2. Epigenetics Stem Cell/Wnt Protein Tyrosine Kinase/RTK JAK/STAT Signaling Apoptosis
  3. JAK STAT Apoptosis
  4. JAK3-IN-20

JAK3-IN-20 is a selective and orally active JAK3 inhibitor with an IC50 of 0.7473 nM. JAK3-IN-20 forms a covalent bond with JAK3 Cys909, outcompetes ATP for catalytic site binding, and blocks JAK-STAT pathway activation. JAK3-IN-20 inhibits migration, proliferation, and tumor growth of Bortezomib (HY-10227)-resistant cancer cells. JAK3-IN-20 induces dose-dependent apoptosis. JAK3-IN-20 can be used for the research of Bortezomib-resistant multiple myeloma.

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

JAK3-IN-20

JAK3-IN-20 Chemical Structure

CAS No. : 3104109-31-8

Size Stock
50 mg   Get quote  
100 mg   Get quote  
250 mg   Get quote  

* Please select Quantity before adding items.

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

JAK3-IN-20 Related Antibodies

Top Publications Citing Use of Products

View All JAK Isoform Specific Products:

View All Isoforms
JAK1 JAK2 JAK3 Tyk2 JAK

View All STAT Isoform Specific Products:

View All Isoforms
STAT3 STAT5 STAT6 STAT1

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

JAK3-IN-20 is a selective and orally active JAK3 inhibitor with an IC50 of 0.7473 nM. JAK3-IN-20 forms a covalent bond with JAK3 Cys909, outcompetes ATP for catalytic site binding, and blocks JAK-STAT pathway activation. JAK3-IN-20 inhibits migration, proliferation, and tumor growth of Bortezomib (HY-10227)-resistant cancer cells. JAK3-IN-20 induces dose-dependent apoptosis. JAK3-IN-20 can be used for the research of Bortezomib-resistant multiple myeloma[1].

IC50 & Target[1]

JAK3

0.7473 nM (IC50)

In Vitro

JAK3-IN-20 (Compound 7n) (60 min) potently inhibits purified JAK3 protein with an IC50 of 0.7473 nM[1].
JAK3-IN-20 (5 nM) shows high selectivity for JAK3, with 96.87% inhibition at 5 nM, and only moderate inhibition of JAK2 and TYK2, with no significant activity against JAK1[1].
JAK3-IN-20 (72 h) potently inhibits proliferation of Bortezomib (HY-10227)-resistant KM3 multiple myeloma cells with an IC50 of 0.245 μM, and also inhibits proliferation of KM3, BaF3-JAK3, Raji, Paca-02, H1975, HK-2, and LX-2 cells with IC50 values of 0.211-4.317 μM[1].
JAK3-IN-20 (0.3125-5.0 μM; 48 h) induces dose-dependent apoptosis and G2/M phase arrest in Bortezomib-resistant KM3 multiple myeloma cells[1].
JAK3-IN-20 (78.13-312.5 nM; 48 h) dose-dependently inhibits migration of Bortezomib-resistant KM3 multiple myeloma cells[1].
JAK3-IN-20 (0.3125-5.0 μM; 48 h) dose-dependently upregulates pro-apoptotic Bax protein and downregulates anti-apoptotic Bcl-2 protein in Bortezomib-resistant KM3 multiple myeloma cells[1].
JAK3-IN-20 (15.6 nM-4 μM; 1-72 h) dose-dependently inhibits STAT5 phosphorylation in Bortezomib-resistant KM3 multiple myeloma cells[1].

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

JAK3-IN-20 Related Antibodies

Apoptosis Analysis[1]

Cell Line: Bortezomib-resistant KM3 multiple myeloma cells
Concentration: 0.3125, 1.25, 5.0 μM
Incubation Time: 48 h
Result: At 0.3125 μM, a small proportion of apoptotic cells (orange-stained nuclei) were observed.
At 1.25 μM, the proportion of apoptotic cells increased
At 5.0 μM, numerous advanced apoptotic cells with cracked nuclei were observed.
Confirmed chromatin condensation and nuclear disintegration across all tested concentrations via DAPI staining.

Western Blot Analysis[1]

Cell Line: Bortezomib-resistant KM3 multiple myeloma cells
Concentration: 15.6, 62.5, 250 nM, 1, 4 μM (24 h); 250 nM (1, 12, 24, 48, 72 h)
Incubation Time: 1, 12, 24, 48, 72 h
Result: At 250 nM, p-STAT5 expression decreased; inhibition increased in a dose-dependent manner, with further decreased p-STAT5 expression at 4 μM.
Showed maximal inhibition of p-STAT5 at 12 h, with gradual recovery of phosphorylation by 24 h in time-course analysis.
Parmacokinetics
Species Dose Route AUC0-t AUC0-∞ MRT0-t MRT0-∞ Cmax F
Rat[1] 3 mg/kg i.v. 762.2 μg/L·h 785.5 μg/L·h 3.592 h 4.410 h 916.5 μg/L /
Rat[1] 30 mg/kg p.o. 3025 μg/L·h 3072 μg/L·h 7.478 h 7.812 h 306.8 μg/L 39.11 %
In Vivo

JAK3-IN-20 (Compound 7n) (60 mg/kg; I.g.,; daily; 21 days) provides superior tumor growth inhibition in a Bortezomib (HY-10227)-resistant multiple myeloma xenograft model, with no significant body weight loss[1].

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

Animal Model: NYG nude mice with KM3 cells (Bortezomib-
resistant) xenograft (~6 weeks old, ~20 g)[1]
Dosage: 60 mg/kg
Administration: p.o.; daily; 21 days
Result: Reduced tumor volume significantly lower than normal saline control and 60 mg/kg Tofacitinib (HY-40354) group on study day 21.
Caused no significant loss of body weight.
Molecular Weight

499.01

Formula

C24H31ClN8O2
CAS No.
SMILES

C=CC(N1CCCC(C1)COC2=NC(NC3=CN(N=C3)C4CCN(CC4)C)=NC5=C2C(Cl)=CN5)=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-IN-20 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-IN-203104109-31-8JAKSTATApoptosisJanus kinaseATPbortezomib-resistant cancer cellsJAK-STAT pathwaySTAT5KM3 cellsmultiple myelomaJAK3Raji cellsCys909BaF3-JAK3 cellsInhibitorinhibitorinhibit

Your Recently Viewed Products:

Inquiry Online

Your information is safe with us. * Required Fields.

Product Name

  

Requested Quantity *

Applicant Name *

 

Salutation

Email Address *

 

Phone Number *

Department

 

Organization Name *

City

State

Country or Region *

      

Remarks

Bulk Inquiry

Inquiry Information

Product Name:
JAK3-IN-20
Cat. No.:
HY-182314
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

SAFETY DATA SHEET (SDS)

Request for HNMR Report

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