NG 25

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Cat.No. 5429 - NG 25 | C29H30F3N5O2 | CAS No. 1315355-93-1
Description: TGF-β-activated kinase (TAK1) inhibitor
Chemical Name: N-[4-[(4-Ethyl-1-piperazinyl)methyl]-3-(trifluoromethyl)phenyl]-4-methyl-3-(1H-pyrrolo[2,3-b]pyridin-4-yloxy)benzamide
Purity: ≥98% (HPLC)
Datasheet
Citations
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Literature

Biological Activity

TGF-β-activated kinase (TAK1) inhibitor (IC50 = 149 nM). Also inhibits LYN, MAP4K2 and Abl kinase activity (IC50 values are 12.9, 21.7 and 75.2 nM, respectively). Suppresses CpG A and CpG B-stimulated secretion of IFN-α and TLR7/8 agonist CL097-stimulated secretion of IFN-β in Gen 2.2 leukemia cells in vitro.

Licensing Information

Sold under license from Dana-Farber Cancer Institute.

Technical Data

M. Wt 537.58
Formula C29H30F3N5O2
Storage Store at -20°C
Purity ≥98% (HPLC)
CAS Number 1315355-93-1
PubChem ID 53340664
InChI Key SMPGEBOIKULBCT-UHFFFAOYSA-N
Smiles CCN1CCN(CC2=C(C(F)(F)F)C=C(NC(C3=CC(OC4=CC=NC5=C4C=CN5)=C(C)C=C3)=O)C=C2)CC1

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 10.75 20

Preparing Stock Solutions

The following data is based on the product molecular weight 537.58. 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.

Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
0.2 mM 9.3 mL 46.5 mL 93.01 mL
1 mM 1.86 mL 9.3 mL 18.6 mL
2 mM 0.93 mL 4.65 mL 9.3 mL
10 mM 0.19 mL 0.93 mL 1.86 mL

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References

References are publications that support the biological activity of the product.

Tan et al (2015) Discovery of type II inhibitors of TGFβ-activated kinase 1 (TAK1) and mitogen-activated protein kinase kinase kinase kinase 2 (MAP4K2). J.Med.Chem. 58 183 PMID: 25075558

Pauls et al (2012) Essential role for IKKβ in production of type 1 interferons by plasmacytoid dendritic cells. J.Biol.Chem. 287 19216 PMID: 22511786

Dzamko et al (2012) The IkappaB kinase family phosphorylates the Parkinson's disease kinase LRRK2 at Ser935 and Ser910 during Toll-like receptor signaling. PLoS ONE 7 e39132 PMID: 22723946


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Keywords: NG 25, NG 25 supplier, NG25, TAK1, TGFbeta, TGFb, TGFβ, activated, kinases, inhibitors, inhibits, MAP4K2, LYN, Abl, Other, Kinases, 5429, Tocris Bioscience

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