BAP1-IN-1
目录号 : GC68724BAP1-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。
Cas No.:353495-21-3
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >99.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
IC50: 0.1-1 μM (BAP1)[1]
BAP1-IN-1 (Compound 8) is a BRCA1 associated protein 1 (BAP1) catalytic activity inhibitor with an IC50 of 0.1-1 μM[1].
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].
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. |
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].
| 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. |
[1]. Wang L, et al. Epigenetic targeted therapy of stabilized BAP1 in ASXL1 gain-of-function mutated leukemia. Nat Cancer. 2021 May;2(5):515-526.
| Cas No. | 353495-21-3 | SDF | Download SDF |
| 分子式 | C18H16N2O2 | 分子量 | 292.33 |
| 溶解度 | DMSO : 50 mg/mL (171.04 mM; Need ultrasonic) | 储存条件 | 4°C, protect from light |
| General tips | 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 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 3.4208 mL | 17.104 mL | 34.2079 mL |
| 5 mM | 0.6842 mL | 3.4208 mL | 6.8416 mL |
| 10 mM | 0.3421 mL | 1.7104 mL | 3.4208 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。