YM155Survivin suppressant,apoptosis inhibitor CAS# 781661-94-7 |
- YM-155 hydrochloride
Catalog No.:BCC2066
CAS No.:355406-09-6
Quality Control & MSDS
3D structure
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| Cas No. | 781661-94-7 | SDF | Download SDF |
| PubChem ID | 11178236 | Appearance | Powder |
| Formula | C20H19BrN4O3 | M.Wt | 443.3 |
| Type of Compound | N/A | Storage | Desiccate at -20°C |
| Synonyms | Sepantronium bromide | ||
| Solubility | H2O : 100 mg/mL (225.59 mM; Need ultrasonic) DMSO : 50 mg/mL (112.79 mM; Need ultrasonic) | ||
| Chemical Name | 1-(2-methoxyethyl)-2-methyl-3-(pyrazin-2-ylmethyl)benzo[f]benzimidazol-3-ium-4,9-dione;bromide | ||
| SMILES | CC1=[N+](C2=C(N1CCOC)C(=O)C3=CC=CC=C3C2=O)CC4=NC=CN=C4.[Br-] | ||
| Standard InChIKey | QBIYUDDJPRGKNJ-UHFFFAOYSA-M | ||
| Standard InChI | InChI=1S/C20H19N4O3.BrH/c1-13-23(9-10-27-2)17-18(24(13)12-14-11-21-7-8-22-14)20(26)16-6-4-3-5-15(16)19(17)25;/h3-8,11H,9-10,12H2,1-2H3;1H/q+1;/p-1 | ||
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months. Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it. |
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| About Packaging | 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial. 2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial. 3. Try to avoid loss or contamination during the experiment. |
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| Shipping Condition | Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request. | ||
| Description | YM155 (Sepantronium Bromide) is a potent inhibitor of Survivin promoter activity with IC50 of 0.54 nM. | |||||
| Targets | Survivin | |||||
| IC50 | 0.54 nM | |||||
| Cell experiment: [1] | |
| Cell lines | PC-3 and PPC-1 cells |
| Preparation method | The solubility of this compound in DMSO is >10 mM. General tips for obtaining a higher concentration: Please warm the tube at 37 °C for 10 minutes and/or shake it in the ultrasonic bath for a while.Stock solution can be stored below -20°C for several months. |
| Reacting condition | 1 μM, 48 hours |
| Applications | In both cell lines, YM155, at concentrations from 10 to 1000 nM, significantly decreased the viability of cells in a dose-dependent manner. When exposed to YM155, PC-3 and PPC-1 showed a concomitant increase in caspase-3 activity. These results suggest that YM155 induces apoptosis in human HRPC cells. |
| Animal experiment: [1] | |
| Animal models | BALB/c nu/nu mice injected with PC-3 cells |
| Dosage form | Subcutaneous injection, 10 mg/kg |
| Application | Mice with large established s.c. xenografted PC-3 tumors received a 3-day continuous infusion of YM155 at 10 mg/kg. Saline control animals showed rapid tumor growth from day 0 (366 mm3) to day 7 (1,123 mm3), with no change in intratumoral surviving and actin protein levels. In contrast, animals treated with YM155 showed tumor regression from day 0 (292 mm3) to day7 (162 mm3), and a clear decrease in intratumoral survivin levels on days 3 and 7 was observed. |
| Other notes | Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal. |
| References: [1] Nakahara T, Takeuchi M, Kinoyama I, et al. YM155, a novel small-molecule survivin suppressant, induces regression of established human hormone-refractory prostate tumor xenografts. Cancer research, 2007, 67(17): 8014-8021. | |
YM155 Dilution Calculator
YM155 Molarity Calculator
| 1 mg | 5 mg | 10 mg | 20 mg | 25 mg | |
| 1 mM | 2.2558 mL | 11.279 mL | 22.5581 mL | 45.1162 mL | 56.3952 mL |
| 5 mM | 0.4512 mL | 2.2558 mL | 4.5116 mL | 9.0232 mL | 11.279 mL |
| 10 mM | 0.2256 mL | 1.1279 mL | 2.2558 mL | 4.5116 mL | 5.6395 mL |
| 50 mM | 0.0451 mL | 0.2256 mL | 0.4512 mL | 0.9023 mL | 1.1279 mL |
| 100 mM | 0.0226 mL | 0.1128 mL | 0.2256 mL | 0.4512 mL | 0.564 mL |
| * Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations. | |||||
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Sepantronium bromide, also known as YM155, is a novel small-molecule suppressant of surviving, the smallest member of inhibitor of apoptosis (IAP) gene family. It exhibits a potent suppressive activity against survivin but has little effect on expression levels of other IAP family members or B-cell lymphoma 2 (BCL-2) related proteins. YM155 also suppresses proliferation in a broad range of human cancer cell lines, induces tumor regression in non-small cell lung cancer (NSCLC), melanoma, bladder, aggressive non-Hodgkin lymphoma, and breast cancer xenograft models, reduces spontaneous metastases, and significantly prolongs the survival of animal harboring established metastatic tumors derived from a human triple-negative breast cancer (TNBC) cell lines.
Reference
Naoki Kaneko, Kentaro Yamanaka, Aya Kita, Kenji Tabata, Takafumi Akabane, and Masamichi Mori. Synergistic antitumor activities of sepantronium bromide (YM155), a surviving suppressant, in combination with microtubule-targeting agents in triple-negative breast cancer cells. Biol Pharm Bull 2013.
Yan-Fang Tao, Jun Lu, Xiao-Juan Du, Li-Chao Sun, Xuan Zhao, Liang Peng, Lan Cao, Pei-Fang Xiao, Li Pang, Dong Wu, Na Wang, Xing Feng, Yan-Hong Li, Jian Ni, Jian Wang and Jian Pan. Survivin selective inhibitor YM155 induce apoptosis in SK-NEP-1 Wilms tumor cells. BMC Cancer 2012, 12:619
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YM155 enhances ABT-737-mediated apoptosis through Mcl-1 downregulation in Mcl-1-overexpressed cancer cells.[Pubmed:28120212]
Mol Cell Biochem. 2017 May;429(1-2):91-102.
ABT-737 is a BH3 mimetic inhibitor of Bcl-xL, Bcl-2, and Bcl-w, and it has been reported for anti-cancer effects in various types of cancer cells. However, ABT-737 fails to induce apoptosis in cancer cell with high levels of Mcl-1 expression. The pharmacological survivin inhibitor YM155 has been reported to induce downregulation of Mcl-1 expression. Therefore, we investigated the effect of YM155 to sensitize resistance against ABT-737 in Mcl-1-overexpressed human renal carcinoma Caki cells. We found that ABT-737 alone and YM155 alone did not induce apoptosis, but YM155 markedly sensitized ABT-737-mediated apoptosis in Mcl-1-overexpressed Caki cells, human glioma cells (U251MG), and human lung carcinoma cells (A549). In contrast, combined treatment with ABT-737 and YM155 did not increase apoptosis in normal mouse kidney cells (TCMK-1) and human mesangial cells (MC). YM155 induced lysosome-dependent downregulation of Mcl-1 expression in Mcl-1-overexpressed Caki cells. In addition, combined treatment with ABT-737 and YM155 induced loss of mitochondrial membrane potential and inhibited interaction of Bcl-xL and Bax. Taken together, our results suggested that YM155 effectively improves sensitivity to ABT-737 through downregulation of Mcl-1 expression.
YM155 Reverses Statin Resistance in Renal Cancer by Reducing Expression of Survivin.[Pubmed:28011476]
Anticancer Res. 2017 Jan;37(1):75-80.
AIM: The purpose of the present study was to clarify whether treatment with YM155, a novel small-molecule inhibitor of survivin, reverses statin resistance in statin-resistant renal cell cancer (RCC). MATERIALS AND METHODS: We induced simvastatin resistance in a renal clear cell carcinoma cell line (Caki-1-staR). In vitro and in vivo models were used to test the efficacy of YM155 and simvastatin. RESULTS: Survivin gene expression was significantly stronger in Caki-1-staR cells than in its parent cells (Caki-1). In Caki-1-staR cells, YM155 significantly reduced expression of survivin gene and cell proliferation in a dose-dependent manner. Treatment with YM155 significantly reversed simvastatin resistance in Caki-1-staR cells. YM155 significantly inhibited the growth of Caki-1-staR tumors in a nude mouse tumor xenograft model. Furthermore, YM155 significantly enhanced the antitumor effects of simvastatin on Caki-1-staR tumors. CONCLUSION: Our results indicate that inhibition of survivin by YM155 overcomes statin resistance in RCC cells.
Intact wound repair activity of human mesenchymal stem cells after YM155 mediated selective ablation of undifferentiated human embryonic stem cells.[Pubmed:28185769]
J Dermatol Sci. 2017 May;86(2):123-131.
BACKGROUND: Risk of teratoma formation during human pluripotent stem cell (hPSC)-based cell therapy is one of the technical hurdles that must be resolved before their wider clinical application. To this end, selective ablation of undifferentiated hPSCs has been achieved using small molecules whose application should be safe for differentiated cells derived from the hPSCs. OBJECTIVE: However, the functional safety of such small molecules in the cells differentiated from hPSCs has not yet been extensively validated. METHOD: We used the survivin inhibitor YM155, which induced highly selective cell death of hPSCs for ablating undifferentiated hESCs after differentiation to human mesenchymal stem cells (hMSCs) and examined whether hMSCs remained fully functional after being exposed by YM155. RESULTS: We demonstrated that human mesenchymal stem cells (hMSCs) derived from human embryonic stem cells (hESCs) remained fully functional in vitro and in vivo, while hESCs were selectively ablated. CONCLUSION: These results suggest that a single treatment with YM155 after differentiation of hMSCs would be a valid approach for teratoma-free cell therapy.
