1. Cell Cycle/DNA Damage
    Cytoskeleton
  2. Kinesin
  3. EMD534085

EMD534085 

Cat. No.: HY-15000 Purity: 99.03%
Handling Instructions

EMD534085 is a potent and selective inhibitor of the mitotic kinesin-5 with an IC50 of 8 nM.

For research use only. We do not sell to patients.

EMD534085 Chemical Structure

EMD534085 Chemical Structure

CAS No. : 858668-07-2

Size Price Stock Quantity
10 mM * 1  mL in DMSO USD 283 In-stock
Estimated Time of Arrival: December 31
1 mg USD 90 In-stock
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5 mg USD 270 In-stock
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10 mg USD 450 In-stock
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25 mg USD 890 In-stock
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50 mg USD 1500 In-stock
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100 mg USD 2500 In-stock
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Based on 1 publication(s) in Google Scholar

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Description

EMD534085 is a potent and selective inhibitor of the mitotic kinesin-5 with an IC50 of 8 nM.

IC50 & Target[1]

Kinesin-5

8 nM (IC50)

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[1]. 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[2].

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[1].

Molecular Weight

476.53

Formula

C₂₅H₃₁F₃N₄O₂

CAS No.

858668-07-2

SMILES

O=C(NC[[email protected]]1CC[[email protected]@]2([H])[[email protected]](C3=CC=CC=C3)NC4=C(C=C(C(F)(F)F)C=C4)[[email protected]@]2([H])O1)NCCN(C)C

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : ≥ 26 mg/mL (54.56 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.0985 mL 10.4925 mL 20.9850 mL
5 mM 0.4197 mL 2.0985 mL 4.1970 mL
10 mM 0.2099 mL 1.0493 mL 2.0985 mL
*Please refer to the solubility information to select the appropriate solvent.
References
Cell Assay
[2]

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
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Keywords:

EMD534085EMD 534085EMD-534085KinesinInhibitorinhibitorinhibit

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EMD534085
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