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Description |
HI-TOPK-032 is a potent and selective TOPK inhibitor. In vitro, HI-TOPK-032 strongly suppressed TOPK kinase activity but had little effect on extracellular signal–regulated kinase 1 (ERK1), c-jun—NH2—kinase 1, or p38 kinase activities. HI-TOPK-032 also inhibited anchorage-dependent and -independent colon cancer cell growth by reducing ERK-RSK phosphorylation as well as increasing colon cancer cell apoptosis through regulation of the abundance of p53, cleaved caspase-7, and cleaved PARP. In vivo, administration of HI-TOPK-032 suppressed tumor growth in a colon cancer xenograft model. HI-TOPK-032 may be further developed as a potential therapeutic against colorectal cancer. The serine-threonine mitogen-activated protein kinase kinase family member T-LAK cell–originated protein kinase (TOPK/PBK) is heavily involved in tumor development, cancer growth, apoptosis, and inflammation |
Chemical Structure |
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Chemical Name |
N-(12-cyanoindolizino[2,3-b]quinoxalin-2-yl)thiophene-2-carboxamide |
SMILES Code |
O=C(C1=CC=CS1)NC2=CC3=C(C#N)C4=NC5=CC=CC=C5N=C4N3C=C2 |
Theoretical Analysis |
XingMo Cat#:XM731 Product Name:HI-TOPK-032 Synonyms:HI-TOPK-032 CAS#:487020-03-1 Chemical Formula:C₂₀H₁₁N₅OS Exact Mass:369.068 Molecular Weight:369.4 Purity:>98%
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Technical Data |
Purity:
>98% (or refer to the Certificate of Analysis)
Shipping Condition:
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition:
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility:
Soluble in DMSO, not in water
Shelf Life:
>2 years if stored properly
Drug Formulation:
This drug may be formulated in DMSO
Stock Solution Storage:
0 - 4 C for short term (days to weeks), or -20 C for long term (months).
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WARNING: This product is for research use only, not for human or veterinary use
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