EMD534085
Based on 1 Customer Validation
EMD534085 is a potent and selective inhibitor of the mitotic kinesin-5 with an IC50 of 8 nM.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 純度 : 99.55%
- CAS 番号: 858668-07-2
- 分子式: C25H31F3N4O2
- 分子量:476.53
-
保管条件: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]
-
生物活性
-
化学情報
-
溶剤 & 溶解度
- 純度とドキュメンテーション
- 参考文献
-
Help & FAQs
-
HY-14846
LitronesibKinesin Inhibitor -
HY-16062
ARQ 621Eg5 Inhibitor -
HY-15187
FilanesibKSP Inhibitor -
HY-50759
IspinesibKSP Inhibitor -
HY-12069
SB-743921 hydrochlorideEg5 Inhibitor -
HY-50672
MK-0731KSP Inhibitor -
HY-110208
BRD9876 -
HY-10299
GSK-923295CENP-E Inhibitor -
HY-132840
SovilnesibKIF18A Inhibitor -
HY-15948
Kif15-IN-1Kinesin Inhibitor -
HY-19944
DimethylenastronKinesin Inhibitor -
HY-12241
AZ82KIFC1 Inhibitor
Kinesin アイソフォーム固有の製品をすべて表示
More
生物活性
製品説明
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] |
体外実験
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. .
体内実験
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
化学情報
-
CAS 番号 858668-07-2
-
性状 Solid
-
分子量 476.53
-
分子式 C25H31F3N4O2
-
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
-
輸送条件
Room temperature in continental US; may vary elsewhere.
-
保管条件
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
溶剤 & 溶解度
体外:
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.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
純度とドキュメンテーション
-
データシート (276 KB)
-
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)
-
取扱説明書 (2659 KB)
参考文献
[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 関連分類
HY-15000 関連分類
Powered by Bioz