KG-655
Based on 1 Customer Validation
KG-655 is a ligand that specifically binds to the ARNT PAS-B domain. KG-655 binds to the internal cavity of ARNT PAS-B to restrict its variable folded conformation, disrupts the interaction between ARNT PAS-B and the transcriptional coactivator TACC3, and promotes the homodimerization of ARNT PAS-B. KG-655 is widely applicable to cancer-related research.
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- Pureza: 99.06%
- No. CAS: 349-58-6
- Fòrmula: C8H4F6O
- Peso molecular:230.11
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Almacenamiento:
4°C, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
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Actividad biológica
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FGFR-TACC3 |
KG-655 (5 μM) promotes homodimerization of the wild-type human ARNT PAS-B domain, though less strongly than KG-548[1].
KG-655 (1 mM) binds to both the β-sheet surface (dependent on residues I364 and I458) and an internal cavity of the wild-type human ARNT PAS-B domain, with the two binding modes acting independently[1].
KG-655 (5 mM) binds to the internal cavity of the ARNT PAS-B ARNTI458V mutant, demonstrating that its internal binding mode is independent of surface binding[1].
KG-655 (5 mM) exhibits millimolar binding affinity to wild-type human ARNT PAS-B via dual surface and internal modes; the Y456T mutation substantially disrupts its surface binding but allows retained, reduced internal cavity binding with high micromolar to low millimolar affinity[1].
KG-655 (5 mM) binds to both the β-sheet surface (via residue I458) and internal cavity of wild-type human ARNT PAS-B, with the two binding modes acting independently as disruption of surface binding does not affect internal binding[1].
KG-655 binds within the internal cavity of the wild-type human ARNT PAS-B domain in multiple orientations, consistent with NOE-based distance restraints and requiring partial opening of the cavity[1].
Binding of KG-655 to human ARNT PAS-B reduces pressure-induced nonlinear 15N chemical shift heterogeneity, with stdev(ci [15N]) decreasing from 84 × (2×10-10 ppm/bar2) to 51 × (2×10-10 ppm/bar2), consistent with internal cavity binding[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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No. CAS 349-58-6
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Appearance <20°C Solid,>21°C Liquid
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Peso molecular 230.11
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Fòrmula C8H4F6O
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Color Colorless to off-white
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SMILES
OC1=CC(C(F)(F)F)=CC(C(F)(F)F)=C1
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
4°C, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)
Solvente y solubilidad
DMSO : 200 mg/mL (869.15 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 (stored under nitrogen). 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 (stored under nitrogen). 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)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 5 mg/mL (21.73 mM); Clear solution
This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL. * In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Pureza y Documentación
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Ficha de datos (274 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
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Instrucciones de manejo (2659 KB)
Referencias
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 (stored under nitrogen). 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 |
|---|---|---|---|---|---|
| DMSO | 1 mM | 4.3457 mL | 21.7287 mL | 43.4575 mL | 108.6437 mL |
| 5 mM | 0.8691 mL | 4.3457 mL | 8.6915 mL | 21.7287 mL | |
| 10 mM | 0.4346 mL | 2.1729 mL | 4.3457 mL | 10.8644 mL | |
| 15 mM | 0.2897 mL | 1.4486 mL | 2.8972 mL | 7.2429 mL | |
| 20 mM | 0.2173 mL | 1.0864 mL | 2.1729 mL | 5.4322 mL | |
| 25 mM | 0.1738 mL | 0.8691 mL | 1.7383 mL | 4.3457 mL | |
| 30 mM | 0.1449 mL | 0.7243 mL | 1.4486 mL | 3.6215 mL | |
| 40 mM | 0.1086 mL | 0.5432 mL | 1.0864 mL | 2.7161 mL | |
| 50 mM | 0.0869 mL | 0.4346 mL | 0.8691 mL | 2.1729 mL | |
| 60 mM | 0.0724 mL | 0.3621 mL | 0.7243 mL | 1.8107 mL | |
| 80 mM | 0.0543 mL | 0.2716 mL | 0.5432 mL | 1.3580 mL | |
| 100 mM | 0.0435 mL | 0.2173 mL | 0.4346 mL | 1.0864 mL |
KG-655 Related Classifications
HY-W012248 Related Classifications
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