A DYRK1B inhibitor (IC50 = 17 nM) that demonstrates 5-fold and 110-fold selectivity against the related family members DYRK1A and DYRK2

AZ191 – 5 mg

Brand:
Cayman
CAS:
1594092-37-1
Storage:
-20
UN-No:
Non-Hazardous - /

Dual-specificity tyrosine-(Y)-phosphorylation regulated kinase 1B (DYRK1B) belongs to a family of nuclear-localized protein kinases and participates in the regulation of the cell cycle with key roles in proliferation and differentiation.{28991} It is upregulated in solid tumors and gain-of-function mutations in the gene encoding this kinase have been linked to metabolic syndrome.{28992,26374} AZ191 is a cell-permeable azaindole that inhibits the serine/threonine kinase activity of DYRK1B (IC50 = 17 nM) with 5-fold and 110-fold selectivity against the related family members DYRK1A and DYRK2, respectively.{28993} This compound has been used as a probe to elucidate the mechanism of DYRK1B regulation of cell cycle progression.{28993}  

 

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Description

A DYRK1B inhibitor (IC50 = 17 nM) that demonstrates 5-fold and 110-fold selectivity against the related family members DYRK1A and DYRK2, respectively; used as a probe to elucidate the mechanism of DYRK1B regulation of cell cycle progression

Formal name: N-​[2-​methoxy-​4-​(4-​methyl-​1-​piperazinyl)​phenyl]​-​4-​(1-​methyl-​1H-​pyrrolo[2,​3-​c]​pyridin-​3-​yl)​-2-​pyrimidinamine

Synonyms: 

Molecular weight: 429.5

CAS: 1594092-37-1

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Kinase Inhibitors|Other Non-Receptor Tyrosine Kinases||Product Type|Biochemicals|Kinase Inhibitors|Other Serine/Threonine Kinases||Product Type|Biochemicals|Small Molecule Inhibitors|Kinases||Research Area|Cell Biology|Cell Cycle

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