EMD534085

Name: EMD534085
Brand: MedChemExpress
SKU: HY-15000
Rating: 4.5 (1 reviews)

Cat. No.: HY-15000 Purity: 99.55%: FAQs
Data Sheet SDS COA Handling Instructions

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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

CAS No. : 858668-07-2

Size	Price	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 283	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 283	In-stock	Estimated Time of Arrival: December 31
Solid
1 mg	USD 90	In-stock	Estimated Time of Arrival: December 31
5 mg	USD 270	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 450	In-stock	Estimated Time of Arrival: December 31
25 mg	USD 890	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 1500	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 2500	In-stock	Estimated Time of Arrival: December 31
200 mg		Get quote
500 mg		Get quote

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Customer Review

Based on 1 publication(s) in Google Scholar

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View All Isoforms

Kinesin-5/Eg5/KSP Kinesin-6 Kinesin-7/CENP-E Kinesin-12 Kinesin-14

Biological Activity
Protocol
Purity & Documentation
References
Customer Review

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)

Cellular Effect

Cell Line	Type	Value	Description	References
HCT-116	IC₅₀	30 nM Compound: EMD-534085	Antiproliferative activity against human HCT116 cells after 48 hrs by crystal violet staining assay Antiproliferative activity against human HCT116 cells after 48 hrs by crystal violet staining assay	[PMID: 20149654]

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].

MedChemExpress (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 reduction without toxic side effects^[1].

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

Molecular Weight

476.53

Formula

C₂₅H₃₁F₃N₄O₂

CAS No.

858668-07-2

Appearance

Solid

Color

White to off-white

SMILES

O=C(NC[C@H]1CC[C@@]2([H])[C@H](C3=CC=CC=C3)NC4=C(C=C(C(F)(F)F)C=C4)[C@@]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	2 years
	-20°C	1 year

Solvent & Solubility

In Vitro:

DMSO : ≥ 26 mg/mL (54.56 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

*"≥" 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

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

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Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Calculation results:

Working solution concentration: mg/mL

Purity & Documentation

Purity: 99.55%

Select Batch:

Data Sheet (276 KB) SDS (252 KB)

COA (252 KB) LCMS (266 KB)

Handling Instructions (2659 KB)

References

[1]. Schiemann K, et al. The discovery and optimization of hexahydro-2H-pyrano[3,2-c]quinolines (HHPQs) as potent and selective inhibitors of the mitotic kinesin-5. Bioorg Med Chem Lett. 2010 Mar 1;20(5):1491-5. [Content Brief]

[2]. Tang Y, et al. Rapid induction of apoptosis during Kinesin-5 inhibitor-induced mitotic arrest in HL60 cells. Cancer Lett. 2011 Nov 1;310(1):15-24. [Content Brief]

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

[1]. Schiemann K, et al. The discovery and optimization of hexahydro-2H-pyrano[3,2-c]quinolines (HHPQs) as potent and selective inhibitors of the mitotic kinesin-5. Bioorg Med Chem Lett. 2010 Mar 1;20(5):1491-5. [Content Brief]

[2]. Tang Y, et al. Rapid induction of apoptosis during Kinesin-5 inhibitor-induced mitotic arrest in HL60 cells. Cancer Lett. 2011 Nov 1;310(1):15-24. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	2.0985 mL	10.4925 mL	20.9850 mL	52.4626 mL
	5 mM	0.4197 mL	2.0985 mL	4.1970 mL	10.4925 mL
	10 mM	0.2099 mL	1.0493 mL	2.0985 mL	5.2463 mL
	15 mM	0.1399 mL	0.6995 mL	1.3990 mL	3.4975 mL
	20 mM	0.1049 mL	0.5246 mL	1.0493 mL	2.6231 mL
	25 mM	0.0839 mL	0.4197 mL	0.8394 mL	2.0985 mL
	30 mM	0.0700 mL	0.3498 mL	0.6995 mL	1.7488 mL
	40 mM	0.0525 mL	0.2623 mL	0.5246 mL	1.3116 mL
	50 mM	0.0420 mL	0.2099 mL	0.4197 mL	1.0493 mL

EMD534085 Related Classifications

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

EMD534085858668-07-2EMD 534085EMD-534085KinesinInhibitorinhibitorinhibit

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EMD534085

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