2. Epigenetics Stem Cell/Wnt Protein Tyrosine Kinase/RTK JAK/STAT Signaling Apoptosis
  3. JAK Apoptosis
  4. JAK3 covalent inhibitor-2

JAK3 covalent inhibitor-2 (compound J1b) is a selective, orally potent JAK3 inhibitor (IC50=7.2 nM) with low toxicity, anti-inflammatory activity and good bioavailability.

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

JAK3 covalent inhibitor-2 Chemical Structure

JAK3 covalent inhibitor-2 Chemical Structure

CAS No. : 2664050-97-7

Size Stock
50 mg   Get quote  
100 mg   Get quote  
250 mg   Get quote  
Synthetic products have potential research and development risk.

* Please select Quantity before adding items.

This product is a controlled substance and not for sale in your territory.

JAK3 covalent inhibitor-2 Related Antibodies

Top Publications Citing Use of Products

View All JAK Isoform Specific Products:

View All Isoforms

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

JAK3 covalent inhibitor-2 (compound J1b) is a selective, orally potent JAK3 inhibitor (IC50=7.2 nM) with low toxicity, anti-inflammatory activity and good bioavailability[1].

IC50 & Target[1]

JAK3

7.2 nM (IC50)

In Vitro

JAK3 covalent inhibitor-2 shows low cytotoxicity among HEK293, LO2, chondrocytes and RAW264.7 with IC50s (72 h) of 86.82 μM (HEK293), 61.79 μM (LO2), >32 μM (chondrocytes) and >32 μM (RAW264.7) respectively[1].
JAK3 covalent inhibitor-2 (100 mM; 90 min) shows t1/2 of 13.1 min and 43.9 min in human and rat liver microsomes, respectively. And the clean rate of 132.5 mL/min/kg and mL/min/kg, resepectively[1].
JAK3 covalent inhibitor-2 ((0.125-8 μM; 48 h)) dose-dependently induces T lymphocytes apoptosis[1].

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

JAK3 covalent inhibitor-2 Related Antibodies

Apoptosis Analysis[1]

Cell Line: CD4+ T cells , CD8[1] T cells
Concentration: 0.125, 0.5, 1, 2, 4, 8 μM
Incubation Time: 48 h
Result: Dose-dependently led to apoptosis among CD4+ and CD8+ T cells
In Vivo

Anti-inflammatory activity: JAK3 covalent inhibitor-2 (30 mg/kg, p.o.; single dose) inhibited carrageenan-induced paw edema in ICR mice, with a rapid reduction in paw thickness in J1b-treated mice[1].
Toxicity: JAK3 covalent inhibitor-2 (2 g/kg, p.o.; single dose) Liver and kidney appeare to be similar to those of normal mice, no weight loss or other adverse effects are observed[1].
Pharmacokinetics: JAK3 covalent inhibitor-2 (5 mg/kg; p.o.), clearance (Cl) 7.37 l/h/kg, oral half-life (t1/2 = 3.77 h), and bioavailability (F = 31.69%)[1].

Pharmacokinetic parameters of compound JAK3 covalent inhibitor-2 in SD rats[1]

JAK3 covalent inhibitor-2 在SD大鼠体内的药代动力学分析[1]

Route Dose (mg/kg) Cmax (mg/L) tmax (h) t1/2 (h) AUC0-t (mg/L·h) V<, V/F (L/kg) Cl, Cl/F (L/h/kg) F (%)
i.v. 5 4497.32 0.08 2.63 2161.38 8.98 (V) 2.32V (Cl) 31.69
p.o. 5 501.8 0.25 3.77 684.87 39.89 (V/F) 7.37 (Cl/F) /

Treatment of arthritis: JAK3 covalent inhibitor-2 ( 60 mg/kg , p.o. once a day) in CIA model almost complete restoration of normal joint status is achieved, and no significant weight changes or other adverse effects are observed[1].

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

Animal Model: ICR mice [1]
Dosage: 30 mg/kg
Administration: p.o.
Result: Showed significant anti-inflammatory activity by oral administration.
Animal Model: C57BL/6 mice[1]
Dosage: 2 g/kg
Administration: p.o.
Result: Inhibited tumor growth. Livers and kidneys appeared to be similar to those of normal mice. No weight loss or other adverse effects were observed.
Animal Model: SD rats[1]
Dosage: 5 mg/kg
Administration: p.o
Result: JAK3 covalent inhibitor-2 had good intestinal absorption and oral bioavailability. Clearance rate (Cl) was 7.37 L/h/kg, oral half‐life (t1/2 = 3.77 h), F = 31.69%
Animal Model: CIA model mouse[1]
Dosage: JAK3 covalent inhibitor-2 (30 mg/kg), JAK3 covalent inhibitor-2 (60 mg/kg,) Tofacitinib（HY-40354） (30 mg/kg)
Administration: p.o.
Result: JAK3 covalent inhibitor-2 group at 60 mg/kg histopathological analysis showed that the joint had returned to almost normal conditions.
Molecular Weight

392.41

Formula

C20H20N6O3
CAS No.
SMILES

[O-][N+](C1=CC=CC(C2=CNC3=NC=NC(N4C[C@H](NC(C=C)=O)CCC4)=C32)=C1)=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
  • No file chosen (Maximum size is: 1024 Kb)
  • If you have published this work, please enter the PubMed ID.
  • Your name will appear on the site.

JAK3 covalent inhibitor-2 Related Classifications

  • Molarity Calculator

  • Dilution Calculator

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass   Concentration   Volume   Molecular Weight *
= × ×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
× = ×
C1   V1   C2   V2
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 covalent inhibitor-22664050-97-7JAKApoptosisJanus kinasecovalent inhibitorsJAK3rheumatoid arthritisselectivity，systemic immunosuppressionCIAInhibitorinhibitorinhibit

Your Recently Viewed Products:

Inquiry Online

Your information is safe with us. * Required Fields.

Product Name

  

Salutation

Applicant Name *

 

Email Address *

Phone Number *

 

Organization Name *

Department *

 

Requested quantity *

Country or Region *

      

Remarks

Bulk Inquiry

Inquiry Information

Product Name:
JAK3 covalent inhibitor-2
Cat. No.:
HY-161354
Quantity:
MCE Japan Authorized Agent:

Customer Review

Thank You for Your Feedback!

Request for HNMR Report

Please fill out this form to request the QC report. We will send it to your Email address shortly.

Your information is safe with us. * Required Fields.

Product Name

  

Lot #

Applicant Name *

 

Email Address *

Phone Number

 

Department *

Organization Name *

 

Country or Region *

Remarks

Request for HNMR Report

We have received your request and will respond to you as soon as possible.