Skip to the beginning of the images gallery

Delgocitinib - 10mM in DMSO, high purity , CAS No.1263774-59-9(DMSO), Janus Kinase (JAK) inhibitor

COA

Grade & Purity:

Moligand™

10mM in DMSO

Cas Number: 1263774-59-9(DMSO)
Molecular Weight: 310.35

In stock

Item Number

D656664

Grouped product items
SKU	Size	Availability	Price	Qty
D656664-1ml	1ml	Available within 8-12 weeks(?) Production requires sourcing of materials. We appreciate your patience and understanding.	$444.90

View related series

Compound libraries (12325) Epigenetics (1496) JAK (149) JAK/STAT Signaling (507) Protein Tyrosine Kinase/RTK (1314) Stem Cell/Wnt (1019)

Basic Description

Specifications & Purity	Moligand™, 10mM in DMSO
Biochemical and Physiological Mechanisms	Delgocitinib (JTE-052) is a specific JAK inhibitor with IC 50 s of 2.8, 2.6, 13 and 58 nM for JAK1 , JAK2 , JAK3 and Tyk2 , respectively.
Storage Temp	Store at -80°C
Shipped In	Ice chest + Ice pads This product requires cold chain shipping. Ground and other economy services are not available.
Grade	Moligand™
Action Type	INHIBITOR
Mechanism of action	Janus Kinase (JAK) inhibitor
Product Description	Delgocitinib (JTE-052) is a specific JAK inhibitor with IC 50 s of 2.8, 2.6, 13 and 58 nM for JAK1 , JAK2 , JAK3 and Tyk2 , respectively In Vitro In the enzymatic assays, Delgocitinib potently inhibits all of the JAK subtypes with IC 50 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 IC 50 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 (IC 50 =8.9±3.6 nM), and its potency is similar to that of CP-690550 (IC 50 =16 nM). 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 (ED 50 =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 . MCE has not independently confirmed the accuracy of these methods. They are for reference only. IC50& Target:JAK2 2.6 nM (IC 50 ) JAK1 2.8 nM (IC 50 ) JAK3 13 nM (IC 50 ) Tyk2 58 nM (IC 50 )

Associated Targets(Human)

TYK2 Tclin Non-receptor tyrosine-protein kinase TYK2 (1 Activities)

Discover Target: TYK2

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

JAK3 Tclin Tyrosine-protein kinase JAK3 (1 Activities)

Discover Target: JAK3

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

JAK1 Tclin Tyrosine-protein kinase JAK1 (1 Activities)

Discover Target: JAK1

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

JAK2 Tclin Tyrosine-protein kinase JAK2 (1 Activities)

Discover Target: JAK2

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

Names and Identifiers

Smiles	CC1CN(C12CCN(C2)C3=NC=NC4=C3C=CN4)C(=O)CC#N
Molecular Weight	310.35

Certificates（CoA,COO,BSE/TSE and Analysis Chart)

C of A & Other Certificates(BSE/TSE, COO):

Analytical Chart:

Solution Calculators

Molarity Calculator

Determine the necessary mass, volume, or concentration for preparing a solution.

Mass

Concentration

Volume

M. Wt*

g/mol

*When preparing stock solutions, always use the batch-specific molecular weight of the product found on the vial label and the Certificate of Analysis (available online).

Dilution Calculator

Determine the dilution needed to prepare a stock solution.

Concentration 1 (C1)

Volume 1 (V1)

Concentration 2 (C2)

Volume 2 (V2)

Reconstitution Calculator

The reconstitution calculator enables you to quickly determine the volume of a reagent needed to reconstitute your vial. Just enter the mass of the reagent and the target concentration, and the calculator will do the rest.

Volume (to add to vial)

Mass (in vial)

Desired Reconstitution Concentration