BAP1-IN-1
Based on 1 publication(s) in Google Scholar
BAP1-IN-1 (Compound 8) is a BRCA1 associated protein 1 (BAP1) catalytic activity inhibitor with an IC50 of 0.1-1 μM.
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- 純度 : 99.86%
- CAS 番号: 353495-21-3
- 分子式: C18H16N2O2
- 分子量:292.33
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保管条件:
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
MedChemExpress(MCE)の使用を引用している文献 BAP1-IN-1
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生物活性
製品説明
IC50 & Target
IC50: 0.1-1 μM (BAP1)[1]
体外実験
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:CAL51 cells
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Concentration:1 μM
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Incubation Time:30 min
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Result:Remarkably inhibited BAP1 catalytic activity.
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Cell Line:THP1, MOML13, K562, THP1-ASXL1-WT and THP1-ASXL1-Y591fs cells
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Concentration:0, 0.1, 0.3, 1, 3 and 10 μM
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Incubation Time:72 h
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Result:K562 cells (ASXL1-Y591*) were significantly more sensitive to the treatment. Cells with ASXL1fs mutations were ten times more sensitive to the treatment.
体内実験
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:NSGS mice, K562 (ASXL1-WT/Y591*) xenograft model and patient-derived tumor cells (ASXL1-WT/Q588*) model[1]
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Dosage:50 mg/kg/d
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Administration:Intraperitoneal injection, drug treatments were started at day 28 after transplantation
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Result:Significantly delayed progression of disease in both models.
化学情報
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CAS 番号 353495-21-3
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性状 Solid
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分子量 292.33
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分子式 C18H16N2O2
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Color Light yellow to yellow
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SMILES
O=[N+](C1=CC2=C(NC(C3=CC=CC=C3)C4C2C=CC4)C=C1)[O-]
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
Publications (1)
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Journal Impact Factor
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Most Recent
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FASEB J
Regulator of Calcineurin 1 Aggravates Tubular Epithelial Cell Injury in Diabetic Mice Through Promoting Liver Kinase B1 Ubiquitination. [Abstract]2026 Mar 31;40(6):e71712. PMID: 41854627
溶剤 & 溶解度
体外:
DMSO : 50 mg/mL (171.04 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
純度とドキュメンテーション
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データシート (275 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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取扱説明書 (2659 KB)
参考文献
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 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 |