1. Epigenetics PROTAC Apoptosis
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  3. A947

A947 是一种有效的选择性 SMARCA2 蛋白水解靶向嵌合分子 (PROTAC)。A947 也是一种有效且具有中等选择性的 SMARCA2 降解剂。A947 对 SMARCA2 溴结构域具有结合亲和力,Kd 值为 93 nM。A947 可用于癌症研究。

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A947 Chemical Structure

A947 Chemical Structure

CAS No. : 2378056-80-3

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

A947 is a potent and selective SMARCA2 proteolysis-targeting chimera molecule (PROTAC). A947 also is a potent and moderately selective SMARCA2 degrader. A947 has binding affinity to the SMARCA2 bromodomain with a Kd value of 93 nM. A947 can be used for the research of cancer[1].

IC50 & Target

Kd: 93 nM (SMARCA2), 65 nM (SMARCA4); DC50 for SMARCA2: 39 pM (in SW1573 cells)[1].

体外研究
(In Vitro)

A947 has binding affinity to the SMARCA2 and SMARCA4 bromodomains with Kd values of 93 nM and 65 nM, respectively[1].
A947 can potently degrade SMARCA2 in SW1573 cells with a DC50 value of 39 pM[1].
A947 (100 nM, 500 nM) mediates ubiquitination and degradation of SMARCA2/4[1].
A947 (0-500 nM) can inhibit growth of SMARCA4-mutant NSCLC cells[1].

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

Western Blot Analysis[1]

Cell Line: SW1573 cells
Concentration: 0-10 nM
Incubation Time: 18 h
Result: Degraded SMARCA2 with amaximal degradation of 96% in 10 nM.

Cell Viability Assay[1]

Cell Line: NCI-H1944 cells
Concentration: 0-500 nM
Incubation Time: 7 days
Result: Showed the dose-dependent inhibition of growth.

Cell Cycle Analysis[1]

Cell Line: HCC2302, NCI-H1793, RERF-LC-AI, NCI-H1944, Calu-6, NCI-H460, A427 cells
Concentration: 0-500 nM
Incubation Time: 48 h
Result: Showed G1 arrest in SMARCA4mut models.

Apoptosis Analysis[1]

Cell Line: NCI-H1944, NCI-H838 cells
Concentration: 100 nM
Incubation Time: 50 h
Result: Induced cells toward apoptotic cell death.
体内研究
(In Vivo)

A947 (i.v.; 40 mg/kg; single-dose, 2 week or every other week, 30 days) has active in SMARCA4-mutant NSCLC xenograft models in vivo[1].

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

Animal Model: SMARCA4-mutant NSCLC xenograft models
Dosage: 40mg/kg
Administration: Intravenous , single-dose, 2 week; Intravenous , every other week, 30 days
Result: Rapidly reduced the tumor SMARCA2 protein levels and significant decreased the tumor growth.
分子量

1121.40

Formula

C61H76N12O7S

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
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  • 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.

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A947
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HY-148381
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