BI605906
Based on 8 publication(s) in Google Scholar
BI605906, a chemical probe, is a novel IKKβ inhibitor with an IC50 value of 380 nM when assayed at 0.1 mM ATP.
Para uso exclusivo en investigación. No vendemos a pacientes.
The BI605906 was designed by Boehringer Ingelheim and could be obtained free of charge through the Boehringer Ingelheim open innovation portal opnMe.com, associated with its negative control.
- Pureza : 99.67%
- No. CAS: 960293-88-3
- Fòrmula: C17H22F2N4O3S2
- Peso molecular:432.51
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Protocolo
- Pureza y Documentación
- Referencias
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) BI605906
More- Mol Cell. 2017 Jun 1;66(5):698-710.e5. [Abstract]
- Proc Natl Acad Sci U S A. 2023 Dec 12;120(50):e2313148120. [Abstract]
- Eur J Pharmacol. 2024 May 5:970:176480. [Abstract]
- Sci Rep. 2019 Jan 17;9(1):193. [Abstract]
- J Biol Chem. 2020 Oct 16;295(42):14325-14342. [Abstract]
- Cytokine. 2023 Sep:169:156302. [Abstract]
- Cell Biochem Funct. 2019 Jan;37(1):4-10. [Abstract]
- McGill University. 2023 Dec.
Customer Validation & Images
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Actividad biológica
Descripciòn
IC50 & Target
[1]|
IKKβ 380 nM (IC50, at 0.1 mM ATP) |
In Vitro
BI605906 is an inhibitor of IKKβ with improved selectivity. BI605906 inhibits IKKβ in vitro with an IC50 value of 380 nM when assayed at 0.1 mM ATP. The only other protein kinase that is inhibited of over 100 tested, which include IKKα, IKKε and TBK1, is the insulin-like growth factor 1 (IGF1) receptor (IC50=7.6 μM). BI605906 partially inhibits the IL-1-stimulated activation of IKKε/TBK1[1]. In primary mouse hepatocytes, Metformin treatment for 3 hours suppresses TNFα-induced degradation of the NF-κB negative regulator IκB, while modulating AMPK and MTOR signaling in a dose-dependent manner. The magnitude of the effect on IκB is comparable with BI605906. Unlike Metformin, BI605906 (10 μM ) does not suppress signaling downstream of mTOR nor does it activate AMPK. TNF-α-dependent expression of CINC-1/CXCL1, CXCL2, IL-1β, and IL-6 is strongly inhibited by both Metformin and BI605906 (10 μM)[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
Chemical Information
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No. CAS 960293-88-3
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Appearance Solid
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Peso molecular 432.51
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Fòrmula C17H22F2N4O3S2
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Color Light yellow to yellow
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SMILES
O=C(C1=C(N)C2=C(C(F)(F)CC)C=C(N3CCC(S(=O)(C)=O)CC3)N=C2S1)N
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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 2 years -20°C 1 year
Publications (8)
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Journal Impact Factor
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Most Recent
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Mol Cell
2017 Jun 1;66(5):698-710.e5. PMID: 28506461
BI605906 purchased from MedChemExpress. Usage Cited in: Mol Cell. 2017 Jun 1;66(5):698-710.e5. [Abstract]
Western blot analysis of cell lysates from primary MEFs using the indicated antibodies. Cells are pre-treated with IKK2i (BI605906, 10 μM) for 1 hr, followed by stimulation with TNF (10 ng/mL) for the indicated times.
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Proc Natl Acad Sci U S A
ALPK1 mutants causing ROSAH syndrome or Spiradenoma are activated by human nucleotide sugars. [Abstract]2023 Dec 12;120(50):e2313148120. PMID: 38060563 -
Eur J Pharmacol
Curcumin analogue NL04 inhibits spinal cord central sensitization in rats with bone cancer pain by inhibiting NLRP3 inflammasome activation and reducing IL-1β production. [Abstract]2024 May 5:970:176480. PMID: 38490468 -
Sci Rep
2019 Jan 17;9(1):193. PMID: 30655563 -
J Biol Chem
2020 Oct 16;295(42):14325-14342. PMID: 32796029 -
Cytokine
TRAF6-TAK1-IKKβ pathway mediates TLR2 agonists activating "one-step" NLRP3 inflammasome in human monocytes. [Abstract]2023 Sep:169:156302. PMID: 37480791 -
Cell Biochem Funct
Metformin inhibits pro-inflammatory responses via targeting nuclear factor-κB in HaCaT cells. [Abstract]2019 Jan;37(1):4-10. PMID: 30520054 -
Solvente y solubilidad
In Vitro:
DMSO : 50 mg/mL (115.60 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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
In Vivo:
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 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 1.25 mg/mL (2.89 mM); Clear solution
This protocol yields a clear solution of ≥ 1.25 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (12.5 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: 1.25 mg/mL (2.89 mM); Suspended solution; Need ultrasonic
This protocol yields a suspended solution of 1.25 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (12.5 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.
In Vivo Dissolution Calculator
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.
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.
Protocolo
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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
Pureza y Documentación
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Ficha de datos (277 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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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, 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 | 2.3121 mL | 11.5604 mL | 23.1209 mL | 57.8021 mL |
| 5 mM | 0.4624 mL | 2.3121 mL | 4.6242 mL | 11.5604 mL | |
| 10 mM | 0.2312 mL | 1.1560 mL | 2.3121 mL | 5.7802 mL | |
| 15 mM | 0.1541 mL | 0.7707 mL | 1.5414 mL | 3.8535 mL | |
| 20 mM | 0.1156 mL | 0.5780 mL | 1.1560 mL | 2.8901 mL | |
| 25 mM | 0.0925 mL | 0.4624 mL | 0.9248 mL | 2.3121 mL | |
| 30 mM | 0.0771 mL | 0.3853 mL | 0.7707 mL | 1.9267 mL | |
| 40 mM | 0.0578 mL | 0.2890 mL | 0.5780 mL | 1.4451 mL | |
| 50 mM | 0.0462 mL | 0.2312 mL | 0.4624 mL | 1.1560 mL | |
| 60 mM | 0.0385 mL | 0.1927 mL | 0.3853 mL | 0.9634 mL | |
| 80 mM | 0.0289 mL | 0.1445 mL | 0.2890 mL | 0.7225 mL | |
| 100 mM | 0.0231 mL | 0.1156 mL | 0.2312 mL | 0.5780 mL |
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