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| 1mg |
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| 5mg |
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| 10mg |
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| Other Sizes |
| Targets |
BSc5367 targets the NIMA-related protein kinase Nek1 (also known as NimA related kinase 1) [17L7]. Nek1 is a serine/threonine kinase that plays a crucial role in cell cycle progression, particularly in the G2/M phase, and in the DNA damage response where it promotes DNA repair and cell survival [5L6-L8]. It is also involved in ciliary formation and function, linking it to polycystic kidney disease (PKD) [5L22-L23]. BSc5367 binds to the kinase domain of Nek1, inhibiting its ATP binding and/or catalytic activity.
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| ln Vitro |
In vitro, BSc5367 is a potent inhibitor of the Nek1 kinase domain, with an IC₅0 of 11.5 nM [17L6-L7]. Its activity is typically assessed using biochemical kinase assays. While its primary role is as a Nek1 inhibitor, some reports also suggest it may have activity against other targets, such as the transcription factor STAT3, but its primary and most potent activity is against Nek1 [5L10-L12].
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| ln Vivo |
BSc5367 is a research tool, and detailed in vivo activity data are not extensively reported in standard product literature. However, since Nek1 dysfunction is implicated in radiation-resistant cancers, BSc5367 could be used in xenograft mouse models to study if Nek1 inhibition can sensitize tumors to radiotherapy. It can also be used in a model of polycystic kidney disease (PKD) to assess its effect on cyst formation and renal function. Specific animal protocols are typically established by individual research groups.
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| Enzyme Assay |
The binding of BSc5367 to the Nek1 kinase is assessed using non-cellular biochemical kinase assays. A typical protocol involves incubating purified recombinant human Nek1 kinase with various concentrations of BSc5367 in the presence of ATP and a specific peptide substrate (e.g., myelin basic protein or a custom peptide). The reaction is allowed to proceed, and the incorporation of phosphate into the substrate is measured. This can be quantified using a radioactivity-based assay (32P-ATP) or a more modern luminescence-based ADP detection kit (e.g., ADP-Glo). The IC₅0 value is calculated from a dose-response curve.
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| Cell Assay |
Cellular assays for BSc5367 utilize cancer cell lines that are known to express functional Nek1 or are dependent on Nek1 for growth and survival. Cells are treated with various concentrations of BSc5367 for 24-72 hours. The primary endpoint is cell viability, measured by MTT, CCK-8, or CellTiter-Glo assays to generate a growth inhibition curve. To confirm the mechanism of action, cells are often treated with DNA damaging agents (e.g., ionizing radiation or cisplatin) in the presence or absence of BSc5367, followed by Western blot analysis for markers of DNA repair (e.g., gammaH2AX, p53) or cell cycle arrest (e.g., cyclin B1). Since Nek1 is involved in DNA repair, BSc5367 is expected to sensitize cells to DNA-damaging chemotherapy.
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| Animal Protocol |
A typical in vivo protocol for BSc5367 involves a xenograft mouse model of cancer, such as a radiation-resistant cancer. Mice are inoculated subcutaneously with cancer cells. Once tumors reach a suitable size, BSc5367 is administered intraperitoneally (IP) at a dose like 10-50 mg/kg daily, either alone or in combination with local tumor radiation therapy. The primary endpoint is tumor growth inhibition (TGI), measured by calipers. Secondary endpoints include survival (Kaplan-Meier curve), tumor tissue analysis for Nek1 activity (e.g., biomarker expression by IHC), and body weight for safety monitoring.
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| ADME/Pharmacokinetics |
Pharmacokinetic properties for BSc5367 are not detailed in standard product literature. As a small molecule, it likely has drug-like properties and is typically prepared in formulations containing DMSO or other solvents for in vivo administration. For research use, standard assays to determine bioavailability and half-life would be required.
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| Toxicity/Toxicokinetics |
Comprehensive toxicological data for BSc5367 are not provided in standard product literature. As a research-use compound, standard safety assessments for acute toxicity, genotoxicity, and organ-specific toxicity are not typically described. For laboratory use, standard chemical safety precautions for handling enzyme inhibitors should be followed.
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| References | |
| Additional Infomation |
BSc5367 (CAS: 3029584-84-4) has a molecular formula of C20H1₅N3O2 and a molecular weight of 329.35 g/mol [5L33-L34]. It is a potent Nek1 inhibitor (IC₅0=11.5 nM) and is used in studies on cell cycle regulation, DNA repair, and microtubule regulation [5L15-L17]. The compound should be stored as a powder at -20degC, away from moisture.
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| Molecular Formula |
C20H15N3O2
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| Molecular Weight |
329.35
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| CAS # |
3029584-84-4
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| Appearance |
White to yellow solid powder
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO :~10 mg/mL (~30.36 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 1 mg/mL (3.04 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 10.0 mg/mL clear DMSO stock solution to 400 μL of PEG300 and mix evenly; then add 50 μL of Tween-80 to the above solution and mix evenly; then add 450 μL of normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: 1 mg/mL (3.04 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 10.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 1 mg/mL (3.04 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.0363 mL | 15.1814 mL | 30.3628 mL | |
| 5 mM | 0.6073 mL | 3.0363 mL | 6.0726 mL | |
| 10 mM | 0.3036 mL | 1.5181 mL | 3.0363 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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