A flavonol that selectively inhibits Pim-1 (IC50 = 0.34 µM) compared to Pim-2

Quercetagetin – 1 mg

Brand:
Cayman
CAS:
90-18-6
Storage:
-20
UN-No:
Non-Hazardous - /

The proto-oncogene serine/threonine-protein kinases, Pim-1 and Pim-2, are enzymes involved in cytokine signaling and participate in various signal transduction pathways, including cell growth, differentiation, and apoptosis. Their overexpression has been implicated in prostate cancer, some forms of leukemia, and lymphoma. Quercetagetin is a flavonol that inhibits Pim-1 with an IC50 value of 0.34 µM.{30314} It is selective for Pim-1, inhibiting Pim-2, PKA, RSK2, and JNK with IC50 values of 3.45, 21.2, 2.82, and 4.6 µM, respectively.{30314,30313} Quercetagetin has been shown to inhibit Pim-1 activity in intact RWPE2 prostate cancer cells with an ED50 value of 5.5 µM, which led to significant growth inhibition.{30314} It can also inhibit the growth of additional prostate epithelial cell lines at a potency proportionate to their respective level of Pim-1 protein.{30314}  

 

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Description

A flavonol that selectively inhibits Pim-1 (IC50 = 0.34 µM) compared to Pim-2, PKA, RSK2, and JNK (IC50s = 3.45, 21.2, 2.82, and 4.6 µM, respectively); inhibits Pim-1 activity in intact RWPE2 prostate cancer cells (ED50 = 5.5 µM) significantly inhibiting their growth

Formal name: 2-(3,4-dihydroxyphenyl)-3,5,6,7-tetrahydroxy-4H-1-benzopyran-4-one

Synonyms:  6-hydroxy Quercetin|NSC 115916

Molecular weight: 318.2

CAS: 90-18-6

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Kinase Inhibitors|PIMs||Product Type|Biochemicals|Natural Products|Flavonoids||Product Type|Biochemicals|Small Molecule Inhibitors|Kinases||Research Area|Cancer|Cell Signaling|PIM Signaling||Research Area|Cell Biology|Cell Signaling

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