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Delgocitinib

Catalog No. T15096 CAS 1263774-59-9

Synonyms: Corectim（Delgocitinib）, JTE-052

Delgocitinib is a potent and specific JAK inhibitor with an IC50 value of 2.8, 2.6, 13 and 58 nM against JAK1, JAK2, JAK3 and Tyk2. Delgocitinib is involved in a variety of inflammatory and autoimmune diseases through JAK-dependent cytokines and can be widely used in the treatment of various inflammatory diseases. Delgocitinib is the world's first JAK topical compound for the treatment of atopic dermatitis.

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Delgocitinib, CAS 1263774-59-9

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Purity: 98%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	Delgocitinib is a potent and specific JAK inhibitor with an IC50 value of 2.8, 2.6, 13 and 58 nM against JAK1, JAK2, JAK3 and Tyk2. Delgocitinib is involved in a variety of inflammatory and autoimmune diseases through JAK-dependent cytokines and can be widely used in the treatment of various inflammatory diseases. Delgocitinib is the world's first JAK topical compound for the treatment of atopic dermatitis.
Targets&IC50	Tyk2:58 nM, JAK1:2.8 nM, JAK2:2.6 nM, JAK3:13 nM
In vitro	Delgocitinib inhibits the phosphorylation of Stat proteins induced by IL-2, IL-6, IL-23, GM-CSF, and IFN-α (IC50: 40±9, 33±14, 84±11, 304±22 and 18±3 nM, respectively), in these cell-based cytokine signaling assays and it also inhibits IL-2-induced proliferation of T cells in a concentration-dependent manner (IC50: 8.9±3.6 nM). Its potency is similar to that of tofacitinib (IC50:16 nM). Delgocitinib effectively inhibits all of the JAK subtypes ( IC50: 2.8±0.6, 2.6±0.2, 13±0 and 58±9 nM for JAK1, JAK2, JAK3 and Tyk2, respectively), in the enzymatic assays. Lineweaver-Burk plots display that the inhibition mode of Delgocitinib toward all JAKs is competitive with ATP (Ki: 2.1±0.3, 1.7±0.0, 5.5±0.3 and 14±1 nM for JAK1, JAK2, JAK3 and Tyk2, respectively) [1].
In vivo	Delgocitinib inhibits radiographic and histological changes of bone destruction and cartilage destruction. Delgocitinib induces the IFN-γ production, however, the potency of the 1-h prior administration(ED50: 0.24 mg/kg) is higher than that of the 6-h prior administration (ED50: 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. In the administration from day 15, Delgocitinib decreases the paw swelling in a dose-dependent manner. 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].

Synonyms	Corectim（Delgocitinib）, JTE-052
Molecular Weight	310.35
Formula	C16H18N6O
CAS No.	1263774-59-9

Storage

Powder: -20°C for 3 years

In solvent: -80°C for 2 years

Solubility Information

DMSO: 50 mg/mL (161.11 mM)

( < 1 mg/ml refers to the product slightly soluble or insoluble )

References and Literature

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):41-5

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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

Delgocitinib 1263774-59-9 Angiogenesis Chromatin/Epigenetic JAK/STAT signaling Stem Cells Tyrosine Kinase/Adaptors JAK Tyrosine Kinases Corectim（Delgocitinib） JTE052 Inhibitor Janus kinase inhibit JTE 052 JTE-052 inhibitor

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