UM-259 hydrochloride
UM-259 hydrochloride is a STING inhibitor with activity against both murine and human STING (including the STINGR232 mutant). UM-259 hydrochloride inhibits STING-dependent signaling pathways, blocks STING oligomerization, and acts on human primary CD14+ monocytes. UM-259 hydrochloride can be used for research on amyotrophic lateral sclerosis, lupus erythematosus, Aicardi-Goutières syndrome, and infant-onset STING-associated vasculopathy.
For research use only. We do not sell to patients.
- Formula: C27H22ClF2N7O5
- Molecular Weight:597.96
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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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
Biological Activity
UM-259 hydrochloride (0.08-40 μM; 1 h + 24 h; diABZI) inhibits STING-dependent signaling pathways in THP1-Dual KI-hSTING-R232 cells, with an EC50 of 1.50 μM[1].
UM-259 hydrochloride (0.2-5 μM; 1 h + 2 h; diABZI) dose-dependently inhibits diABZI-induced IFNβ and IL6 gene expression in iBMDM, and exhibits superior potency to LB244 (HY-156117) at a concentration of 5 μM[1].
UM-259 hydrochloride (0.2-5 μM; 1 h +24 h; diABZI) dose-dependently inhibits diABZI-induced IFNβ secretion in iBMDMs, and its efficacy at 5 μM is superior to that of LB244[1].
UM-259 hydrochloride (2.5 μM; 1 h + 16 h; diABZI) inhibits diABZI-induced IFNβ secretion in primary human CD14+ monocytes[1].
UM-259 hydrochloride (5 μM; 1 h+0-120 min; diABZI) inhibits diABZI-induced phosphorylation of TBK1 and IRF3 in wild-type bone marrow-derived macrophages (BMDMs)[1].
UM-259 hydrochloride (5 μM; 1 h+30 min; diABZI) blocks diABZI-induced STING oligomerization in wild-type bone marrow-derived macrophages (BMDMs)[1].
UM-259 hydrochloride (0.2-5 μM; 24 h) exhibits only limited cytotoxicity against iBMDMs[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:primary human CD14+ monocytes
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Concentration:2.5 μM
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Incubation Time:1 h pre-incubation, followed by 16 h incubation with diABZI
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Result:Blocked diABZI-induced IFNβ secretion, reducing levels to near baseline (DMSO without diABZI) levels.
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Cell Line:wild-type bone marrow-derived macrophages (BMDMs)
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Concentration:5 μM
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Incubation Time:1 h pre-incubation, followed by 0-120 min incubation with diABZI
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Result:Inhibited diABZI-induced phosphorylation of TBK1 and IRF3, reducing phosphorylated protein levels compared to vehicle-treated cells at all time points tested.
Blocked diABZI-induced STING oligomer formation, with only STING monomers detected in native fractions (similar to unstimulated cells), while vehicle-treated cells showed robust STING oligomer formation.
Chemical Information
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Appearance Solid
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Molecular Weight 597.96
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Formula C27H22ClF2N7O5
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SMILES
O=C(C1=NOC(C2=CC=C(F)C=C2F)=C1)NC3(C4=NC5=CC=CC=C5N4)CCN(C(C6=CC=C([N+]([O-])=O)O6)=N)CC3.Cl
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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 : 100 mg/mL (167.24 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. 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: ≥ 2.5 mg/mL (4.18 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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: ≥ 2.5 mg/mL (4.18 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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.
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
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 | 1.6724 mL | 8.3618 mL | 16.7235 mL | 41.8088 mL |
| 5 mM | 0.3345 mL | 1.6724 mL | 3.3447 mL | 8.3618 mL | |
| 10 mM | 0.1672 mL | 0.8362 mL | 1.6724 mL | 4.1809 mL | |
| 15 mM | 0.1115 mL | 0.5575 mL | 1.1149 mL | 2.7873 mL | |
| 20 mM | 0.0836 mL | 0.4181 mL | 0.8362 mL | 2.0904 mL | |
| 25 mM | 0.0669 mL | 0.3345 mL | 0.6689 mL | 1.6724 mL | |
| 30 mM | 0.0557 mL | 0.2787 mL | 0.5575 mL | 1.3936 mL | |
| 40 mM | 0.0418 mL | 0.2090 mL | 0.4181 mL | 1.0452 mL | |
| 50 mM | 0.0334 mL | 0.1672 mL | 0.3345 mL | 0.8362 mL | |
| 60 mM | 0.0279 mL | 0.1394 mL | 0.2787 mL | 0.6968 mL | |
| 80 mM | 0.0209 mL | 0.1045 mL | 0.2090 mL | 0.5226 mL | |
| 100 mM | 0.0167 mL | 0.0836 mL | 0.1672 mL | 0.4181 mL |
UM-259 hydrochloride Related Classifications
HY-178049A Related Classifications
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