Delgocitinib (Synonyms: JTE-052)

Name: Delgocitinib
Brand: MedChemExpress
SKU: HY-109053
Rating: 4.5 (1 reviews)

Cat. No.: HY-109053 Purity: 99.87%: FAQs
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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.

Delgocitinib Chemical Structure

CAS No. : 1263774-59-9

Size	Price	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 444	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 444	In-stock	Estimated Time of Arrival: December 31
Solid
1 mg	USD 210	In-stock	Estimated Time of Arrival: December 31
5 mg	USD 400	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 620	In-stock	Estimated Time of Arrival: December 31
25 mg	USD 1180	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 1829	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 2712	In-stock	Estimated Time of Arrival: December 31
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Based on 1 publication(s) in Google Scholar

Other Forms of Delgocitinib:

Delgocitinib ethanolate Get quote

1 Publications Citing Use of MCE Delgocitinib

•J Clin Med. 2020 Mar 24;9(3):891. [Abstract]

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View All Isoforms

JAK1 JAK2 JAK3 Tyk2 JAK

Biological Activity
Protocol
Purity & Documentation
References
Customer Review

Description

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^[1].

IC₅₀ & Target^[1]

JAK2

2.6 nM (IC₅₀)

JAK1

2.8 nM (IC₅₀)

JAK3

13 nM (IC₅₀)

Tyk2

58 nM (IC₅₀)

Cellular Effect

Cell Line	Type	Value	Description	References
A549	IC₅₀	0.025 μM Compound: ent-60, JTE-052	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	[PMID: 32511913]
PBMC	IC₅₀	0.018 μM Compound: ent-60, JTE-052	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	[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	[PMID: 32511913]
PBMC	IC₅₀	0.04 μM Compound: ent-60, JTE-052	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	[PMID: 32511913]
PBMC	IC₅₀	0.084 μM Compound: ent-60, JTE-052	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	[PMID: 32511913]
PBMC	IC₅₀	0.3 μM Compound: ent-60, JTE-052	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	[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	[PMID: 32511913]
Sf9	IC₅₀	0.013 μM Compound: ent-60, JTE-052	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	[PMID: 32511913]
T-cell	IC₅₀	0.0089 μM Compound: ent-60, JTE-052	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	[PMID: 32511913]
T-cell	IC₅₀	8.9 nM Compound: 17	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	[PMID: 32120325]

In Vitro

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 K_i 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.

In Vivo

Delgocitinib decreases the IFN-γ production, but the potency of the 1-h prior administration is higher than that of the 6-h prior administration (ED₅₀=0.24 versus 1.3 mg/kg). In the administration from day 1, Delgocitinib prevents the development of hind paw swelling and histological changes of inflammatory cell infiltration and synovial cell hyperplasia. Delgocitinib inhibits radiographic and histological changes of bone destruction and cartilage destruction. In the administration from day 15, Delgocitinib decreases the paw swelling in a dose-dependent manner. In addition, Delgocitinib ameliorates the inflammatory cell infiltration, synovial cell hyperplasia, and cartilage/bone destructions in the histological and radiographic examinations at the end of the study^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial

Molecular Weight

310.35

Formula

C₁₆H₁₈N₆O

CAS No.

1263774-59-9

Appearance

Solid

Color

White to off-white

SMILES

O=C(N(C[C@@H]1C)[C@]21CN(C3=C(C=CN4)C4=NC=N3)CC2)CC#N

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Solvent & Solubility

In Vitro:

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.

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	3.2222 mL	16.1108 mL	32.2217 mL
5 mM	0.6444 mL	3.2222 mL	6.4443 mL
10 mM	0.3222 mL	1.6111 mL	3.2222 mL

View the 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.

Molarity Calculator
Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

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.

Protocol 1

Add each solvent one by one: 5% DMSO 40% PEG300 5% Tween-80 50% Saline
Solubility: ≥ 2.5 mg/mL (8.06 mM); Clear solution
Protocol 2

Add each solvent one by one: 5% DMSO 95% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (8.06 mM); Clear solution
Protocol 3

Add each solvent one by one: 1% DMSO 99% Saline
Solubility: ≥ 0.5 mg/mL (1.61 mM); Clear solution

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

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μL

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

DMSO +

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Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

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).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

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

Purity: 99.87%

Select Batch:

Data Sheet (278 KB) SDS (393 KB)

COA (248 KB) LCMS (94 KB)

Handling Instructions (2659 KB)

References

[1]. Tanimoto A, et al. Pharmacological properties of JTE-052: a novel potent JAK inhibitor that suppresses various inflammatory responses in vitro and in vivo. Inflamm Res. 2015 Jan;64(1):41-51. [Content Brief]

Cell Assay ^[1]	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]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration ^[1]	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]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
References	[1]. Tanimoto A, et al. Pharmacological properties of JTE-052: a novel potent JAK inhibitor that suppresses various inflammatory responses in vitro and in vivo. Inflamm Res. 2015 Jan;64(1):41-51. [Content Brief]

Complete Stock Solution Preparation Table

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

Delgocitinib Related Classifications

Inflammation/Immunology

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Delgocitinib1263774-59-9JTE-052JTE052JTE 052JAKJanus kinaseInhibitorinhibitorinhibit

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Delgocitinib (Synonyms: JTE-052)

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Other Forms of Delgocitinib:

Delgocitinib Related Antibodies

1 Publications Citing Use of MCE Delgocitinib

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References

Customer Review

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Complete Stock Solution Preparation Table

Delgocitinib Related Classifications

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