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Cat. No. M8930
EMD534085 Structure
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10mg USD 400  USD400 In stock
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Quality Control & Documentation
Biological Activity

EMD534085 is a potent and selective inhibitor of the mitotic kinesin-5 with an IC50 of 8 nM. 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 shows significantly accumulated phospho-Histone H3 level starting at 6 hrs post thymidine release.

In vivo: In a low dose PK of EMD 534085 in mice the clearance is 1.8 L/h/kg on average, the volume of distribution is 7.4 L/kg and the half life around 2.5 h. The bioavailability in high dose experiments (>10 mg/kg) is always above 50% in mice. Intraperitonal administration of EMD 534085 enables significant systemic exposure in mice leading to a significant tumor growth reduction without toxic side effects.

Protocol (for reference only)
Cell Experiment
Cell lines Epithelial cell lines HeLa and MCF7
Preparation method 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.
Concentrations 500 nM
Incubation time
Animal Experiment
Animal models
Chemical Information
Molecular Weight 476.53
Formula C25H31F3N4O2
CAS Number 858668-07-2
Solubility (25°C) DMSO: ≥ 20 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.


[1] Orth JD, et al. Mol Biol Cell. Prolonged mitotic arrest triggers partial activation of apoptosis, resulting in DNA damage and p53 induction.

[2] Tang Y, et al. Cancer Lett. Rapid induction of apoptosis during Kinesin-5 inhibitor-induced mitotic arrest in HL60 cells.

[3] Schiemann K, et al. Bioorg Med Chem Lett. The discovery and optimization of hexahydro-2H-pyrano[3,2-c]quinolines (HHPQs) as potent and selective inhibitors of the mitotic kinesin-5.

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Keywords: EMD534085 supplier, Kinesin, inhibitors, activators

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