YM155 (Synonyms: Sepantronium bromide) |
رقم الكتالوجGC13107
One-Click Copy Product Info
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YM155, a small imidazolium-based compound, potently inhibits survivin promoter activity with an IC50 value of 0.54nM.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 781661-94-7
Sample solution is provided at 25 µL, 10mM.
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YM155, a small imidazolium-based compound, potently inhibits survivin promoter activity with an IC50 value of 0.54nM [1]. YM155 can suppress survivin expression through the disruption of SP1 binding to the survivin core promoter and of ILF3–p54/nrb complex[2]. YM155 has been widely used to induce tumor cell apoptosis and promote tumor regression in diverse cell and animal models[3].
In vitro, YM155 treatment for 120 hours significantly inhibited the proliferation of UKF-NB-3 and UKF-NB-6 cells with IC50 values of 0.49 and 0.65nM, respectively[4]. Treatment of H1299 cells with YM155 at 40nM for 24h significantly induced cell death and promoted mitochondrial dysfunction, leading to a reduction in tricarboxylic acid (TCA) cycle intermediates[5]. Treatment with 10nM YM155 for 24 hours significantly inhibited PANC-1 cell viability and induced downregulation of PI3K, p-ERK, and p-STAT3 in PANC-1 cells[6].
In vivo, YM155 treatment via subcutaneous injection at a dose of 2 mg/kg/day for 21 days remarkably reduced tumor growth in the SH-SY5Y cell xenograft model of mice, without affecting body weight[7]. Continuous subcutaneous infusion of YM155 (5mg/kg/day) for 21 days significantly inhibited the development of ascites in Primary effusion lymphoma (PEL) xenograft mice[8].
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[J]. Cancer research, 2007, 67(17): 8014-8021.
[2] Rauch A, Hennig D, Schäfer C, et al. Survivin and YM155: how faithful is the liaison?[J]. Biochimica et Biophysica Acta (BBA)-Reviews on Cancer, 2014, 1845(2): 202-220.
[3] Tolcher A W, Quinn D I, Ferrari A, et al. A phase II study of YM155, a novel small-molecule suppressor of survivin, in castration-resistant taxane-pretreated prostate cancer[J]. Annals of oncology, 2012, 23(4): 968-973.
[4] Voges Y, Michaelis M, Rothweiler F, et al. Effects of YM155 on survivin levels and viability in neuroblastoma cells with acquired drug resistance[J]. Cell death & disease, 2016, 7(10): e2410-e2410.
[5] Mondal A, Jia D, Bhatt V, et al. Ym155 localizes to the mitochondria leading to mitochondria dysfunction and activation of AMPK that inhibits BMP signaling in lung cancer cells[J]. Scientific reports, 2022, 12(1): 13135.
[6] Na Y S, Yang S J, Kim S M, et al. YM155 induces EGFR suppression in pancreatic cancer cells[J]. PloS one, 2012, 7(6): e38625.
[7] Li X, Yang F, He N, et al. YM155 inhibits neuroblastoma growth through degradation of MYCN: A new role as a USP7 inhibitor[J]. European Journal of Pharmaceutical Sciences, 2023, 181: 106343.
[8] Kojima Y, Hayakawa F, Morishita T, et al. YM155 induces apoptosis through proteasome-dependent degradation of MCL-1 in primary effusion lymphoma[J]. Pharmacological research, 2017, 120: 242-251.
| Cell experiment [1]: | |
Cell lines | PC-3 cells |
Preparation Method | PC-3 cells were cultured in DMEM medium supplemented with 10% heat-inactivated fetal bovine serum and placed in a 37°C humidified incubator at 5% CO2. After 48h of culture in the presence of YM155 (1, 10, 100, and 1000nM), PC-3 cells were harvested by trypsin digestion and centrifugation and resuspended in DMEM medium. The cell suspension was diluted in an equal volume of trypan blue (0.4% working solution). Live (unstained) and dead (stained) cells were counted using a blood cell counter. |
Reaction Conditions | 1, 10, 100, and 1000nM; 48h |
Applications | YM155 significantly inhibited the viability of PC-3 cells in a dose-dependent manner. |
| Animal experiment [2]: | |
Animal models | Female BALB/c-nu mice |
Preparation Method | Six-week-old female BALB/c-nu mice were maintained in a standard sterile environment. SH-SY5Y cells (2×106) were collected and mixed with an equal volume of Matrigel and injected subcutaneously into the flank of mice. After tumor formation, mice were randomly divided into two groups: vehicle group (saline) or YM155 group. YM155 was injected subcutaneously continuously at a dose of 2mg/kg/day for 21 days using a micro-osmotic pump. Tumor diameter was measured twice a week, and tumor volume was calculated as the product of length × width2×0.5. |
Dosage form | 2mg/kg/day for 21 days; s.c. |
Applications | YM155 treatment remarkably reduced tumor growth in the SH-SY5Y cell xenograft model of mice. |
References: | |
| Cas No. | 781661-94-7 | SDF | |
| المرادفات | Sepantronium bromide | ||
| Chemical Name | 1-(2-methoxyethyl)-2-methyl-3-(pyrazin-2-ylmethyl)benzo[f]benzimidazol-3-ium-4,9-dione;bromide | ||
| Canonical SMILES | CC1=[N+](C2=C(N1CCOC)C(=O)C3=CC=CC=C3C2=O)CC4=NC=CN=C4.[Br-] | ||
| Formula | C20H19BrN4O3 | M.Wt | 443.3 |
| الذوبان | ≥ 22.15 mg/mL in DMSO, ≥ 13.49 mg/mL in EtOH with ultrasonic, ≥ 96.2 mg/mL in Water with ultrasonic | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.2558 mL | 11.279 mL | 22.5581 mL |
| 5 mM | 451.2 μL | 2.2558 mL | 4.5116 mL |
| 10 mM | 225.6 μL | 1.1279 mL | 2.2558 mL |
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Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
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Quality Control & SDS
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- Purity: >98.00% Appearance: A solid
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Average Rating: 5 (Based on Reviews and 30 reference(s) in Google Scholar.)