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EMD534085 - 10mM in DMSO, high purity , CAS No.858668-07-2(DMSO)

  • 10mM in DMSO
Item Number
E654521
Grouped product items
SKUSizeAvailabilityPrice Qty
E654521-1ml
1ml
Available within 8-12 weeks(?)
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$237.90

Basic Description

Specifications & Purity10mM in DMSO
Biochemical and Physiological MechanismsEMD534085 is a potent and selective inhibitor of the mitotic kinesin-5 with an IC 50 of 8 nM.
Storage TempStore at -80°C
Shipped InIce chest + Ice pads
Product Description

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 )

Associated Targets(Human)

KIF11 Tchem Kinesin-like protein KIF11 (1 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

Names and Identifiers

Canonical SMILES CN(C)CCNC(=O)NCC1CCC2C(NC3=C(C2O1)C=C(C=C3)C(F)(F)F)C4=CC=CC=C4
Molecular Weight 476.53

Certificates

C of A & Other Certificates(BSE/TSE, COO)

Related Documents

Solution Calculators