A KDM2/7 inhibitor (IC50s = 6.8

TC-E 5002 – 1 mg

Brand:
Cayman
CAS:
1453071-47-0
Storage:
-20
UN-No:
Non-Hazardous - /

TC-E 5002 is an inhibitor of the histone lysine demethylase (KDM) subfamily KDM2/7 (IC50s = 6.8, 0.2, and 1.2 µM for KDM2A, KDM7A, and KDM7B, respectively).{39306} It is selective for the KDM2/7 subfamily over KDM4A, KDM4C, KDM5A, and KDM6A/UTX (IC50s = >120, 83, 55, and 100 µM, respectively). It inhibits the growth of N2a, KYSE150, and HeLa cells with GI50 values of 86, 16, and 40 µM, respectively, which are in the range where it increases H3K27me2 levels in KYSE150 and HeLa cells. TC-E 5002 decreases gene expression of E2F1, a transcription factor activated by KDM7B that leads to progression of the cell cycle. In addition, TC-E 5002 treatment leads to cell cycle arrest at the G0/G1 phase in KYSE150 and HeLa cells.  

 

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Description

A KDM2/7 inhibitor (IC50s = 6.8, 0.2, and 1.2 µM for KDM2A, KDM7A, and KDM7B, respectively); selective for the KDM2/7 subfamily over KDM4A, KDM4C, KDM5A, and KDM6A/UTX (IC50s = >120, 83, 55, and 100 µM, respectively); inhibits growth of N2a, KYSE150, and HeLa cells (GI50s = 86, 16, and 40 µM, respectively); increases H3K27me2 levels, decreases gene expression of E2F1, and leads to cell cycle arrest in the G0/G1 phase in vitro,,

Formal name: N-(9-cyclopropyl-1-oxononyl)-N-hydroxy-β-alanine

Synonyms: 

Molecular weight: 285.4

CAS: 1453071-47-0

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Small Molecule Inhibitors|Demethylases||Research Area|Cancer|Cell Cycle|G1||Research Area|Cancer|Transcription Factors

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