10mM in DMSO for sensitive chromatographic and analytical workflows requiring minimal baseline interference.
Store at -80°C Ships Dry ice packs + Cold packs Check lot-specific COA for exact specifications.
SDS, COA, datasheet, and spec sheet available for download. Lot-specific COA accessible via lot number lookup.
Cited in 0 peer-reviewed publications across chromatography, organic synthesis, and cross-coupling reactions.
EMD534085 is a potent and selective inhibitor of the mitotic kinesin-5 with an IC 50 of 8 nM.
In Vitro
EMD 534085 does not inhibit any other tested kinesins (BimC, CEN-PE, Chromokinesin, KHC, KIF3C, KIFC3, MKLP-1, and MCAK) at 1 μM or 10 μM concentration, showing selectively over kinesin-5. EMD 534085 binds to the allosteric pocket of kinesin-5. 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. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
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\nreduction without toxic side effects . MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Cell Assay
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. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
IC50& Target:Kinesin-5 8 nM (IC 50 )
| 異性体SMILES | CN(C)CCNC(=O)NC[C@H]1CC[C@H]2[C@@H](NC3=C([C@H]2O1)C=C(C=C3)C(F)(F)F)C4=CC=CC=C4 |
|---|---|
| 代替CAS番号 | 1035647-06-3,858668-07-2 |
| PubChem CID | 23634407 |
| MeSH用語 | EMD 534085;EMD-534085;EMD534085 |
| 分子量 | 476.53 |
Comprehensive hazard, handling, storage, and regulatory compliance document.
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