LTβR-IN-1
Based on 1 Customer Validation
LTβR-IN-1 (Compound 919278) is a potent, selective lymphotoxin β receptor (LTβR) inhibitor. LTβR-IN-1 also selectively inhibits the nuclear translocation of p52 depended on TNF12A, instead of the nuclear translocation of p65 mediated by TNF-α receptor. LTβR-IN-1 regulates the NF-kB signaling pathway IN a ligand-independent manner.
For research use only. We do not sell to patients.
- Purity: 99.79%
- CAS No.: 2189366-77-4
- Formula: C18H16N4O2
- Molecular Weight:320.35
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
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Biological Activity
LTβR; p52 translocation; MAP3K14; NF-κB[1]
LTβR-IN-1 (compound 919278) (1 nM-100 μM; 30 min) inhibits p52 nuclear translocation in response to stimulation with Anti-LTβR or TWEAK (20 ng/mL, respectively; 4 h) with IC50s of 0.169 μM and 0.167 μM, respectively[1].
LTβR-IN-1 (3 nM-30 μM; 45 min) reduces the binding affinities of both CDK12 and its associated protein, CCNK in both TWEAK-stimulated and control U-2 OS cells, with IC50s of 50-61 nM for CDK12 and 29-68 nM for CCNK, respectively[1].
LTβR-IN-1 reduces the mRNA abundance of MAP3K14 in with an IC50 value of 0.32 μM in U-2 OS cells[1].
LTβR-IN-1 (1-10 μM; 30 min) decreases the phosphorylation of serine-2 (Ser2) on the C-terminal domain (CTD) of RNA polymerase (Pol) II[1].
LTβR-IN-1 regulates the noncanonical pathway in a ligandindependent manner and selectively inhibits the noncanonical pathway while sparing the canonical NF-kB signaling pathway[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:U-2 OS cells
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Concentration:1 μM, 3 μM, and 10 μM
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Incubation Time:30 min
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Result:Reduced the phosphorylating of Ser2 in cells stimulated by 20 ng/mL TWEAK for 4 hr.
Note: CDK12 activated RNA Pol II–mediated transcription by phosphorylating Ser2 within the 52 heptad (Y1S2P3T4S5P6S7) repeats in the C-terminal domain (CTD) of RNA Pol II. Ser2 phosphorylation aids in the release of paused RNA Pol II from promoters, resulting in transcriptional elongation, which is particularly important for the transcription of some long, complex genes.
Chemical Information
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CAS No. 2189366-77-4
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Appearance Solid
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Molecular Weight 320.35
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Formula C18H16N4O2
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Color White to off-white
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SMILES
C[C@@H](N(CC1=C2C=CC=C1)C2=O)C(NC3=NC4=CC=CC=C4N3)=O
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvent & Solubility
DMSO : 200 mg/mL (624.32 mM; ultrasonic and warming and heat to 60°C; 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)
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: ≥ 2.08 mg/mL (6.49 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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: ≥ 2.08 mg/mL (6.49 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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.
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.
Purity & Documentation
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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)
References
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 |
|---|---|---|---|---|---|
| DMSO | 1 mM | 3.1216 mL | 15.6079 mL | 31.2159 mL | 78.0396 mL |
| 5 mM | 0.6243 mL | 3.1216 mL | 6.2432 mL | 15.6079 mL | |
| 10 mM | 0.3122 mL | 1.5608 mL | 3.1216 mL | 7.8040 mL | |
| 15 mM | 0.2081 mL | 1.0405 mL | 2.0811 mL | 5.2026 mL | |
| 20 mM | 0.1561 mL | 0.7804 mL | 1.5608 mL | 3.9020 mL | |
| 25 mM | 0.1249 mL | 0.6243 mL | 1.2486 mL | 3.1216 mL | |
| 30 mM | 0.1041 mL | 0.5203 mL | 1.0405 mL | 2.6013 mL | |
| 40 mM | 0.0780 mL | 0.3902 mL | 0.7804 mL | 1.9510 mL | |
| 50 mM | 0.0624 mL | 0.3122 mL | 0.6243 mL | 1.5608 mL | |
| 60 mM | 0.0520 mL | 0.2601 mL | 0.5203 mL | 1.3007 mL | |
| 80 mM | 0.0390 mL | 0.1951 mL | 0.3902 mL | 0.9755 mL | |
| 100 mM | 0.0312 mL | 0.1561 mL | 0.3122 mL | 0.7804 mL |
LTβR-IN-1 Related Classifications
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