TCS 21311

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Cat.No. 4221 - TCS 21311 | C27H25F3N4O4 | CAS No. 1260181-14-3
Description: Potent JAK3 inhibitor. Also inhibits GSK-3β and PKC
Alternative Names: NIBR3049
Chemical Name: 3-[5-[4-(2-Hydroxy-2-methyl-1-oxopropyl)-1-piperazinyl]-2-(trifluoromethyl)phenyl]-4-(1H-indol-3-yl)-1H-pyrrole-2,5-dione
Purity: ≥98% (HPLC)
Datasheet
Citations
Literature
Pathways

Biological Activity

Potent JAK3 inhibitor (IC50 = 8 nM). Selective for JAK3 over JAK1, JAK2 and TYK2 (IC50 values are 1017, 2550 and 8055 nM respectively). Also inhibits GSK-3β, PKCα and PKCθ (IC50 values are 3, 13 and 68 nM respectively).

Compound Libraries

TCS 21311 is also offered as part of the Tocriscreen Plus and Tocriscreen Kinase Inhibitor Toolbox II. Find out more about compound libraries available from Tocris.

Technical Data

M. Wt 526.51
Formula C27H25F3N4O4
Storage Desiccate at RT
Purity ≥98% (HPLC)
CAS Number 1260181-14-3
PubChem ID 50925411
InChI Key CLGRAWDGLMENOD-UHFFFAOYSA-N
Smiles O=C(N1)C(C3=CNC4=C3C=CC=C4)=C(C2=C(C(F)(F)F)C=CC(N5CCN(C(C(O)(C)C)=O)CC5)=C2)C1=O

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

All Tocris products are intended for laboratory research use only.

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 52.65 100

Preparing Stock Solutions

The following data is based on the product molecular weight 526.51. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.9 mL 9.5 mL 18.99 mL
5 mM 0.38 mL 1.9 mL 3.8 mL
10 mM 0.19 mL 0.95 mL 1.9 mL
50 mM 0.04 mL 0.19 mL 0.38 mL

Molarity Calculator

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Reconstitution Calculator

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Dilution Calculator

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Product Datasheets

Safety Datasheet

References

References are publications that support the products' biological activity.

Thoma et al (2010) Identification of a potent Janus kinase 3 inhibitor with high selectivity within the Janus kinase family. J.Med.Chem. 54 284 PMID:


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View Related Products by Product Action

View all JAK Kinase Inhibitors

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Citations for TCS 21311

Citations are publications that use Tocris products.

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Reviews

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Literature in this Area

Cancer

Cancer Research Product Guide

A collection of over 750 products for cancer research, the guide includes research tools for the study of:

  • Cancer Metabolism
  • Epigenetics in Cancer
  • Receptor Signaling
  • Cell Cycle and DNA Damage Repair
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Immunology Product Listing

A collection of over 190 products for immunology research, the guide includes research tools for the study of:

  • Chemokine and Cytokine Signaling
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Kinases

Kinases Product Listing

A collection of over 400 products for kinase research, the listing includes inhibitors of:

  • Receptor Tyrosine Kinases
  • Protein Kinases A, C, D and G
  • PI-3 Kinase, Akt and mTOR
  • MAPK Signaling
  • Receptor Serine/Threonine Kinases

Pathways for TCS 21311

JAK-STAT

JAK-STAT Signaling Pathway

The JAK-STAT signaling pathway has several roles, including the control of cell proliferation and hematopoiesis. It is the main signal transduction cascade from cytokine receptors.

Protocols

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