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BAP1-IN-1 (Compound 8) 是一种 BRCA1 相关蛋白 1 (BAP1) 催化活性抑制剂,其 IC50 为 0.1-1 μM。

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BAP1-IN-1 Chemical Structure

BAP1-IN-1 Chemical Structure

CAS No. : 353495-21-3

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规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ¥407
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5 mg ¥370
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10 mg ¥590
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Customer Review

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

BAP1-IN-1 (Compound 8) is a BRCA1 associated protein 1 (BAP1) catalytic activity inhibitor with an IC50 of 0.1-1 μM[1].

IC50 & Target

IC50: 0.1-1 μM (BAP1)[1]

体外研究
(In Vitro)

BAP1-IN-1 (Compound 8) (1 μM; 30 min) specifically inhibits BAP1 not just in vitro but also within the cellular context[1].
BAP1-IN-1 (0.1 μM; 24 h) significantly alters 240 genes in BAP1-WT cells, whereas only 33 transcripts are changed in BAP1-KO cells, demonstrating that the gene expression changes mainly depend on the presence of BAP1 protein[1].
BAP1-IN-1 (0-10 μM; 72 h) selectively inhibits cells with ASXL1 GOF mutations[1].

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

Western Blot Analysis[1]

Cell Line: CAL51 cells
Concentration: 1 μM
Incubation Time: 30 min
Result: Remarkably inhibited BAP1 catalytic activity.

Cell Viability Assay[1]

Cell Line: THP1, MOML13, K562, THP1-ASXL1-WT and THP1-ASXL1-Y591fs cells
Concentration: 0, 0.1, 0.3, 1, 3 and 10 μM
Incubation Time: 72 h
Result: K562 cells (ASXL1-Y591*) were significantly more sensitive to the treatment. Cells with ASXL1fs mutations were ten times more sensitive to the treatment.
体内研究
(In Vivo)

BAP1-IN-1 (Compound 8) (50 mg/kg/d; i.p.; 4 weeks) delays the progression of ASXL1-mutant leukemia and improves survival in mice[1].

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

Animal Model: NSGS mice, K562 (ASXL1-WT/Y591*) xenograft model and patient-derived tumor cells (ASXL1-WT/Q588*) model[1]
Dosage: 50 mg/kg/d
Administration: Intraperitoneal injection, drug treatments were started at day 28 after transplantation
Result: Significantly delayed progression of disease in both models.
分子量

292.33

Formula

C18H16N2O2

CAS 号
性状

固体

颜色

Light yellow to yellow

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

溶解性数据
细胞实验: 

DMSO 中的溶解度 : 50 mg/mL (171.04 mM; 超声助溶; 吸湿的 DMSO 对产品的溶解度有显著影响,请使用新开封的 DMSO)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 3.4208 mL 17.1040 mL 34.2079 mL
5 mM 0.6842 mL 3.4208 mL 6.8416 mL
查看完整储备液配制表

* 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 (protect from light)。-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。

  • 摩尔计算器

  • 稀释计算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量
=
浓度
×
体积
×
分子量 *

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

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start)

C1

×
体积 (start)

V1

=
浓度 (final)

C2

×
体积 (final)

V2

动物溶解方案计算器
请输入动物实验的基本信息:

给药剂量

mg/kg

动物的平均体重

g

每只动物的给药体积

μL

动物数量

由于实验过程有损耗,建议您多配一只动物的量
计算结果
工作液所需浓度 : mg/mL
纯度 & 产品资料

纯度: 99.52%

参考文献

完整储备液配制表

* 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 (protect from light)。-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。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 3.4208 mL 17.1040 mL 34.2079 mL 85.5198 mL
5 mM 0.6842 mL 3.4208 mL 6.8416 mL 17.1040 mL
10 mM 0.3421 mL 1.7104 mL 3.4208 mL 8.5520 mL
15 mM 0.2281 mL 1.1403 mL 2.2805 mL 5.7013 mL
20 mM 0.1710 mL 0.8552 mL 1.7104 mL 4.2760 mL
25 mM 0.1368 mL 0.6842 mL 1.3683 mL 3.4208 mL
30 mM 0.1140 mL 0.5701 mL 1.1403 mL 2.8507 mL
40 mM 0.0855 mL 0.4276 mL 0.8552 mL 2.1380 mL
50 mM 0.0684 mL 0.3421 mL 0.6842 mL 1.7104 mL
60 mM 0.0570 mL 0.2851 mL 0.5701 mL 1.4253 mL
80 mM 0.0428 mL 0.2138 mL 0.4276 mL 1.0690 mL
100 mM 0.0342 mL 0.1710 mL 0.3421 mL 0.8552 mL
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.

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产品名称:
BAP1-IN-1
目录号:
HY-W327122
需求量: