| Size | Price | Stock | Qty |
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| 5mg |
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| Targets |
SJ-000063181 targets the bone morphogenetic protein (BMP) signaling pathway. BMPs are members of the transforming growth factor-beta (TGF-beta) superfamily that regulate a wide range of biological processes including embryonic development, cell proliferation, differentiation, and bone formation. SJ-000063181 acts as an activator of BMP signaling, promoting the activation of BMP receptors and subsequent phosphorylation of downstream SMAD transcription factors (SMAD1, SMAD5, SMAD8), thereby regulating target gene expression.
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| ln Vitro |
In vitro, SJ-000063181 potently activates BMP signaling with an EC50 ≤ 1 microM. It induces the phosphorylation of SMAD1/5/8, the downstream effector proteins of BMP receptor activation. This activation leads to the transcriptional upregulation of BMP target genes involved in osteoblast differentiation and embryonic patterning. The compound is used as a chemical probe to study BMP signaling in various cell lines, including C2C12 myoblasts and MC3T3-E1 osteoblasts, to investigate bone formation and developmental processes.
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| ln Vivo |
In vivo, SJ-000063181 has demonstrated the ability to penetrate zebrafish embryos, making it a useful tool for studying BMP signaling during embryonic development. In zebrafish models, the compound can modulate BMP-dependent developmental processes such as dorsoventral patterning, fin formation, and skeletal development. These studies help elucidate the temporal and spatial requirements of BMP signaling in vertebrate embryogenesis. The compound has not yet been extensively studied in mammalian in vivo models.
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| Enzyme Assay |
For non-cell-based binding or activity assays, standard protocols for BMP signaling activation are not cell-free assays, as BMP signaling requires cellular membrane receptors. However, an in vitro kinase activity assay using recombinant BMP receptors (BMPR1A or BMPR1B) and purified SMAD1 protein can be performed. SJ-000063181 is incubated with the kinase, ATP, and SMAD1 substrate. Phosphorylated SMAD1 is detected using a phospho-specific antibody in an ELISA or western blot format. The EC50 is calculated from the dose-response curve.
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| Cell Assay |
For in vitro cell-based assays, C2C12 myoblast cells are seeded in 24-well plates and cultured to 70-80% confluency. Cells are serum-starved overnight and then treated with varying concentrations of SJ-000063181 (e.g., 0.1-10 microM) for 1-4 hours. Cells are lysed, and protein lysates are analyzed by western blotting using antibodies against phosphorylated SMAD1/5/8 (p-SMAD1/5/8) and total SMAD1 as a loading control. The EC50 for p-SMAD1/5/8 induction is calculated from densitometry analysis.
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| Animal Protocol |
For in vivo studies in zebrafish embryos, fertilized zebrafish embryos are collected and staged. At the 1-2 cell stage, embryos are microinjected with SJ-000063181 (typically 1-10 microM final concentration) or incubated in embryo water containing the compound for 24-48 hours at 28degC. Control embryos receive vehicle (0.1% DMSO). Embryos are then fixed and subjected to whole-mount in situ hybridization (WISH) to visualize the expression of BMP target genes (e.g., msx, bmp4) or stained with alizarin red to visualize skeletal development. The effects on dorsoventral patterning are assessed microscopically.
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| ADME/Pharmacokinetics |
As a small molecule research probe, detailed pharmacokinetic data for SJ-000063181 is not publicly available. The compound has a molecular weight of 296.72 g/mol and is soluble in DMSO. For in vivo studies in zebrafish, the compound is directly added to the embryo water, where it is absorbed through the chorion and skin. The compound is metabolically stable enough for developmental studies lasting 24-72 hours. Mammalian PK studies would be required if the compound is to be advanced to preclinical models.
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| Toxicity/Toxicokinetics |
Specific toxicity data for SJ-000063181 is not available as it is a research-grade compound not intended for human use. In zebrafish toxicity studies, the compound is typically used at concentrations of 1-10 microM without significant acute toxicity or developmental malformations at lower doses, but high concentrations may cause non-specific effects or embryonic lethality. Standard safety precautions (gloves, lab coat) should be used when handling the compound powder. It should be stored protected from light at -80degC for long-term stability.
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| References | |
| Additional Infomation |
SJ-000063181 is a valuable chemical probe for investigating BMP signaling, a pathway critical for bone formation and embryonic development. Its small molecular weight and ability to penetrate zebrafish embryos make it particularly useful for developmental biology studies in this model organism. By activating BMP signaling, it can be used to study dorsoventral patterning, organogenesis, and skeletal development. It is not a pharmaceutical drug and is not approved for clinical use. The compound is for research use only.
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| Molecular Formula |
C14H14CLFN2O2
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|---|---|
| Molecular Weight |
296.724565982819
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| Exact Mass |
296.072
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| CAS # |
945189-68-4
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| PubChem CID |
17253337
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| Appearance |
White to off-white solid powder
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| LogP |
3.9
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
20
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| Complexity |
343
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| Defined Atom Stereocenter Count |
0
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| SMILES |
CC(C)CC1=CC(=NO1)C(=O)NC2=CC(=C(C=C2)F)Cl
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| InChi Key |
PBZNVOPQXYXTPC-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C14H14ClFN2O2/c1-8(2)5-10-7-13(18-20-10)14(19)17-9-3-4-12(16)11(15)6-9/h3-4,6-8H,5H2,1-2H3,(H,17,19)
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| Chemical Name |
N-(3-chloro-4-fluorophenyl)-5-(2-methylpropyl)-1,2-oxazole-3-carboxamide
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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 Note: This product requires protection from light (avoid light exposure) during transportation and storage. |
| 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 : ~100 mg/mL (~337.02 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (8.43 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (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 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.3702 mL | 16.8509 mL | 33.7018 mL | |
| 5 mM | 0.6740 mL | 3.3702 mL | 6.7404 mL | |
| 10 mM | 0.3370 mL | 1.6851 mL | 3.3702 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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