JAK3-IN-11
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.
- CAS No.: 2412734-00-8
- Formula: C23H23N5O2
- Molecular Weight:401.46
-
Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
-
Biological Activity
-
Chemical Information
- Purity & Documentation
- References
-
Help & FAQs
Biological Activity
|
JAK3 1.7 nM (IC50) |
JAK2 1 μM (IC50) |
JAK1 1.32 μM (IC50) |
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
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.
-
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.
MedChemExpress (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].
a Area under the concentration time curve.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%
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%.
Chemical Information
-
CAS No. 2412734-00-8
-
Molecular Weight 401.46
-
Formula C23H23N5O2
-
SMILES
C=CC(NC1=CC=C(C=C1)C2=NC(NC3=CC=C(C=C3)N4CCOCC4)=NC=C2)=O
-
Shipping
Room temperature in continental US; may vary elsewhere.
-
Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
JAK3-IN-11 Related Classifications
HY-146727 Related Classifications
Powered by Bioz