ホームページ Apoptosis Survivin inhibitor - IAP inhibitor - Autophagy activator Sepantronium Bromide (YM155) For research use only.

Sepantronium Bromide (YM155)

Sepantronium Bromide(YM155) is a potent survivin suppressant by inhibiting Survivin promoter activity with IC50 of 0.54 nM in HeLa-SURP-luc and CHO-SV40-luc cells; does not significantly inhibit SV40 promoter activity, but is observed to slightly inhibit the interaction of Survivin with XIAP. YM155 down-regulates survivin and XIAP, modulates autophagy and induces autophagy-dependent DNA damage in breast cancer cells. Phase 2.

Sepantronium Bromide (YM155)化学構造

CAS No. 781661-94-7

サイズ 価格(税別) 在庫状況
10mM (1mL in DMSO) JPY 29500 国内在庫あり
JPY 22000 国内在庫あり
JPY 55500 国内在庫あり
JPY 115500 国内在庫あり
JPY 418500 国内在庫なし(納期7~10日)

代表番号: 045-509-1970|電子メール：[email protected]
よく尋ねられる質問

文献中Selleckの製品使用例（175）

製品安全説明書

現在のバッチを見る： 純度： 99.45%
99.45

Sepantronium Bromide (YM155)関連製品

シグナル伝達経路

Survivin Signaling Pathways

Survivinシグナル伝達経路

Survivin阻害剤の選択性比較

Cell Data

Cell Lines Assay Type Concentration Incubation Time 活性情報 PMID
WSU-DLCL2 Growth Inhibition Assay 10 nM 24 h inhibits cell proliferation 24486595
SU-DHL-8 Growth Inhibition Assay 10 nM 24 h inhibits cell proliferation 24486595
DB Growth Inhibition Assay 10 nM 24 h inhibits cell proliferation 24486595
TE13 Growth Inhibition Assay 0-100 nM 24/48 h decreases cell viability in a dose-dependent manner 25139395
Eca109 Growth Inhibition Assay 0-100 nM 24/48 h decreases cell viability in a dose-dependent manner 25139395
TE13 Function Assay 1-50 nM 48 h suppresses survivin expression in a dose dependent manner 25139395
Eca109 Function Assay 1-50 nM 48 h suppresses survivin expression in a dose dependent manner 25139395
INA-6  Apoptosis Assay 0-50 nM 24 h induces apoptosis 25296978
U-266 Apoptosis Assay 0-50 nM 24 h induces apoptosis 25296978
SK-MM-2 Growth Inhibition Assay 0-500 nM 48 h inhibits cell growth in a dose-dependent manner 25296978
KMS-12-BM Growth Inhibition Assay 0-500 nM 48 h inhibits cell growth in a dose-dependent manner 25296978
MOLP-2 Growth Inhibition Assay 0-500 nM 48 h inhibits cell growth in a dose-dependent manner 25296978
L-363 Growth Inhibition Assay 0-500 nM 48 h inhibits cell growth in a dose-dependent manner 25296978
OPM-2 Growth Inhibition Assay 0-500 nM 48 h inhibits cell growth in a dose-dependent manner 25296978
NCI-H929 Growth Inhibition Assay 0-500 nM 48 h inhibits cell growth in a dose-dependent manner 25296978
HG-1 Growth Inhibition Assay 0-500 nM 48 h inhibits cell growth in a dose-dependent manner 25296978
MOLP-8 Growth Inhibition Assay 0-500 nM 48 h inhibits cell growth in a dose-dependent manner 25296978
U-266 Growth Inhibition Assay 0-500 nM 48 h inhibits cell growth in a dose-dependent manner 25296978
INA-6 Growth Inhibition Assay 0-500 nM 48 h inhibits cell growth in a dose-dependent manner 25296978
SACC-83 Function Assay 5 nM 48 h decreases nuclear expression of HIF-1α 25485635
AGS  Growth Inhibition Assay 10/20 nM 48 h inhibits cell growth in a dose-dependent manner 25635055
KATOIII Growth Inhibition Assay 10/20 nM 48 h inhibits cell growth in a dose-dependent manner 25635055
U-CH1  Growth Inhibition Assay 0-5 μM 24/48 h IC50=9.03 nM for 48h 25640185
MUG-Chor  Growth Inhibition Assay 0-5 μM 24/48 h IC50=7.05 nM for 48h 25640185
MV4-11 Function Assay 0–1 μM 72 h induces downregulation of Survivin 25659731
Kasumi-1 Function Assay 0–1 μM 72 h induces downregulation of Survivin 25659731
AML-193 Function Assay 0–1 μM 72 h induces downregulation of Survivin 25659731
CMK Function Assay 0–1 μM 72 h induces downregulation of Survivin 25659731
THP-1 Function Assay 0–1 μM 72 h induces downregulation of Survivin 25659731
M-07e Function Assay 0–1 μM 72 h induces downregulation of Survivin 25659731
THP-1 Apoptosis Assay 1 μM 72 h induces apoptosis 25659731
ACC-2 Growth Inhibition Assay 0-100 nM 24 h inhibits cell growth in a dose-dependent manner 24370995
ACC-2 Apoptosis Assay 0-20 nM 24 h induces apoptosis in a dose-dependent manner 24370995
ACC-2 Function Assay 0-20 nM 24 h increases the conversion of LC3I to LC3II 24370995
BFTC905 Growth Inhibition Assay 0-1000 nM 48 h  IC50=20 nM, inhibits cell growth in a dose-dependent manner 24297644
T24 Growth Inhibition Assay 0-1000 nM 48 h  IC50=20 nM, inhibits cell growth in a dose-dependent manner 24297644
TSGH8301  Growth Inhibition Assay 0-1000 nM 48 h  IC50=20 nM, inhibits cell growth in a dose-dependent manner 24297644
BFTC909 Growth Inhibition Assay 0-1000 nM 48 h  IC50=20 nM, inhibits cell growth in a dose-dependent manner 24297644
BFTC905 Apoptosis Assay 20 nM 48 h induces apoptosis 24297644
BFTC905 Function Assay 20 nM 48 h decreases the expression of LC3B-II 24297644
A2780p Function Assay 0-100 nM 24 h induces Survivin downregulation  24262875
A2780cis Function Assay 0-100 nM 24 h induces Survivin downregulation  24262875
A2780p Apoptosis Assay 5-100 nM 24/48 h increases apoptosis in a concentration-dependent manner 24262875
A2780cis Apoptosis Assay 5-100 nM 24/48 h increases apoptosis in a concentration-dependent manner 24262875
SH-SY5Y Apoptosis Assay 1/10/100 µM 72 h induces apoptosis in a dose-dependent manner 24254560
HL-60  Function Assay 1 μM 6/12/24 h inhibits the expression of survivin 23618862
U937  Function Assay 1 μM 6/12/24 h inhibits the expression of survivin 23618862
HL-60 Apoptosis Assay 0.1/1 μM 8 h induces apoptosis 23618862
Sk-NEP-1  Growth Inhibition Assay 1-10000 nM 24 h IC50=100 nM 23267699
SK-NEP-1  Apoptosis Assay 50/100 nM 12/24 h induces apoptosis 23267699
M059J Growth Inhibition Assay 0-50 nM 48 h inhibits cell growth in a dose-dependent manner 22770110
M059K Growth Inhibition Assay 0-50 nM 48 h inhibits cell growth in a dose-dependent manner 22770110
M059J Apoptosis Assay 30 nM 24 h induces apoptosis 22770110
M059K Apoptosis Assay 30 nM 24 h induces apoptosis 22770110
PANC-1 Growth Inhibition Assay 0.01-1000 nM 48 h IC50=3.69 nM 22723871
MIAPaCa-2 Growth Inhibition Assay 0.01-1000 nM 48 h IC50=29.36 nM 22723871
BxPC-3 Growth Inhibition Assay 0.01-1000 nM 48 h IC50=30.26 nM 22723871
PANC-1 Function Assay 0-1000 nM 24 h induces downregulation of XIAP and survivin expression 22723871
MIAPaCa-2 Function Assay 0-1000 nM 24 h induces downregulation of XIAP and survivin expression 22723871
BxPC-3 Function Assay 0-1000 nM 24 h induces downregulation of XIAP and survivin expression 22723871
TC-32 Growth Inhibition Assay 0.1-1000 nM EC50=3.0 nM, inhibits cell growth in a dose-dependent manner 22961763
TC-71 Growth Inhibition Assay 0.1-1000 nM EC50=5.7 nM, inhibits cell growth in a dose-dependent manner 22961763
SK-ES-1 Growth Inhibition Assay 0.1-1000 nM EC50=2.8 nM, inhibits cell growth in a dose-dependent manner 22961763
RD-ES Growth Inhibition Assay 0.1-1000 nM EC50=6.2 nM, inhibits cell growth in a dose-dependent manner 22961763
HEK293 Growth Inhibition Assay 0.1-1000 nM EC50=23.0 nM, inhibits cell growth in a dose-dependent manner 22961763
MT-3 + SB203580 Kinase Assay 72 h IC50=38.41 ± 5.02 nM for DR5 expression 24866585
MT-3 + NAC Kinase Assay 72 h IC50=56.2 ± 2.07 nM for DR5 expression 24866585
SUM-159 Kinase Assay 72 h IC50=69.4 ± 4.23 nM for DR5 expression 24866585
MDA-MB-468 Kinase Assay 72 h IC50=0.07 ± 0.02 nM for DR5 expression 24866585
MT-3 Kinase Assay 72 h IC50=54.11 ± 4.32 nM for DR5 expression 24866585
SUM-159 Kinase Assay 72 h IC50=1.72 ± 0.33 nM for DR4 expression 24866585
MDA-MB-468 Kinase Assay 72 h IC50=0.11 ± 0.01 nM for DR4 expression 24866585
MT-3 Kinase Assay 72 h IC50=2.86 ± 0.54 nM for DR4 expression 24866585
SK-BR-3 Growth Inhibition Assay 72 h IC50=7 ± 0.3 nM 25220225
MDA-MB-231 Growth Inhibition Assay 72 h IC50=5 ± 1 nM 25220225
MCF7-TamC6 Growth Inhibition Assay 72 h IC50=6 ± 0.1 nM 25220225
MCF7-TamC3 Growth Inhibition Assay 72 h IC50=6 ± 3 nM 25220225
MCF7-TamR8 Growth Inhibition Assay 72 h IC50=15 ± 6 nM 25220225
MCF7-TamR7 Growth Inhibition Assay 72 h IC50=8 ± 3 nM 25220225
MCF7-TamR6 Growth Inhibition Assay 72 h IC50=8 ± 6 nM 25220225
MCF7 Growth Inhibition Assay 72 h IC50=13 ± 6 nM 25220225
ME-1 Growth Inhibition Assay 72 h IC50=0.684 ± 0.179 μM 25659731
HEL Growth Inhibition Assay 72 h IC50=0.559 ± 0.038 μM 25659731
OCI/AML3 Growth Inhibition Assay 72 h IC50=0.011 ± 0.002 μM 25659731
ML-2 Growth Inhibition Assay 72 h IC50=0.009 ± 0.002 μM 25659731
HL-60 Growth Inhibition Assay 72 h IC50=0.001 ± 0.0002 μM 25659731
AML-193 Growth Inhibition Assay 72 h IC50=0.462 ± 0.060 μM 25659731
MV4-11 Growth Inhibition Assay 72 h IC50=0.055 ± 0.028 μM 25659731
CMK Growth Inhibition Assay 72 h IC50=0.053 ± 0.009 μM 25659731
THP-1 Growth Inhibition Assay 72 h IC50=0.051 ± 0.013 μM 25659731
M-07e Growth Inhibition Assay 72 h IC50=0.040 ± 0.013 μM 25659731
Kasumi-1 Growth Inhibition Assay 72 h IC50=0.009 ± 0.0009 μM 25659731
HL-60 Growth Inhibition Assay 72 h IC50=0.3 nM 23618862
U937  Growth Inhibition Assay 72 h IC50=0.8 nM 23618862
DB Growth Inhibition Assay 48 h GI50=3.5 nM 21237508
Pfeiffer Growth Inhibition Assay 48 h GI50=3.9 nM 21237508
SU-DHL-5 Growth Inhibition Assay 48 h GI50=0.23 nM 21237508
SU-DHL-8 Growth Inhibition Assay 48 h GI50=1.4 nM 21237508
WSU-DLCL-2 Growth Inhibition Assay 48 h GI50=1.4 nM 21237508
RPMI-7951 Growth Inhibition Assay GI50=3.2 nM 21737502
SK-MEL-5 Growth Inhibition Assay GI50=4.2 nM 21737502
A375 Growth Inhibition Assay GI50=6.3 nM 21737502
SK-MEL-28 Growth Inhibition Assay GI50=7.6 nM 21737502
SK-MEL-2 Growth Inhibition Assay GI50=11 nM 21737502
A549 Growth inhibition assay Growth inhibition of human A549 cells, IC50=0.0134μM 28814374
DU145 Cytotoxicity assay Cytotoxicity against human DU145 cells by MTT assay, EC50=0.0138μM 28774426
PC3 Cytotoxicity assay Cytotoxicity against human PC3 cells by MTT assay, EC50=0.092μM 28774426
A549 Function assay Inhibition of PAK1 in human A549 cells, IC50=0.5μM 28814374
他の多くの細胞株試験データをご覧になる場合はこちらをクリックして下さい

生物活性

製品説明 Sepantronium Bromide(YM155) is a potent survivin suppressant by inhibiting Survivin promoter activity with IC50 of 0.54 nM in HeLa-SURP-luc and CHO-SV40-luc cells; does not significantly inhibit SV40 promoter activity, but is observed to slightly inhibit the interaction of Survivin with XIAP. YM155 down-regulates survivin and XIAP, modulates autophagy and induces autophagy-dependent DNA damage in breast cancer cells. Phase 2.
Targets
Survivin [1]
(HeLa-SURP-luc, CHO-SV40-luc cells)
0.54 nM
In Vitro
In vitro

YM155 is not sensitive to survivn gene promoter-driven luciferase reporter activity even at 30 μM. YM155 significantly inhibits endogenous survivin expression in PC-3 and PPC-1 human HRPC cells with deficient p53 through transcriptional inhibition of the survivin gene promoter. On the contrary YM155 shows no sufficient effect on protein expression of c-IAP2, XIAP, Bcl-2, Bcl-xL, Bad, α-actin, and β-tubulin at 100 nM. YM155 indicates great apoptosis in human cancer cell lines including PC-3 and PPC-1 with a concomitant increase in caspase-3 activity. YM155 potently inhibits human cancer cell lines (mutated or truncated p53) including PC-3, PPC-1, DU145, TSU-Pr1, 22Rv1, SK-MEL-5 and A375 with IC50 from 2.3 to 11 nM, respectively. [1] YM155 increases the sensitivity of NSCLC cells to γ-radiation. The combination of YM155 and γ-radiation increases both the number of apoptotic cells and the activity of caspase-3. YM155 delays the repair of radiation-induced double-strand breaks in nuclear DNA. [2]
Kinase Assay Promoter-luciferase reporter assay
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
細胞実験 細胞株 Hormone refractory prostate cancer cell lines (PC-3, PPC-1, DU145, TSU-Pr1 and 22Rv1) and malignant melanoma cell lines (SK-MEL-5 and A375)
濃度 ~ 100 nM
反応時間 48 hours
実験の流れ

Cells are seeded in 96-well plates at a density of 5-40 × 103. YM155 is dissolved in DMSO and added to cells for 48 hours. Then the cell count is determined by sulforhodamine B assay.
実験結果図 Methods Biomarkers 結果図 PMID
Western blot p-STAT3 / STAT3 β-catenin / c-Myc / Cyclin D1 / CD44 Survivin / XIAP / Caspase-7 / Caspase-9 / Caspase-3 / Cleaved Caspase-8 / PARP 22723871
Immunofluorescence PARP-1 / PAR EGFR 26090615
Growth inhibition assay Cell viability 29636860
In Vivo
In Vivo

YM155 completely inhibits the tumor growth of PC-3 s.c. xenografted prostate tumors at doses of 3 and 10 mg/kg, without body weight loss and blood cell count decrease. Pharmacokinetic analysis shows that YM155 is highly distributed to tumor tissue. Moreover, YM155 shows 80% TGI at a dose of 5 mg/kg in PC-3 orthotopic xenografts. [1] The combination therapy with YM155 and γ-radiation shows great antitumor activity against H460 or Calu6 xenografts in nude mice. [2]
動物実験 動物モデル PC-3 s.c. (orthotopic) xenografts in male nude mice (BALB/c nu/nu)
投与量 5 mg/kg
投与経路 Subcutaneous injection as a 3-day continuous infusion per week for 3 weeks by an implanted micro-osmotic pump
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT05263583 Recruiting
High-grade B-cell Lymphoma|Burkitt Lymphoma|Lymphoma B-Cell|Lymphoma Large B-Cell Diffuse|Lymphatic Diseases|Lymphoma High-Grade|C-MYC/BCL2 Double-Hit High-Grade B-Cell Lymphoma|C-MYC/BCL6 Double-Hit High-Grade B-Cell Lymphoma|C-Myc Gene Rearrangement
Cothera Bioscience Inc
 December 9 2022 Phase 2
NCT01023386 Completed
Cancer
Astellas Pharma Inc
 November 2009 Phase 1

化学情報

分子量 443.29 化学式

C20H19BrN4O3
CAS No. 781661-94-7 SDF Download Sepantronium Bromide (YM155) SDFをダウンロードする
Smiles CC1=[N+](C2=C(N1CCOC)C(=O)C3=CC=CC=C3C2=O)CC4=NC=CN=C4.[Br-]
保管

In vitro
Batch:

Water : 89 mg/mL

DMSO : 55 mg/mL ( (124.07 mM)； 吸湿したDMSOは溶解度を減少させます。新しいDMSOをご使用ください。)

Ethanol : 6 mg/mL

モル濃度計算器

in vivo
Batch:

Add solvents to the product individually and in order.

投与溶液組成計算機

実験計算

モル濃度計算器

質量 濃度 体積 分子量

投与溶液組成計算機(クリア溶液)

ステップ１：実験データを入力してください。（実験操作によるロスを考慮し、動物数を1匹分多くして計算・調製することを推奨します）

mg/kg g μL 匹

ステップ２：投与溶媒の組成を入力してください。（ロット毎に適した溶解組成が異なる場合があります。詳細については弊社までお問い合わせください）

% DMSO % % Tween 80 % ddH2O
%DMSO %

計算結果：

投与溶媒濃度： mg/ml;

DMSOストック溶液調製方法： mg 試薬を μL DMSOに溶解する（濃度 mg/mL, 注：濃度が当該ロットのDMSO溶解度を超える場合はご連絡ください。 )

投与溶媒調製方法：Take μL DMSOストック溶液に μL PEG300，を加え、完全溶解後μL Tween 80，を加えて完全溶解させた後 μL ddH2O，を加え完全に溶解させます。

投与溶媒調製方法：μL DMSOストック溶液に μL Corn oil，を加え、完全溶解。

注意：１.ストック溶液に沈殿、混濁などがないことをご確認ください；
２.順番通りに溶剤を加えてください。次のステップに進む前に溶液に沈殿、混濁などがないことを確認してから加えてください。ボルテックス、ソニケーション、水浴加熱など物理的な方法で溶解を早めることは可能です。

技術サポート

ストックの作り方、阻害剤の保管方法、細胞実験や動物実験の際に注意すべき点など、製品を取扱う時に問い合わせが多かった質問に対しては取扱説明書でお答えしています。

Handling Instructions

他に質問がある場合は、お気軽にお問い合わせください。

* 必須

大学・企業名を記入してください
名前を記入してください
電子メール・アドレスを記入してください 有効なメールアドレスを入力してください
お問い合わせ内容をご入力ください
Tags: Sepantronium Bromide (YM155)を買う | Sepantronium Bromide (YM155) ic50 | Sepantronium Bromide (YM155)供給者 | Sepantronium Bromide (YM155)を購入する | Sepantronium Bromide (YM155)費用 | Sepantronium Bromide (YM155)生産者 | オーダーSepantronium Bromide (YM155) | Sepantronium Bromide (YM155)化学構造 | Sepantronium Bromide (YM155)分子量 | Sepantronium Bromide (YM155)代理店