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HI-TOPK-032

Catalog No. T15481 CAS 487020-03-1

HI-TOPK-032 is an effective and specific inhibitor of TOPK.

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HI-TOPK-032, CAS 487020-03-1

Pack Size	Availability	Price/USD
2 mg	In stock	$ 39.00
5 mg	In stock	$ 63.00
10 mg	In stock	$ 94.00
25 mg	In stock	$ 198.00
50 mg	In stock	$ 337.00
100 mg	In stock	$ 579.00
1 mL * 10 mM (in DMSO)	In stock	$ 68.00

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Purity: 98.69%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	HI-TOPK-032 is an effective and specific inhibitor of TOPK.
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.
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.

Molecular Weight	369.4
Formula	C20H11N5OS
CAS No.	487020-03-1

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 7 mg/mL (18.94 mM)

References and Literature

1. Kim DJ, et al. Novel TOPK inhibitor HI-TOPK-032 effectively suppresses colon cancer growth. Cancer Res. 2012 Jun 15;72(12):3060-8.

Related compound libraries

This product is contained In the following compound libraries：

Kinase Inhibitor Library Inhibitor Library Anti-Aging Compound Library Anti-Prostate Cancer Compound Library HIF-1 Signaling Pathway Compound Library MAPK Inhibitor Library Immunology/Inflammation Compound Library Bioactive Compounds Library Max Anti-Colorectal Cancer Compound Library Anti-Ovarian Cancer Compound Library

Related Products

Related compounds with same targets

OTS964 hydrochloride OTS514 hydrochloride Ilaprazole sodium Cephradine Ilaprazole OTS514

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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO (Master liquid concentration mg/mL)，Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

Method for preparing in vivo formulation：Take μL DMSO master liquid, next add μL PEG300， mix and clarify, next add μL Tween 80，mix and clarify, next add μL ddH₂O, mix and clarify.

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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

HI-TOPK-032 487020-03-1 MAPK TOPK HITOPK032 inhibit HI TOPK 032 HI-TOPK032 HI-TOPK 032 Inhibitor inhibitor

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