2OH-BNPP1
Based on 3 publication(s) in Google Scholar
2OH-BNPP1 is an inhibitor of BUB1 kinase, a Ser/Thr kinase, used for the treatment of cancer.
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- Reinheit: 99.65%
- CAS. Nr.: 833481-73-5
- Formel: C16H19N5O
- Molecular Weight:297.35
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Speicherung:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Biologische Aktivität
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Chemical Information
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Lösungsmittel & Löslichkeit
- Protokoll
- Reinheit & Dokumentation
- Verweise
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) 2OH-BNPP1
More
Biologische Aktivität
BUB1 kinase[1]
2OH-BNPP1 (0.1-50 μM) abrogates TGFβ signaling in a dose dependent manner. 2OH-BNPP1 dose-dependently impairs the TGFβ-induced phosphorylation of proteins that mediate canonical and non-canonical TGFβ signaling in multiple cancer cell lines and normal cell lines[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS. Nr. 833481-73-5
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Appearance Solid
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Molecular Weight 297.35
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Formel C16H19N5O
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Color White to off-white
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SMILES
OC1=CC=CC=C1CC2=NN(C(C)(C)C)C3=NC=NC(N)=C32
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (3)
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Journal Impact Factor
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Most Recent
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Life Sci
BUB1 potentiates gastric cancer proliferation and metastasis by activating TRAF6/NF-κB/FGF18 through m6A modification. [Abstract]2024 Jul 16:122916. PMID: 39025206 -
J Virol
2018 Aug 29;92(18):e00254-18. PMID: 29976667 -
Thorac Cancer
Budding uninhibited by benzimidazoles 1 overexpression is associated with poor prognosis and malignant phenotype: A promising therapeutic target for lung adenocarcinoma. [Abstract]2023 Apr;14(10):893-912. PMID: 36825773
Lösungsmittel & Löslichkeit
DMSO : 100 mg/mL (336.30 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
For the following dissolution methods, please prepare the working solution directly:
It is recommended to prepare fresh solutions and use them promptly within a short period of time.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 50% PEG300 50% Saline
Solubility: 10 mg/mL (33.63 mM); Suspended solution; Need ultrasonic
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Protokoll
In vitro kinase assays are performed using 200 ng of protein (BUB1-WT, or a kinase inactive mutant BUB1-KD), and 2 µg of substrate (TGFBRI-WT, TGFBRI-KD, SMAD3 or H2A) in 1X kinase buffer (50 mM Tris-HCl, 150 mM NaCl, 10 mM MgCl2, 1% (v/v) Glycerol, 0.1% (v/v) Triton X 100, DTT, PMSF, Na3VO4 (1 mM each), 2 mM NaF and β-glycerol phosphate) in 20 µL volume containing 10 µCi 32p-ATP and 300 µM cold ATP. Reactions are run at 30ºC for 0.5-1 hour and quenched using Laemmli buffer and resolved using a 4-12% Bis-Tris gel. Quantitative autoradiography is performed using a Typhoon FLA 9000 scanner.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Cell line-derived xenografts are established by implanting 2.5×106 A549 cells subcutaneously into each flank of 4-6 week old male SCID mice. When tumors reach a volume between 40 to 60 mm3, mice are injected with a single intraperetoneal dose of SB431542 (10 mg/kg body weight), a dose previously reported to inhibit TGFβ signaling in mouse models, or 2OH-BNPP1 (50 mg/kg), or vehicle (DMSO). Tumors are excised 4 hours after treatment and fixed in formalin. Paraffin-embedded sections are stained using an antibody for phosphorylated SMAD2, and micrographs are taken with an Olympus microscope fitted with an Olympus DP-70 high resolution digital camera. The proportion of nuclei that stains positive for phosphorylated SMAD2 are counted in three random fields per tumor per treatment condition [vehicle (n=4), SB431542 (n=2), and 2OH-BNPP1 (n=5)]. A two -ided Student's t-test is performed to assess statistical significance. Slides are adjusted for brightness and contrast with Adobe Photoshop CS2, but the micrographs undergo no further manipulations.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Reinheit & Dokumentation
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Data Sheet (284 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Handling Instructions (2659 KB)
Verweise
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 3.3630 mL | 16.8152 mL | 33.6304 mL | 84.0760 mL |
| 5 mM | 0.6726 mL | 3.3630 mL | 6.7261 mL | 16.8152 mL | |
| 10 mM | 0.3363 mL | 1.6815 mL | 3.3630 mL | 8.4076 mL | |
| 15 mM | 0.2242 mL | 1.1210 mL | 2.2420 mL | 5.6051 mL | |
| 20 mM | 0.1682 mL | 0.8408 mL | 1.6815 mL | 4.2038 mL | |
| 25 mM | 0.1345 mL | 0.6726 mL | 1.3452 mL | 3.3630 mL | |
| 30 mM | 0.1121 mL | 0.5605 mL | 1.1210 mL | 2.8025 mL | |
| 40 mM | 0.0841 mL | 0.4204 mL | 0.8408 mL | 2.1019 mL | |
| 50 mM | 0.0673 mL | 0.3363 mL | 0.6726 mL | 1.6815 mL | |
| 60 mM | 0.0561 mL | 0.2803 mL | 0.5605 mL | 1.4013 mL | |
| 80 mM | 0.0420 mL | 0.2102 mL | 0.4204 mL | 1.0510 mL | |
| 100 mM | 0.0336 mL | 0.1682 mL | 0.3363 mL | 0.8408 mL |
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