An inhibitor of TOPK (IC50 = ~2 µM)

HI TOPK 032 – 5 mg

Brand:
Cayman
CAS:
487020-03-1
Storage:
-20
UN-No:
Non-Hazardous - /

HI TOPK 032 is an inhibitor of lymphokine-activated killer T cell-originated protein kinase (TOPK), blocking phosphorylation of the substrate histone H2AX with an IC50 value of ~2 µM and providing complete inhibition at 5 µM.{31844} It also inhibits checkpoint kinase 1 (Chk1; IC50 = 9.6 µM).{31845} In addition, HI TOPK 032 inhibits MEK1, achieving 40% inhibition at 5 µM, but it does not alter the activities of ERK1, JNK1, or p38 MAPK at 2 µM.{31844} HI TOPK 032 decreases the growth of colon cancer and glioma initiating cells in vitro and suppresses tumor growth in vivo.{31844,31843}  

 

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SKU: 19815 - Category:

Description

An inhibitor of TOPK (IC50 = ~2 µM), Chk1 (IC50 = 9.6 µM), and MEK1 (40% inhibition at 5 µM); decreases the growth of colon cancer and glioma initiating cells in vitro and suppresses tumor growth in vivo

Formal name: N-(12-cyanoindolizino[2,3-b]quinoxalin-2-yl)-2-thiophenecarboxamide

Synonyms: 

Molecular weight: 369.4

CAS: 487020-03-1

Purity: ≥95%

Formulation: A crystalline solid

Product Type|Biochemicals|Kinase Inhibitors|Checkpoint Kinases||Product Type|Biochemicals|Kinase Inhibitors|RAS/RAF/MEK/ERK/MAPK||Product Type|Biochemicals|Small Molecule Inhibitors|Kinases||Research Area|Cancer|Cell Cycle||Research Area|Cancer|Cell Signaling

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