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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).
EMD534085
Catalog No. TQ0314Cas No. 858668-07-2
EMD534085 is an effective and selective mitotic kinesin-5 inhibitor (IC50: 8 nM).
| Pack Size | Price | Availability | Quantity |
|---|---|---|---|
| 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
Chemical Properties
| 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]. |
| 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 | |||||||||||||||||||||||||||||||
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(mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.Preparation method for in vivo formula: Take 50 μL DMSO main solution, add 300 μLPEG300 mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O mix well and clarify
main solution, add 300 μLPEG300 mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O mix well and clarifyFor Reference Only. Please develop an appropriate dissolution method based on your laboratory animals and route of administration.
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