录号：
HY-162706
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