1. Apoptosis
    Autophagy
  2. Survivin
    Autophagy
  3. YM-155 hydrochloride

YM-155 hydrochloride 

Cat. No.: HY-10194A
Handling Instructions

YM-155 hydrochloride is a novel survivin suppressant with an IC50 of 0.54 nM for the inhibition of survivin promoter activity.

For research use only. We do not sell to patients.

YM-155 hydrochloride Chemical Structure

YM-155 hydrochloride Chemical Structure

CAS No. : 355406-09-6

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Top Publications Citing Use of Products

    YM-155 hydrochloride purchased from MCE. Usage Cited in: Nutrients. 2018 Mar 15;10(3). pii: E353.

    Influences of YM155, a chemical inhibitor of survivin on ABT-737-induced apoptosis are analyzed by western blot.

    YM-155 hydrochloride purchased from MCE. Usage Cited in: Anticancer Res. 2019 Feb;39(2):609-617. 

    A2780 CSLCs are treated in the presence or absence of AS602801 (7.5 μM) and/or YM155 (10 nM) for 3 days, and then subjected to western blot analysis of survivin and glyceraldehyde 3-phosphate dehydrogenase (GAPDH).
    • Biological Activity

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    • References

    Description

    YM-155 hydrochloride is a novel survivin suppressant with an IC50 of 0.54 nM for the inhibition of survivin promoter activity.

    IC50 & Target

    IC50: 0.54 nM (survivin)

    In Vitro

    YM155 (30 μM) is not sensitive to survivn gene promoter-driven luciferase reporter activity. YM155 shows significant supression on endogenous survivin expression in PC-3 and PPC-1 human HRPC cells with deficient p53 via transcriptional inhibition of the survivin gene promoter. YM155 (100 nM) does not affect protein expression of c-IAP2, XIAP, Bcl-2, Bcl-xL, Bad, α-actin, and β-tubulin. YM155 potently inhibits human cancer cell lines (mutated or truncated p53) such as PC-3, PPC-1, DU145, TSU-Pr1, 22Rv1, SK-MEL-5 and A375 with IC50s ranging from 2.3 to 11 nM, respectively[1]. YM155 resultin in an increase in sensitivity of NSCLC cells to γ-radiation. YM155 combined with γ-radiation increases both the number of apoptotic cells and the activity of caspase-3. In addition, YM155 delays the repair of radiation-induced double-strand breaks in nuclear DNA[2].

    In Vivo

    YM155 (3 and 10 mg/kg) inhibits the tumor growth in PC-3 xenografts, without obvious body weight loss and blood cell count decrease. YM155 is highly distributed to tumor tissue in vivo. YM155 shows 80% TGI at a dose of 5 mg/kg in PC-3 orthotopic xenografts[1]. YM155 in combination with γ-radiation shows potent antitumor activity against H460 or Calu6 xenografts in nude mice[2]. In this orthotopic renal and metastatic lung tumors models, YM155 and IL-2 additively decreases tumor weight, lung metastasis, and luciferin-stained tumor images[3].

    Clinical Trial
    Storage

    Please store the product under the recommended conditions in the Certificate of Analysis.

    References
    Kinase Assay
    [1]

    A 2,767-bp sequence of human survivin gene promoter is isolated from human genomic DNA by PCR using Pyrobest polymerase and the following primers: 5'-GCGCGCTCGAGTCTAGACATGCGGATATATTC-3' and 5'-GCGCGAA-GCTTTGGCGGTTAATGGCGCGC-3'. The resulting PCR fragment is digested with XhoI/HindIII and ligated into the XhoI/HindIII cleavage site of the pGL3-Basic vector. The resulting plasmid is named pSUR-luc. DNA sequencing is done on all amplified sequences by a DNA sequencer. The activity of pSUR-luc is confirmed by luciferase assay with transiently transfected HeLa-S3 cells. Luciferase assay is done. The pGL3 control vector, which contains the SV40 promoter and enhancer sequences, is used. HeLa cells are stably transfected with pSUR-luc and pSV2bsr by Lipofect-AMINE 2000. After blasticidin selection at 10 μg/mL, a single colony is chosen based on appropriate luciferase signals and genetic stability over time and named HeLa-SURP-luc. CHO cells are stably transfected with pGL3-control and pSV2bsr. After blasticidin selection at 10 μg/mL, a single colony is chosen based on appropriate luciferase signals and genetic stability over time and named CHO-SV40-luc. Stocked cells from the HeLa-SURP-luc and CHO-SV40-luc clones are used for chemical screening and characterization of YM155. YM155 in DMSO are added to the cells, which had been seeded the previous day on 96-well plastic plates at 5×103 per well. Luciferase activity is measured 24 hours later. IC50 is calculated by logistic analysis.

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

    Cell Assay
    [1]

    The antiproliferative activity of YM-155 is measured. After treatment with YM-155 for 48 h, the cell count is determined by sulforhodamine B assay. The GI50 value is calculated by logistic analysis, which is the drug concentration resulting in a 50% reduction in the net protein increase (as measured by sulforhodamine B staining) in control cells during the drug incubation. The assay is done in triplicate, and the mean GI50 value is obtained from the results of four independent assays.

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

    Animal Administration
    [1]

    Five-week-old male nude mice (BALB/c nu/nu) are used for the assay. PC-3 cells (2×106-3×106) are injected into the flanks of the mice and allowed to reach a tumor volume of > 100 mm3 in tumor volume (length×width2×0.5). YM-155 is s.c. administered as a 3-day continuous infusion per week for 2 weeks using an implanted micro-osmotic pump or i.v. administered five times a week for 2 weeks. The percentage of tumor growth inhibition 14 days after initial YM-155 administration is calculated for each group using the following formula: MTV=100×{1-[(MTV of the treated group on day 14)-(MTV of the treated group on day 0)]/[(MTV of the control group on day 14)-(MTV of the control group on day 0)]}, where MTV is mean tumor volume. For both the frozen tumors and plasma samples, survivin expression levels are analyzed by Western blotting and YM-155 drug concentration by high-performance liquid chromatography/triple quadrupole mass spectrometry (LC/MS/MS) using validated methods.

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

    References
    Molecular Weight

    398.84

    Formula

    C₂₀H₁₉ClN₄O₃

    CAS No.

    355406-09-6

    SMILES

    O=C(C1=C2[N+](CC3=NC=CN=C3)=C(C)N1CCOC)C4=C(C=CC=C4)C2=O.[Cl-]

    Shipping

    Room temperature in continental US; may vary elsewhere

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    Cat. No.:
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    Cat. No.: HY-10194A