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EMD534085

Catalog No. TQ0314 CAS 858668-07-2

EMD534085 is an effective and selective mitotic kinesin-5 inhibitor (IC50: 8 nM).

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EMD534085, CAS 858668-07-2

Pack Size	Availability	Price/USD
500 μg	35 days	$ 98.00
1 mg	35 days	$ 180.00
5 mg	35 days	$ 788.00
10 mg	35 days	$ 1,370.00

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Biological Description

Chemical Properties

Storage & Solubility Information

Description	EMD534085 is an effective and selective mitotic kinesin-5 inhibitor (IC50: 8 nM).
Targets&IC50	Kinesin-5:8 nM
In vitro	EMD 534085 does not inhibit any other tested kinesins at 1 μM or 10 μM concentration, showing selectively over kinesin-5. EMD 534085 binds to the allosteric pocket of kinesin-5 [1]. EMD534085 induces rapid cell death in HL60 during mitotic arrest. Caspase-8, ?9, ?3, ?7 are activated; Parp1 is cleaved; Mcl1 and XIAP are degraded in EMD534085-treated HL60 cells. EMD534085 treated HL60 cells also show significantly accumulated phospho-histone H3 level starting at 6 hrs post thymidine release [2].
In vivo	In a pharmacokinetic study of EMD 534085 conducted at a low dose in mice, average clearance was observed at 1.8 L/h/kg, with a volume of distribution of 7.4 L/kg and a half-life approximately 2.5 hours. High dose experiments (>10 mg/kg) consistently demonstrated a bioavailability exceeding 50% in mice. Intraperitoneal administration of EMD 534085 resulted in significant systemic exposure, contributing to a notable reduction in tumor growth without inducing toxic side effects [1].
Cell Research	Epithelial cell lines HeLa and MCF7 are synchronized in G2-phase using RO-3306. Cells are treated with 10 μM RO-3306 for 16 hrs, and then are ished and released to either warm growth medium or medium supplemented with 500 nM EMD534085 [2].

Molecular Weight	476.53
Formula	C25H31F3N4O2
CAS No.	858668-07-2

Storage

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

Solubility Information

DMSO: 25 mg/mL (52.46 mM)

References and Literature

1. Schiemann K, et al. The discovery and optimization of hexahydro-2H-pyrano[3,2-c]quinolines (HHPQs) as potent and selective inhibitors of the mitotic kinesin-5. Bioorg Med Chem Lett. 2010 Mar 1;20(5):1491-5. 2. Tang Y, et al. Rapid induction of apoptosis during Kinesin-5 inhibitor-induced mitotic arrest in HL60 cells. Cancer Lett. 2011 Nov 1;310(1):15-24.

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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

EMD534085 858668-07-2 Cytoskeletal Signaling Kinesin EMD-534085 EMD 534085 inhibitor inhibit

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