JAK3-IN-11

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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

CAS No. : 2412734-00-8

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Biological Activity
Purity & Documentation
References
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Description

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].

MedChemExpress (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].

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].

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
t_1/2(h)^e	0.47 ± 0.06	1.52 ± 0.34
C_max(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 = AUC_0-t(po)/AUC_0-t × 100%.

Molecular Weight

401.46

Formula

C₂₃H₂₃N₅O₂

CAS No.

2412734-00-8

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

Handling Instructions (2659 KB)

References

[1]. Lei Shu, et al. Design, synthesis, and pharmacological evaluation of 4- or 6-phenyl-pyrimidine derivatives as novel and selective Janus kinase 3 inhibitors. Eur J Med Chem. 2020 Apr 1;191:112148. [Content Brief]

JAK3-IN-11 Related Classifications

Inflammation/Immunology

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Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

JAK3-IN-112412734-00-8JAKJanus kinaseT cellRaw 264.7autoimmune diseasesInhibitorinhibitorinhibit

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