Hck-IN-1
Based on 1 publication(s) in Google Scholar
Hck-IN-1 (compound B9), a diphenylpyrazolo compound, is a selective Nef-dependent Hck inhibitor with IC50s of 2.8 μM, >20 μM for Nef:Hck complex and Hck, respectively. Hck-IN-1 is a direct and wide HIV-1 Nef antagonists with an IC50 of 100-300 nM for wild-type HIV-1 replication. Hck-IN-1 binds pocket residue Asn126 and has anti-retroviral activity.
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- Reinheit: 98.10%
- CAS. Nr.: 1473404-51-1
- Formel: C16H11ClN6O3S
- Molecular Weight:402.81
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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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Publications Citing Use of MedChemExpress (MCE) Hck-IN-1
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Biologische Aktivität
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HIV-1 Nef 100-300 nM (IC50) |
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Cell Line
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Type | Value | Description | References |
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| TZM | CC50 |
10 μM
Compound: 1; B9
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Cytotoxicity against human TZM-bl cells by Cell Titer Blue assay
Cytotoxicity against human TZM-bl cells by Cell Titer Blue assay
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[PMID: 26852364] |
Hck-IN-1 (compound B9) shows weak activity against other Src-family members in vitro, with IC50 values >20 μM for c-Src, Lck and Lyn[1].
B9 (1 μM; 8 days) completely inhibits Nef-dependent SFK activation at a concentration of 1.0 μM[1].
Hck-IN-1 (0.1, 0.3, 1, 3 μM) also inhibits Nef-mediated enhancement of HIV-1 infectivity in a concentration-dependent manner in the reporter cell line, TZM-bl[1].
Hck-IN-1 inhibits the replication of all eleven HIV-1 Nef chimeras with IC50 values of ~ 300 nM in CEM-T4 cells, demonstrating that the compound is broadly active against HIV replication supported by a wide range of HIV-1 Nef proteins[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:CEM-T4 cells
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Concentration:1 μM
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Incubation Time:8 days
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Result:Completely inhibited Nef-dependent SFK activation at a concentration of 1.0 μM.
Chemical Information
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CAS. Nr. 1473404-51-1
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Appearance Solid
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Molecular Weight 402.81
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Formel C16H11ClN6O3S
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Color Yellow to orange
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SMILES
S=C(N1N=C(C2=CC=C([N+]([O-])=O)C=C2)C(/N=N/C3=CC=CC(Cl)=C3)=C1O)N
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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 (1)
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Journal Impact Factor
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Most Recent
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PLoS One
A novel small molecule screening assay using normal human chondrocytes toward osteoarthritis drug discovery. [Abstract]2024 Nov 1;19(11):e0308647. PMID: 39485774
Lösungsmittel & Löslichkeit
DMSO : 12.5 mg/mL (31.03 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)
Reinheit & Dokumentation
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Data Sheet (278 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 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 | 2.4826 mL | 12.4128 mL | 24.8256 mL | 62.0640 mL |
| 5 mM | 0.4965 mL | 2.4826 mL | 4.9651 mL | 12.4128 mL | |
| 10 mM | 0.2483 mL | 1.2413 mL | 2.4826 mL | 6.2064 mL | |
| 15 mM | 0.1655 mL | 0.8275 mL | 1.6550 mL | 4.1376 mL | |
| 20 mM | 0.1241 mL | 0.6206 mL | 1.2413 mL | 3.1032 mL | |
| 25 mM | 0.0993 mL | 0.4965 mL | 0.9930 mL | 2.4826 mL | |
| 30 mM | 0.0828 mL | 0.4138 mL | 0.8275 mL | 2.0688 mL |
Hck-IN-1 Related Classifications
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