Delgocitinib
Based on 2 publication(s) in Google Scholar
Delgocitinib (JTE-052) is a specific JAK inhibitor with IC50s of 2.8, 2.6, 13 and 58 nM for JAK1, JAK2, JAK3 and Tyk2, respectively.
For research use only. We do not sell to patients.
- Purity: 99.61%
- CAS No.: 1263774-59-9
- Formula: C16H18N6O
- Molecular Weight:310.35
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Protocol
- Purity & Documentation
- References
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Help & FAQs
Publications Citing Use of MedChemExpress (MCE) Delgocitinib
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Biological Activity
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JAK2 2.6 nM (IC50) |
JAK1 2.8 nM (IC50) |
JAK3 13 nM (IC50) |
Tyk2 58 nM (IC50) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| A549 | IC50 |
0.025 μM
Compound: ent-60, JTE-052
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Inhibition of JAK1/JAK2 in human A549 assessed as reduction in IL31-induced Stat3 phosphorylation preincubated for 30 mins followed by IL31 stimulation and measured after 15 mins
Inhibition of JAK1/JAK2 in human A549 assessed as reduction in IL31-induced Stat3 phosphorylation preincubated for 30 mins followed by IL31 stimulation and measured after 15 mins
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[PMID: 32511913] |
| PBMC | IC50 |
0.018 μM
Compound: ent-60, JTE-052
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Inhibition of JAK1/Tyk2 in human PBMC assessed as reduction in INFalpha-induced Stat1 phosphorylation in CD3+CD4+ cells preincubated for 30 mins followed by INFalpha stimulation and measured after 15 mins
Inhibition of JAK1/Tyk2 in human PBMC assessed as reduction in INFalpha-induced Stat1 phosphorylation in CD3+CD4+ cells preincubated for 30 mins followed by INFalpha stimulation and measured after 15 mins
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[PMID: 32511913] |
| PBMC | IC50 |
0.033 μM
Compound: ent-60, JTE-052
|
Inhibition of JAK1/JAK2 in human PBMC assessed as reduction in IL6-induced Stat3 phosphorylation in CD3- CD4+ cells preincubated for 30 mins followed by IL6 stimulation and measured after 15 mins
Inhibition of JAK1/JAK2 in human PBMC assessed as reduction in IL6-induced Stat3 phosphorylation in CD3- CD4+ cells preincubated for 30 mins followed by IL6 stimulation and measured after 15 mins
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[PMID: 32511913] |
| PBMC | IC50 |
0.04 μM
Compound: ent-60, JTE-052
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Inhibition of JAK1/JAK3 in human PBMC assessed as reduction in IL2-induced Stat5 phosphorylation in CD3+CD4+ cells preincubated for 30 mins followed by IL2 stimulation and measured after 15 mins
Inhibition of JAK1/JAK3 in human PBMC assessed as reduction in IL2-induced Stat5 phosphorylation in CD3+CD4+ cells preincubated for 30 mins followed by IL2 stimulation and measured after 15 mins
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[PMID: 32511913] |
| PBMC | IC50 |
0.084 μM
Compound: ent-60, JTE-052
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Inhibition of JAK2/Tyk2 in human PBMC assessed as reduction in IL-23-induced Stat3 phosphorylation in CD3+CD4+ cells preincubated for 30 mins followed by IL-23 stimulation and measured after 15 mins
Inhibition of JAK2/Tyk2 in human PBMC assessed as reduction in IL-23-induced Stat3 phosphorylation in CD3+CD4+ cells preincubated for 30 mins followed by IL-23 stimulation and measured after 15 mins
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[PMID: 32511913] |
| PBMC | IC50 |
0.3 μM
Compound: ent-60, JTE-052
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Inhibition of JAK2 in human PBMC assessed as reduction in GM-CSF-induced Stat5 phosphorylation in CD3- CD4+ cells preincubated for 30 mins followed by GM-CSF stimulation and measured after 15 mins
Inhibition of JAK2 in human PBMC assessed as reduction in GM-CSF-induced Stat5 phosphorylation in CD3- CD4+ cells preincubated for 30 mins followed by GM-CSF stimulation and measured after 15 mins
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[PMID: 32511913] |
| Sf21 | IC50 |
0.0026 μM
Compound: ent-60, JTE-052
|
Inhibition of N-terminal GST-fused human JAK2 (880 to end residues) expressed in baculovirus infected Sf21 cells using TK-substrate-biotin as substrate incubated for 60 mins in presence of ATP by fluorescence method
Inhibition of N-terminal GST-fused human JAK2 (880 to end residues) expressed in baculovirus infected Sf21 cells using TK-substrate-biotin as substrate incubated for 60 mins in presence of ATP by fluorescence method
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[PMID: 32511913] |
| Sf9 | IC50 |
0.013 μM
Compound: ent-60, JTE-052
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Inhibition of human JAK3 (780 to end residues) expressed in baculovirus infected Sf9 cells using TK-substrate-biotin as substrate incubated for 60 mins in presence of ATP by fluorescence method
Inhibition of human JAK3 (780 to end residues) expressed in baculovirus infected Sf9 cells using TK-substrate-biotin as substrate incubated for 60 mins in presence of ATP by fluorescence method
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[PMID: 32511913] |
| T-cell | IC50 |
0.0089 μM
Compound: ent-60, JTE-052
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Inhibition of IL2-induced human T cell proliferation preincubated for 30 mins followed by IL2 stimulation and measured after 3 days by [3H]thymidine incorporation based scintillation counting method
Inhibition of IL2-induced human T cell proliferation preincubated for 30 mins followed by IL2 stimulation and measured after 3 days by [3H]thymidine incorporation based scintillation counting method
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[PMID: 32511913] |
| T-cell | IC50 |
8.9 nM
Compound: 17
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Inhibition of IL-2 induced human T cell proliferation preincubated with compound for 30 mins followed by IL-2 induction and measured after 3 days in the presence of [3H]thymidine by scintillation counter analysis
Inhibition of IL-2 induced human T cell proliferation preincubated with compound for 30 mins followed by IL-2 induction and measured after 3 days in the presence of [3H]thymidine by scintillation counter analysis
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[PMID: 32120325] |
In the enzymatic assays, Delgocitinib potently inhibits all of the JAK subtypes with IC50 values of 2.8±0.6, 2.6±0.2, 13±0 and 58±9 nM for JAK1, JAK2, JAK3 and Tyk2, respectively. Lineweaver-Burk plots show that the inhibition mode of Delgocitinib toward all JAKs is competitive with ATP with Ki values of 2.1±0.3, 1.7±0.0, 5.5±0.3 and 14±1 nM for JAK1, JAK2, JAK3 and Tyk2, respectively. In these cell-based cytokine signaling assays, Delgocitinib inhibits the phosphorylation of Stat proteins induced by IL-2, IL-6, IL-23, GM-CSF, and IFN-α with IC50 values of 40±9, 33±14, 84±11, 304±22 and 18±3 nM, respectively. Delgocitinib also inhibits IL-2-induced proliferation of T cells in a concentration-dependent manner (IC50=8.9±3.6 nM), and its potency is similar to that of CP-690550 (IC50=16 nM)[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 1263774-59-9
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Appearance Solid
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Molecular Weight 310.35
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Formula C16H18N6O
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Color White to off-white
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SMILES
O=C(N(C[C@@H]1C)[C@]21CN(C3=C(C=CN4)C4=NC=N3)CC2)CC#N
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Synonyms
JTE-052
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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 2 years -20°C 1 year
Publications (2)
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Journal Impact Factor
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Most Recent
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J Clin Med
Aryl Hydrocarbon Receptor Activation Downregulates IL-33 Expression in Keratinocytes via Ovo-Like 1. [Abstract]2020 Mar 24;9(3):891. PMID: 32214018 -
Solvent & Solubility
DMSO : ≥ 58 mg/mL (186.89 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
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)
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.
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.
Protocol
For determination of IL-2-induced T cell proliferation, human T cells are precultured with 10 μg/mL PHA-M for 3 days and plated in 96-well plates at 1.0×104 cells/well in the presence or absence of various concentrations of Delgocitinib. Following preincubation with Delgocitinib for 30 min at 37°C, the cells are stimulated by adding 20 ng/mL recombinant human IL-2 to each well and incubated for 3 days at 37°C under 5 % CO2. After completion of the culture period, the cells are harvested with a 96-well harvester and counted in a scintillation counter[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Lewis rats are used in this study. First, collagen-induced arthritis (CIA) is induced in rats. Lewis rats are immunized with 1 mL of the emulsion (1 mg of type II collagen) via ten intradermal injections on the back under anesthesia. The rats are then challenged with 0.2 mL of the emulsion injected into the base of the tail on day 8 under anesthesia. Delgocitinib is given orally once daily from day 1 to day 21 (preventive administration) or from day 15 to day 28 (therapeutic administration). After arthritis induction, the hind paw volume is measured by a water displacement method using a plethysmometer. On day 22 or day 29, the rats are euthanized, and their hind paws are excised and X-rayed or processed for histological evaluation[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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)
- 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, 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 | 3.2222 mL | 16.1108 mL | 32.2217 mL | 80.5542 mL |
| 5 mM | 0.6444 mL | 3.2222 mL | 6.4443 mL | 16.1108 mL | |
| 10 mM | 0.3222 mL | 1.6111 mL | 3.2222 mL | 8.0554 mL | |
| 15 mM | 0.2148 mL | 1.0741 mL | 2.1481 mL | 5.3703 mL | |
| 20 mM | 0.1611 mL | 0.8055 mL | 1.6111 mL | 4.0277 mL | |
| 25 mM | 0.1289 mL | 0.6444 mL | 1.2889 mL | 3.2222 mL | |
| 30 mM | 0.1074 mL | 0.5370 mL | 1.0741 mL | 2.6851 mL | |
| 40 mM | 0.0806 mL | 0.4028 mL | 0.8055 mL | 2.0139 mL | |
| 50 mM | 0.0644 mL | 0.3222 mL | 0.6444 mL | 1.6111 mL | |
| 60 mM | 0.0537 mL | 0.2685 mL | 0.5370 mL | 1.3426 mL | |
| 80 mM | 0.0403 mL | 0.2014 mL | 0.4028 mL | 1.0069 mL | |
| 100 mM | 0.0322 mL | 0.1611 mL | 0.3222 mL | 0.8055 mL |
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