EMD534085
Based on 1 Customer Validation
EMD534085 is a potent and selective inhibitor of the mitotic kinesin-5 with an IC50 of 8 nM.
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- Reinheit : 99.55%
- CAS. Nr.: 858668-07-2
- Formel: C25H31F3N4O2
- Molecular Weight:476.53
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Speicherung:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biologische Aktivität
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Chemical Information
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Lösungsmittel & Löslichkeit
- Protokoll
- Reinheit & Dokumentation
- Verweise
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Help & FAQs
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Biologische Aktivität
Beschreibung
IC50 & Target
[1]|
Kinesin-5 8 nM (IC50) |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
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| HCT-116 | IC50 |
30 nM
Compound: EMD-534085
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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
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[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. Further protocols information, click here.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS. Nr. 858668-07-2
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Appearance Solid
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Molecular Weight 476.53
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Formel C25H31F3N4O2
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Color White to off-white
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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
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Lösungsmittel & Löslichkeit
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.
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.
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.
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
Protokoll
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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
Reinheit & Dokumentation
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Data Sheet (276 KB)
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SDS (254 KB)
- English - EN (254 KB)
- Français - FR (254 KB)
- Deutsch - DE (254 KB)
- Norwegian - NO (254 KB)
- Español - ES (254 KB)
- Swedish - SV (254 KB)
- Italian - IT (254 KB)
- Korean - KR (254 KB)
- Portuguese - PT (254 KB)
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Handling Instructions (2659 KB)
Verweise
[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
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.
| 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
HY-15000 Related Classifications
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