SHIP1-IN-1
Based on 1 Customer Validation
SHIP1-IN-1 is an orally active, blood-brain barrier-permeable SHIP1 ligand. SHIP1-IN-1 exhibits IC50 values of 384 μM and 177 μM against human SHIP1, and an IC50 value of 379 μM against murine SHIP1. SHIP1-IN-1 alters the binding state of SHIP1 to phosphatidylinositol membranes, and regulates phosphoinositide pools and phosphorylated AKT levels. SHIP1-IN-1 enhances the uptake of myelin/membrane fragments and amyloid proteins by microglia, alters gene expression and reduces IL-1β levels. SHIP1-IN-1 can be used in studies related to Alzheimer's disease.
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- Pureté : 99.89%
- CAS No.: 3027375-00-1
- Formule: C20H21ClN4O
- Masse moléculaire:368.86
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Stockage:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Activité biologique
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Chemical Information
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Solvant et solubilité
- Pureté et documentation
- Références
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Help & FAQs
Activité biologique
Description
IC50 & Target
[1]|
IL-1β |
Akt |
In Vitro
SHIP1-IN-1 (compound 32) inhibits the human two‑domain SHIP1 protein construct with an IC50 of 384 μM, the human five‑domain SHIP1 protein construct with an IC50 of 177 μM, and the murine five‑domain SHIP1 protein construct with an IC50 of 379 μM[1].
SHIP1-IN-1 (1.0-10 μM) modulates the phosphoinositide association profile of the human five-domain SHIP1 protein, increasing relative binding to PI(3,4)P2 at higher concentrations[1].
SHIP1-IN-1 (60 min treatment at 37 °C; 3 min heating at 44.2 °C) engages full-length SHIP1 in HMC3 cells, reducing protein thermal stability with an AC50 of 40.4 μM[1].
SHIP1-IN-1 (15 min) modulates proximal SHIP1-dependent AKT signaling in IL-4-conditioned THP-1 cells, reducing the pAKT (S473)/tAKT ratio with an IC50 of 4.0 μM and the pAKT (T308)/tAKT ratio with an IC50 of 5.3 μM[1].
SHIP1-IN-1 enhances pHrodo-myelin/membrane debris uptake in both BV2 murine microglia (EC50 = 0.777 μM) and primary murine microglia (EC50 = 0.484 μM), while reducing cell count and nuclear intensity with IC50 values of 3.45 and 6.46 μM in BV2 cells, and 5.65 and 19.4 μM in primary microglia, respectively[1].
SHIP1-IN-1 (50 nM-950 μM; 20 min pre-incubation with enzyme, 10 min reaction with substrate) inhibits purified SHIP1 Ptase-C2 domain activity with an IC50 of 302 μM[2].
SHIP1-IN-1 (Example 9) increases phagocytosis, reduces cell count, and alters nuclear intensity in primary mouse microglia in an in vitro high-content imaging assay[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:C57BL/6J (wild type, male/female, 14 months old); hAbetaSAA knock-in (APP-SAA KI, male/female, 14 months old)[1]
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Dosage:150 mg/kg
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Administration:p.o.; three times at 12-h intervals
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Result:Achieved brain exposure sufficient to alter gene expression and reduce IL-1β levels.
Chemical Information
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CAS No. 3027375-00-1
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Appearance Solid
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Masse moléculaire 368.86
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Formule C20H21ClN4O
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Color Off-white to light yellow
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SMILES
ClC(C=CC=C1)=C1COC2=CN=CC(C3=CN(C4CCNCC4)N=C3)=C2
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Solvant et solubilité
In Vitro:
DMSO : 50 mg/mL (135.55 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 (sealed storage, away from moisture). 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 (sealed storage, away from moisture). 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)
Pureté et documentation
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Fiche technique (273 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Instruction de manipulation (2659 KB)
Références
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 (sealed storage, away from moisture). 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 | 2.7111 mL | 13.5553 mL | 27.1106 mL | 67.7764 mL |
| 5 mM | 0.5422 mL | 2.7111 mL | 5.4221 mL | 13.5553 mL | |
| 10 mM | 0.2711 mL | 1.3555 mL | 2.7111 mL | 6.7776 mL | |
| 15 mM | 0.1807 mL | 0.9037 mL | 1.8074 mL | 4.5184 mL | |
| 20 mM | 0.1356 mL | 0.6778 mL | 1.3555 mL | 3.3888 mL | |
| 25 mM | 0.1084 mL | 0.5422 mL | 1.0844 mL | 2.7111 mL | |
| 30 mM | 0.0904 mL | 0.4518 mL | 0.9037 mL | 2.2592 mL | |
| 40 mM | 0.0678 mL | 0.3389 mL | 0.6778 mL | 1.6944 mL | |
| 50 mM | 0.0542 mL | 0.2711 mL | 0.5422 mL | 1.3555 mL | |
| 60 mM | 0.0452 mL | 0.2259 mL | 0.4518 mL | 1.1296 mL | |
| 80 mM | 0.0339 mL | 0.1694 mL | 0.3389 mL | 0.8472 mL | |
| 100 mM | 0.0271 mL | 0.1356 mL | 0.2711 mL | 0.6778 mL |
SHIP1-IN-1 Related Classifications
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