Home 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) Chemical Structure

Sepantronium Bromide (YM155) Chemical Structure

CAS No. 781661-94-7

Purity & Quality Control

Sepantronium Bromide (YM155) Related Products

Signaling Pathway

Survivin Signaling Pathways

Survivin Signaling Pathway

Cell Data

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
Kasumi-1 Growth Inhibition Assay 72 h DMSO IC50=0.009 ± 0.0009 μM 25659731
M-07e Growth Inhibition Assay 72 h DMSO IC50=0.040 ± 0.013 μM 25659731
THP-1 Growth Inhibition Assay 72 h DMSO IC50=0.051 ± 0.013 μM 25659731
CMK Growth Inhibition Assay 72 h DMSO IC50=0.053 ± 0.009 μM 25659731
MV4-11 Growth Inhibition Assay 72 h DMSO IC50=0.055 ± 0.028 μM 25659731
AML-193 Growth Inhibition Assay 72 h DMSO IC50=0.462 ± 0.060 μM 25659731
HL-60 Growth Inhibition Assay 72 h DMSO IC50=0.001 ± 0.0002 μM 25659731
ML-2 Growth Inhibition Assay 72 h DMSO IC50=0.009 ± 0.002 μM 25659731
OCI/AML3 Growth Inhibition Assay 72 h DMSO IC50=0.011 ± 0.002 μM 25659731
HEL Growth Inhibition Assay 72 h DMSO IC50=0.559 ± 0.038 μM 25659731
ME-1 Growth Inhibition Assay 72 h DMSO IC50=0.684 ± 0.179 μM 25659731
THP-1 Apoptosis Assay 1 μM 72 h DMSO induces apoptosis 25659731
M-07e Function Assay 0–1 μM 72 h DMSO induces downregulation of Survivin 25659731
THP-1 Function Assay 0–1 μM 72 h DMSO induces downregulation of Survivin 25659731
CMK Function Assay 0–1 μM 72 h DMSO induces downregulation of Survivin 25659731
AML-193 Function Assay 0–1 μM 72 h DMSO induces downregulation of Survivin 25659731
Kasumi-1 Function Assay 0–1 μM 72 h DMSO induces downregulation of Survivin 25659731
MV4-11 Function Assay 0–1 μM 72 h DMSO induces downregulation of Survivin 25659731
MUG-Chor  Growth Inhibition Assay 0-5 μM 24/48 h IC50=7.05 nM for 48h 25640185
U-CH1  Growth Inhibition Assay 0-5 μM 24/48 h IC50=9.03 nM for 48h 25640185
KATOIII Growth Inhibition Assay 10/20 nM 48 h inhibits cell growth in a dose-dependent manner 25635055
AGS  Growth Inhibition Assay 10/20 nM 48 h inhibits cell growth in a dose-dependent manner 25635055
SACC-83 Function Assay 5 nM 48 h decreases nuclear expression of HIF-1α 25485635
INA-6 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
MOLP-8 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
NCI-H929 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
L-363 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
KMS-12-BM Growth Inhibition Assay 0-500 nM 48 h inhibits cell growth in a dose-dependent manner 25296978
SK-MM-2 Growth Inhibition Assay 0-500 nM 48 h inhibits cell growth in a dose-dependent manner 25296978
U-266 Apoptosis Assay 0-50 nM 24 h induces apoptosis 25296978
INA-6  Apoptosis Assay 0-50 nM 24 h induces apoptosis 25296978
MCF7 Growth Inhibition Assay 72 h IC50=13 ± 6 nM 25220225
MCF7-TamR6 Growth Inhibition Assay 72 h IC50=8 ± 6 nM 25220225
MCF7-TamR7 Growth Inhibition Assay 72 h IC50=8 ± 3 nM 25220225
MCF7-TamR8 Growth Inhibition Assay 72 h IC50=15 ± 6 nM 25220225
MCF7-TamC3 Growth Inhibition Assay 72 h IC50=6 ± 3 nM 25220225
MCF7-TamC6 Growth Inhibition Assay 72 h IC50=6 ± 0.1 nM 25220225
MDA-MB-231 Growth Inhibition Assay 72 h IC50=5 ± 1 nM 25220225
SK-BR-3 Growth Inhibition Assay 72 h IC50=7 ± 0.3 nM 25220225
Eca109 Function Assay 1-50 nM 48 h DMSO suppresses survivin expression in a dose dependent manner 25139395
TE13 Function Assay 1-50 nM 48 h DMSO suppresses survivin expression in a dose dependent manner 25139395
Eca109 Growth Inhibition Assay 0-100 nM 24/48 h DMSO decreases cell viability in a dose-dependent manner 25139395
TE13 Growth Inhibition Assay 0-100 nM 24/48 h DMSO decreases cell viability in a dose-dependent manner 25139395
MT-3 Kinase Assay 72 h DMSO IC50=2.86 ± 0.54 nM for DR4 expression 24866585
MDA-MB-468 Kinase Assay 72 h DMSO IC50=0.11 ± 0.01 nM for DR4 expression 24866585
SUM-159 Kinase Assay 72 h DMSO IC50=1.72 ± 0.33 nM for DR4 expression 24866585
MT-3 Kinase Assay 72 h DMSO IC50=54.11 ± 4.32 nM for DR5 expression 24866585
MDA-MB-468 Kinase Assay 72 h DMSO IC50=0.07 ± 0.02 nM for DR5 expression 24866585
SUM-159 Kinase Assay 72 h DMSO IC50=69.4 ± 4.23 nM for DR5 expression 24866585
MT-3 + NAC Kinase Assay 72 h DMSO IC50=56.2 ± 2.07 nM for DR5 expression 24866585
MT-3 + SB203580 Kinase Assay 72 h DMSO IC50=38.41 ± 5.02 nM for DR5 expression 24866585
DB Growth Inhibition Assay 10 nM 24 h DMSO inhibits cell proliferation 24486595
SU-DHL-8 Growth Inhibition Assay 10 nM 24 h DMSO inhibits cell proliferation 24486595
WSU-DLCL2 Growth Inhibition Assay 10 nM 24 h DMSO inhibits cell proliferation 24486595
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  DMSO IC50=20 nM, inhibits cell growth in a dose-dependent manner 24297644
T24 Growth Inhibition Assay 0-1000 nM 48 h  DMSO IC50=20 nM, inhibits cell growth in a dose-dependent manner 24297644
TSGH8301  Growth Inhibition Assay 0-1000 nM 48 h  DMSO IC50=20 nM, inhibits cell growth in a dose-dependent manner 24297644
BFTC909 Growth Inhibition Assay 0-1000 nM 48 h  DMSO IC50=20 nM, inhibits cell growth in a dose-dependent manner 24297644
BFTC905 Apoptosis Assay 20 nM 48 h DMSO induces apoptosis 24297644
BFTC905 Function Assay 20 nM 48 h DMSO decreases the expression of LC3B-II 24297644
A2780p Function Assay 0-100 nM 24 h DMSO induces Survivin downregulation  24262875
A2780cis Function Assay 0-100 nM 24 h DMSO induces Survivin downregulation  24262875
A2780p Apoptosis Assay 5-100 nM 24/48 h DMSO increases apoptosis in a concentration-dependent manner 24262875
A2780cis Apoptosis Assay 5-100 nM 24/48 h DMSO increases apoptosis in a concentration-dependent manner 24262875
SH-SY5Y Apoptosis Assay 1/10/100 µM 72 h DMSO induces apoptosis in a dose-dependent manner 24254560
HL-60 Growth Inhibition Assay 72 h DMSO IC50=0.3 nM 23618862
U937  Growth Inhibition Assay 72 h DMSO IC50=0.8 nM 23618862
HL-60  Function Assay 1 μM 6/12/24 h DMSO inhibits the expression of survivin 23618862
U937  Function Assay 1 μM 6/12/24 h DMSO inhibits the expression of survivin 23618862
HL-60 Apoptosis Assay 0.1/1 μM 8 h DMSO induces apoptosis 23618862
Sk-NEP-1  Growth Inhibition Assay 1-10000 nM 24 h DMSO IC50=100 nM 23267699
SK-NEP-1  Apoptosis Assay 50/100 nM 12/24 h DMSO induces apoptosis 23267699
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
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
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
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
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
Click to View More Cell Line Experimental Data

Biological Activity

Description 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
Cell Research Cell lines 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)
Concentrations ~ 100 nM
Incubation Time 48 hours
Method

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.
Experimental Result Images Methods Biomarkers Images 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]
Animal Research Animal Models PC-3 s.c. (orthotopic) xenografts in male nude mice (BALB/c nu/nu)
Dosages 5 mg/kg
Administration 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

Chemical Information & Solubility

Molecular Weight 443.29 Formula

C20H19BrN4O3
CAS No. 781661-94-7 SDF Download Sepantronium Bromide (YM155) SDF
Smiles CC1=[N+](C2=C(N1CCOC)C(=O)C3=CC=CC=C3C2=O)CC4=NC=CN=C4.[Br-]
Storage (From the date of receipt)

In vitro
Batch:

Water : 89 mg/mL

DMSO : 55 mg/mL ( (124.07 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 6 mg/mL


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In vivo
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