OD36
Based on 1 Customer Validation
OD36 is a RIPK2 inhibitor with an IC50 of 5.3 nM. OD36 is a macrocyclic inhibitor with potent binding to the ALK2 kinase ATP pocket. OD36 shows ALK2-directed activity with KDs of 37 nM.
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- Pureza: 99.33%
- No. CAS: 1638644-62-8
- Fòrmula: C16H15ClN4O2
- Peso molecular:330.77
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Pureza y Documentación
- Referencias
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Help & FAQs
Actividad biológica
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RIPK2 5.3 nM (IC50) |
ACVR1 37 nM (Kd) |
ACVR1 47 nM (IC50) |
ALK2 R206H 22 nM (IC50) |
OD36 also inhibits ALK2 and ALK2 R206H with IC50s of 47 and 22 nM, respevtively[1].
OD36 shows activity against ALK1 with a KD of 90 nM[2].
OD36 potently antagonize mutant ALK2 signaling and osteogenic differentiation[2].
OD36 (0.1-1 μM; 24 h) efficiently inhibits BMP-6 (50 ng/mL)-induced p-Smad1/5 in KS483 cells[2].
Preincubation of fibrodysplasia ossificans progressiva (FOP) endothelial colony-forming cells (ECFCs) with OD36 (0.5 μM) completely prevents the activation of Smad1/5 and gene targets ID-1 and ID-3 in response to activin A[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:KS483 cells
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Concentration:0.1, 0.2, and 1 μM
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Incubation Time:
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Result:Inhibited BMP-6 induced p-Smad1/5.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:C57BL/6 mice, muramyl dipeptide (MDP)-induced model of peritonitis[3]
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Dosage:6.25 mg/kg
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Administration:Intraperitoneal injection, 30 min prior to MDP
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Result:Inhibited the recruitment of inflammatory cells to the peritoneum, specifically that of neutrophils, and, to a lesser extent, lymphocytes. Decreased RIPK2-specific genes as well as inflammatory cytokine and chemokine gene expression.
Chemical Information
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No. CAS 1638644-62-8
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Appearance Solid
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Peso molecular 330.77
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Fòrmula C16H15ClN4O2
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Color White to off-white
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SMILES
ClC1=CC(C2=C3N/C(C=CN3N=C2)=N/CCOCCO4)=CC4=C1
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvente y solubilidad
DMSO : 33.33 mg/mL (100.76 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. 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. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Pureza y Documentación
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Ficha de datos (283 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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Instrucciones de manejo (2659 KB)
Referencias
[1]. Justine T Tigno-Aranjuez, et al. In vivo inhibition of RIPK2 kinase alleviates inflammatory disease. J Biol Chem. 2014 Oct 24;289(43):29651-64. [Content Brief]
[2]. Gonzalo Sánchez-Duffhues, et al. Development of Macrocycle Kinase Inhibitors for ALK2 Using Fibrodysplasia Ossificans Progressiva-Derived Endothelial Cells. JBMR Plus. 2019 Oct 7;3(11):e10230. [Content Brief]
[3]. Tigno-Aranjuez JT, et al. In vivo inhibition of RIPK2 kinase alleviates inflammatory disease. J Biol Chem. 2014 Oct 24;289(43):29651-64. [Content Brief]
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. 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 |
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| DMSO | 1 mM | 3.0232 mL | 15.1162 mL | 30.2325 mL | 75.5812 mL |
| 5 mM | 0.6046 mL | 3.0232 mL | 6.0465 mL | 15.1162 mL | |
| 10 mM | 0.3023 mL | 1.5116 mL | 3.0232 mL | 7.5581 mL | |
| 15 mM | 0.2015 mL | 1.0077 mL | 2.0155 mL | 5.0387 mL | |
| 20 mM | 0.1512 mL | 0.7558 mL | 1.5116 mL | 3.7791 mL | |
| 25 mM | 0.1209 mL | 0.6046 mL | 1.2093 mL | 3.0232 mL | |
| 30 mM | 0.1008 mL | 0.5039 mL | 1.0077 mL | 2.5194 mL | |
| 40 mM | 0.0756 mL | 0.3779 mL | 0.7558 mL | 1.8895 mL | |
| 50 mM | 0.0605 mL | 0.3023 mL | 0.6046 mL | 1.5116 mL | |
| 60 mM | 0.0504 mL | 0.2519 mL | 0.5039 mL | 1.2597 mL | |
| 80 mM | 0.0378 mL | 0.1890 mL | 0.3779 mL | 0.9448 mL | |
| 100 mM | 0.0302 mL | 0.1512 mL | 0.3023 mL | 0.7558 mL |
OD36 Related Classifications
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