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JAK3-IN-11

Catalog No. T9811 CAS 2412734-00-8

JAK3-IN-11 (Compound 12) exhibits potent, noncytotoxic, irreversible, orally active JAK3 inhibitory activity (IC50 = 1.7 nM) with an excellent selectivity profile (<588-fold compared to other JAK isoforms), covalently binds to the ATP-binding pocket in JAK3. JAK3-IN-11 strongly inhibits JAK3-dependent signaling and T-cell proliferation which is a promising tool for studying autoimmune diseases [1].

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JAK3-IN-11, CAS 2412734-00-8

Pack Size	Availability	Price/USD
25 mg	10-14 weeks	$ 1,520.00
50 mg	10-14 weeks	$ 1,980.00
100 mg	10-14 weeks	$ 2,500.00

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This compound is a customized synthesis product. We have a strong synthesis team with excellent synthesis technology and capabilities. However, due to various objective factors, there is a low probability that the synthesis will not be successful. If you need to learn more, please feel free to consult us, we will serve you wholeheartedly.

Biological Description

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Description	JAK3-IN-11 (Compound 12) exhibits potent, noncytotoxic, irreversible, orally active JAK3 inhibitory activity (IC50 = 1.7 nM) with an excellent selectivity profile (>588-fold compared to other JAK isoforms), covalently binds to the ATP-binding pocket in JAK3. JAK3-IN-11 strongly inhibits JAK3-dependent signaling and T-cell proliferation which is a promising tool for studying autoimmune diseases [1].
In vitro	JAK3-IN-11 (Compound 12) demonstrates no significant cytotoxic effects at a concentration of 10 μM over 72 hours. It exhibits potent suppression of T cell proliferation, with IC 50 values of 0.83 μM and 0.77 μM under anti-CD3/CD28 and IL-2 stimulation respectively, indicating strong immunosuppressive activity through selective inhibition of JAK3. Additionally, JAK3-IN-11 inhibits IL-2 or IL-15-induced phosphorylation of STAT5 in a dose-dependent manner within 1 hour, ranging from 0-10 μM. This compound notably binds covalently and irreversibly to JAK3, highlighting its targeted action on this kinase. The observed effects were supported by cell proliferation assays using mouse T cells and Western blot analysis for phosphorylation status, underscoring the compound's effectiveness in modulating relevant immune pathways.
In vivo	JAK3-IN-11 (Compound 12) effectively inhibits oxazolone (OXZ)-induced delayed-type hypersensitivity (DTH) in Balb/c mice in a dose-dependent manner, administered orally at doses of 0-30 mg/kg before and throughout a 6-day challenge phase. This compound was tested in an animal model specifically designed to induce DTH responses with OXZ. The study observed varying doses of 30, 10, and 3 mg/kg showing a dose-dependent reduction in DTH responses. Additionally, in male ICR mice, preliminary pharmacokinetic analysis of JAK3-IN-11 was conducted, demonstrating significant data following oral gavage and intravenous administration at doses of 30 mg/kg and 10 mg/kg, respectively. Key pharmacokinetic parameters were measured, including area under the concentration-time curve (AUC(0-t) and AUC(0-∞)), mean residence time (MRT), steady-state volume (Vz), plasma clearance (CLz), terminal half-life (t 1/2), peak plasma concentrations (C max), and bioavailability, revealing insights into the compound's absorption, distribution, metabolism, and excretion properties.

Molecular Weight	401.46
Formula	C23H23N5O2
CAS No.	2412734-00-8

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Powder: -20°C for 3 years | In solvent: -80°C for 1 year

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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

JAK3-IN-11 2412734-00-8 JAK-3-IN-11 JAK3IN11 JAK3 IN 11 inhibitor inhibit

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