HI-TOPK-032

SKU: orb1308229

Description

HI-TOPK-032 is a potent and selective small-molecule inhibitor of the TOPK kinase. It is a valuable research tool for studying TOPK's role in cancer cell proliferation and has demonstrated utility in both in vitro assays and in vivo xenograft models.

Research Area

Cancer Biology, Signal Transduction

Key Properties

• CAS Number: 487020-03-1
• MW: 369.4
• Purity: 98.69% (May vary between batches)
• Formula: C₂₀H₁₁N₅OS
• SMILES: O=C(Nc1ccn2c(c1)c(C#N)c1nc3ccccc3nc21)c1cccs1
• Target: TOPK
• Solubility: DMSO:3.7 mg/mL (10.02 mM)

Bioactivity

• In Vivo:
  HI-TOPK-032 (1 or 10 mg/kg; mice) treatment, obviously inhibits HCT-116 tumor growth by more than 60% relative to the vehicle-treated group. Mice are well tolerated with HI-TOPK-032 treatment. The expression of p53 is strongly caused, and phosphorylation of ERK and RSK, a direct downstream protein of ERK. Which is markedly inhibited in the HI-TOPK-032-treated group.
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• In Vitro:
  HI-TOPK-032 effectively suppresses both anchorage-dependent and independent growth of colon cancer cells by diminishing ERK-RSK phosphorylation and promoting apoptosis, evidenced by increased levels of p53, cleaved caspase-7, and cleaved PARP. At its highest concentration (5 μM), it also reduces MEK1 activity by 40%, showcasing its potency. While it significantly inhibits TOPK kinase activity, its impact on ERK1, c-jun-NH2-kinase 1, and p38 kinase activities remains minimal. The compound adeptly binds to the ATP-binding site of TOPK, forming hydrogen bonds with GLY83 and ASP151, and engaging in hydrophobic interactions with LYS30, highlighting its specificity and effective mechanism of action.
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Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

inhibit, Inhibitor, HI-TOPK 032, HITOPK032, HI-TOPK032, HI-TOPK-032, HI TOPK 032, TOPK

Compound Identifiers

PubChem CID

1936439