1. Epigenetics
    Stem Cell/Wnt
    JAK/STAT Signaling
  2. JAK
  3. JAK3-IN-11

JAK3-IN-11 

Cat. No.: HY-146727
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JAK3-IN-11 (Compound 12), a potent, noncytotoxic, irreversible, orally active JAK3 inhibitor with IC50 value of 1.7 nM, has excellent selectivity (>588-fold compared to other JAK isoforms), covalently bind to the ATP-binding pocket in JAK3. JAK3-IN-11 strongly inhibits JAK3-dependent signaling and T cell proliferation, is a promising tool for study autoimmune diseases.

For research use only. We do not sell to patients.

JAK3-IN-11 Chemical Structure

JAK3-IN-11 Chemical Structure

CAS No. : 2412734-00-8

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Description

JAK3-IN-11 (Compound 12), a potent, noncytotoxic, irreversible, orally active JAK3 inhibitor with IC50 value of 1.7 nM, has excellent selectivity (>588-fold compared to other JAK isoforms), covalently bind to the ATP-binding pocket in JAK3. JAK3-IN-11 strongly inhibits JAK3-dependent signaling and T cell proliferation, is a promising tool for study autoimmune diseases[1].

IC50 & Target[1]

JAK3

1.7 nM (IC50)

JAK2

1 μM (IC50)

JAK1

1.32 μM (IC50)

In Vitro

JAK3-IN-11 (Compound 12) (10 μM, 72 h) has no obvious cytotoxicity at a concentration of 10 μM[1].
JAK3-IN-11 (Compound 12) (72 h) displays strong inhibition for T cell proliferation with IC50 values of 0.83 μM (anti-CD3/CD28 stimulation) and 0.77 μM (IL-2 stimulation)[1].
JAK3-IN-11 (Compound 12) (0-10 μM, 1h) abrogates IL-2 or IL-15-induced phosphorylation of STAT5 in a concentration-dependent manner[1].
JAK3-IN-11 (Compound 12) covalently binds to JAK3 and irreversibly inhibits JAK3[1].

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

Cell Proliferation Assay[1]

Cell Line: Mouse T cells in complete RPMI1640 medium then exposed to anti-CD3/anti-CD28 or IL-2.
Concentration:
Incubation Time: 72 h.
Result: Displayed strong inhibition for T cell proliferation with an IC50 values of 0.83 μM (anti-CD3/CD28 stimulation) and 0.77 μM (IL-2 stimulation), showed obvious significant immunosuppressive activity under selective inhibition of JAK3.

Western Blot Analysis[1]

Cell Line: Purified T cells were pre-activated coated with anti-CD3 and anti-CD28 for 72 h, then cultured with IL-2 (50 U/mL) for 36 h, then, cultured without IL-2 for 36 h
Concentration: 0.01, 0.1, 1, 10 μM.
Incubation Time: 1 h.
Result: Abrogated IL-2 or IL-15-induced phosphorylation of STAT5 in a concentration-dependent manner.
In Vivo

JAK3-IN-11 (Compound 12) (Oxazolone (OXZ)-induced DTH Balb/c mice; 0-30 mg/kg; PO, prior to and during the challenge phase, 6 days) inhibits oxazolone (OXZ)-induced delayed type hypersensitivity (DTH) responses in a dose-dependent manner[1].

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

Animal Model: Oxazolone (OXZ)-induced DTH Balb/c mice model[1].
Dosage: 30, 10, and 3 mg/kg.
Administration: PO, prior to and during the challenge phase, 6 days.
Result: Inhibited oxazolone (OXZ)-induced delayed type hypersensitivity (DTH) responses in a dose-dependent manner.
Animal Model: Male ICR mice[1].
Dosage: 30 mg/kg for oral gavage, 10 mg/kg for intravenous administration.
Administration: Pharmacokinetic Analysis
Result: Preliminary pharmacokinetic data of JAK3-IN-11 (Compound 12) in male ICR Mice[1]
Male ICR mice, 30 mg/kg for oral gavage, 10 mg/kg for intravenous administration[1].
Compound 12 iv (10 mg/kg) po (30 mg/kg)
AUC(0-t) (mg/L*h)a 1244.41 ± 77.83 889.42 ± 48.32
AUC(0-∞) (mg/L*h) 1274.41 ± 57.18 897.12 ± 56.72
MRT (0-∞) (h)b 0.73 ± 0.08 1.42 ± 0.38
Vz (L/kg)c 8.36 ± 1.83 220.42 ± 24.71
CLz (L/h/kg)d 8.15 ± 1.21 97.14 ± 20.87
t1/2 (h)e 0.47 ± 0.06 1.52 ± 0.34
Cmax (mg/L)f 8763.23 ± 324.65 2008.21 ± 189.44
Bioavailability(%)g 23.82%
a Area under the concentration time curve.
b Mean residence time.
c Volume in steady state.
d Plasma clearance.
e Terminal half-life.
f Peak plasma concentrations.
g Bioavailability = AUC0-t(po)/AUC0-t × 100%.
Molecular Weight

401.46

Formula

C23H23N5O2

CAS No.
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