EMD534085

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

Catalog No. TQ0314Cas No. 858668-07-2

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EMD534085

Catalog No. TQ0314Cas No. 858668-07-2

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

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Pack Size	Price	Availability
500 μg	$98	35 days
1 mg	$180	35 days
5 mg	$788	35 days
10 mg	$1,370	35 days

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Product Introduction

Bioactivity

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 other tested kinesins at 1 μM or 10 μM concentrations, showing selectivity for kinesin-5. EMD 534085 binds to the allosteric pocket of kinesin-5 [1]. It induces rapid cell death in HL60 cells during mitotic arrest, activating caspase-8, -9, -3, -7; cleaving Parp1; and degrading Mcl1 and XIAP. Additionally, EMD 534085-treated HL60 cells exhibit a significantly increased phospho-histone H3 level starting 6 hours 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].

Chemical Properties

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

Storage & Solubility Information

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.

Solubility Information

DMSO: 25 mg/mL (52.46 mM)

Solution Preparation Table

DMSO

	1mg	5mg	10mg	50mg
1 mM	2.0985 mL	10.4925 mL	20.9850 mL	104.9252 mL
5 mM	0.4197 mL	2.0985 mL	4.1970 mL	20.9850 mL
10 mM	0.2099 mL	1.0493 mL	2.0985 mL	10.4925 mL
20 mM	0.1049 mL	0.5246 mL	1.0493 mL	5.2463 mL
50 mM	0.0420 mL	0.2099 mL	0.4197 mL	2.0985 mL

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