1. Immunology/Inflammation
    Protein Tyrosine Kinase/RTK
  2. IRAK
  3. HG-12-6

HG-12-6 

Cat. No.: HY-123956
Handling Instructions

HG-12-6 is a type II inhibitor of IRAK4. HG-12-6 shows preferential binding to unphosphorylated inactive IRAK4 with an IC50 of 165 nM. HG-12-6 can modulate IRAK4 activity in autoimmunity and inflammation.

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

HG-12-6 Chemical Structure

HG-12-6 Chemical Structure

CAS No. : 2222354-57-4

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Description

HG-12-6 is a type II inhibitor of IRAK4. HG-12-6 shows preferential binding to unphosphorylated inactive IRAK4 with an IC50 of 165 nM. HG-12-6 can modulate IRAK4 activity in autoimmunity and inflammation[1].

IC50 & Target[1]

IRAK4

165 nM (IC50, Unphosphorylated inactive IRAK4 )

IRAK4

2876 nM (IC50, Phosphorylated active IRAK4 )

In Vitro

The in-house compound HG-12-6 has a similar chemical scaffold as Ponatinib. The most differentiating components are the head of the inhibitor and the lack of a methyl substituent on ring A. Without the methyl substituent on ring A, the entire HG-12-6 molecule shifts inward to the ATP pocket in comparison with the binding mode of Ponatinib[1].
HG-12-6 has a better binding affinity for the unphosphorylated inactive IRAK4 kinase domain (IC50 of 165 nM) than the phosphorylated active IRAK4 kinase domain (IC50 of 2876 nM)[1].

Molecular Weight

580.62

Formula

C₂₉H₂₇F₃N₆O₂S

CAS No.

2222354-57-4

SMILES

O=C(NC1=CC=C(CN2CCNCC2)C(C(F)(F)F)=C1)C3=CC=CC(C4=CC=C5C(SC(NC(C6CC6)=O)=N5)=N4)=C3

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

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Keywords:

HG-12-6IRAKInterleukin-1 receptor associated kinaseIL-1R associated kinaseIRAK4IL-1unphosphorylatedautoimmunityinflammationvariableconformationsInhibitorinhibitorinhibit

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HG-12-6
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HY-123956
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