Art. -Nr.: HY-18621

OTS514

4 Cited Publications

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Based on 4 publication(s) in Google Scholar

OTS514 is a highly potent TOPK inhibitor with an IC₅₀ of 2.6 nM. OTS514 strongly suppresses the growth of TOPK-positive cancer cells. OTS514 induces cell cycle arrest and apoptosis.

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Reinheit: 99.77%
CAS. Nr.: 1338540-63-8
Formel: C₂₁H₂₀N₂O₂S
Molecular Weight:364.46

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

OTS514 Chemical Structure

CAS. Nr.: 1338540-63-8

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Publications (4)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

OTS514 is a highly potent TOPK inhibitor with an IC₅₀ of 2.6 nM. OTS514 strongly suppresses the growth of TOPK-positive cancer cells^[1]. OTS514 induces cell cycle arrest and apoptosis^[2].

IC₅₀ & Target

IC50: 2.6 nM (TOPK)^[1]

Cellular Effect

Cell Line	Type	Value	Description	References
769-P	IC₅₀	20.7 nM Compound: OTS514	Cytotoxicity against human 769-P cells assessed as decrease in cell viability after 72 hrs by MTT assay Cytotoxicity against human 769-P cells assessed as decrease in cell viability after 72 hrs by MTT assay	[PMID: 30108692]
786-0	IC₅₀	44.1 nM Compound: OTS514	Cytotoxicity against human 786-O cells assessed as decrease in cell viability after 72 hrs by MTT assay Cytotoxicity against human 786-O cells assessed as decrease in cell viability after 72 hrs by MTT assay	[PMID: 30108692]
A2780	IC₅₀	10 nM Compound: OTS514	Cytotoxicity against human A2780 cells assessed as decrease in cell viability after 72 hrs by CCK8 assay Cytotoxicity against human A2780 cells assessed as decrease in cell viability after 72 hrs by CCK8 assay	[PMID: 30108692]
A549	IC₅₀	6.5 nM Compound: OTS514	Cytotoxicity against human A549 cells assessed as decrease in cell viability after 72 hrs by CCK8 assay Cytotoxicity against human A549 cells assessed as decrease in cell viability after 72 hrs by CCK8 assay	[PMID: 30108692]
BT-474	IC₅₀	6258 nM Compound: CICAMPA-10	Cytotoxicity against human BT-474 cells incubated for 48 hrs by CCK-8 reagent microplate reader assay Cytotoxicity against human BT-474 cells incubated for 48 hrs by CCK-8 reagent microplate reader assay	[PMID: 36827953]
CAKI-1	IC₅₀	27.8 nM Compound: OTS514	Cytotoxicity against human Caki1 cells assessed as decrease in cell viability after 72 hrs by MTT assay Cytotoxicity against human Caki1 cells assessed as decrease in cell viability after 72 hrs by MTT assay	[PMID: 30108692]
CAKI-2	IC₅₀	20.1 nM Compound: OTS514	Cytotoxicity against human Caki2 cells assessed as decrease in cell viability after 72 hrs by MTT assay Cytotoxicity against human Caki2 cells assessed as decrease in cell viability after 72 hrs by MTT assay	[PMID: 30108692]
Caov-3 cell line	IC₅₀	5.1 nM Compound: OTS514	Cytotoxicity against human Caov3 cells assessed as decrease in cell viability after 72 hrs by CCK8 assay Cytotoxicity against human Caov3 cells assessed as decrease in cell viability after 72 hrs by CCK8 assay	[PMID: 30108692]
CWR22R	IC₅₀	8 nM Compound: OTS514	Cytotoxicity against human 22Rv1 cells assessed as decrease in cell viability after 72 hrs by CCK8 assay Cytotoxicity against human 22Rv1 cells assessed as decrease in cell viability after 72 hrs by CCK8 assay	[PMID: 30108692]
Daudi	IC₅₀	3.7 nM Compound: OTS514	Cytotoxicity against human Daudi cells assessed as decrease in cell viability after 72 hrs by CCK8 assay Cytotoxicity against human Daudi cells assessed as decrease in cell viability after 72 hrs by CCK8 assay	[PMID: 30108692]
DU-4475	IC₅₀	6.4 nM Compound: OTS514	Cytotoxicity against human DU4475 cells assessed as decrease in cell viability after 72 hrs by CCK8 assay Cytotoxicity against human DU4475 cells assessed as decrease in cell viability after 72 hrs by CCK8 assay	[PMID: 30108692]
HCT-116	IC₅₀	4.8 nM Compound: OTS514	Cytotoxicity against human HCT116 cells assessed as decrease in cell viability after 72 hrs by CCK8 assay Cytotoxicity against human HCT116 cells assessed as decrease in cell viability after 72 hrs by CCK8 assay	[PMID: 30108692]
HepG2	IC₅₀	8.5 nM Compound: OTS514	Cytotoxicity against human HepG2 cells assessed as decrease in cell viability after 72 hrs by CCK8 assay Cytotoxicity against human HepG2 cells assessed as decrease in cell viability after 72 hrs by CCK8 assay	[PMID: 30108692]
K562	IC₅₀	36.8 nM Compound: OTS514	Cytotoxicity against human K562 cells assessed as decrease in cell viability after 48 hrs by MTT assay Cytotoxicity against human K562 cells assessed as decrease in cell viability after 48 hrs by MTT assay	[PMID: 30108692]
KG-1	IC₅₀	48.7 nM Compound: OTS514	Cytotoxicity against human KG1 cells assessed as decrease in cell viability after 48 hrs by MTT assay Cytotoxicity against human KG1 cells assessed as decrease in cell viability after 48 hrs by MTT assay	[PMID: 30108692]
KG-1a	IC₅₀	26.2 nM Compound: OTS514	Cytotoxicity against human KG1a cells assessed as decrease in cell viability after 48 hrs by MTT assay Cytotoxicity against human KG1a cells assessed as decrease in cell viability after 48 hrs by MTT assay	[PMID: 30108692]
Lu-99 cell line	IC₅₀	1.5 nM Compound: OTS514	Cytotoxicity against human LU99 cells assessed as decrease in cell viability after 72 hrs by CCK8 assay Cytotoxicity against human LU99 cells assessed as decrease in cell viability after 72 hrs by CCK8 assay	[PMID: 30108692]
MDA-MB-231	IC₅₀	14 nM Compound: OTS514	Cytotoxicity against human MDA-MB-231 cells assessed as decrease in cell viability after 72 hrs by CCK8 assay Cytotoxicity against human MDA-MB-231 cells assessed as decrease in cell viability after 72 hrs by CCK8 assay	[PMID: 30108692]
MIA PaCa-2	IC₅₀	5.2 nM Compound: OTS514	Cytotoxicity against human MIAPaCa2 cells assessed as decrease in cell viability after 72 hrs by CCK8 assay Cytotoxicity against human MIAPaCa2 cells assessed as decrease in cell viability after 72 hrs by CCK8 assay	[PMID: 30108692]
MKN-1	IC₅₀	4.6 nM Compound: OTS514	Cytotoxicity against human MKN1 cells assessed as decrease in cell viability after 72 hrs by CCK8 assay Cytotoxicity against human MKN1 cells assessed as decrease in cell viability after 72 hrs by CCK8 assay	[PMID: 30108692]
MKN-45	IC₅₀	6.1 nM Compound: OTS514	Cytotoxicity against human MKN45 cells assessed as decrease in cell viability after 72 hrs by CCK8 assay Cytotoxicity against human MKN45 cells assessed as decrease in cell viability after 72 hrs by CCK8 assay	[PMID: 30108692]
ML-2	IC₅₀	17.9 nM Compound: OTS514	Cytotoxicity against human ML2 cells assessed as decrease in cell viability after 48 hrs by MTT assay Cytotoxicity against human ML2 cells assessed as decrease in cell viability after 48 hrs by MTT assay	[PMID: 30108692]
MOLM-13	IC₅₀	9 nM Compound: OTS514	Cytotoxicity against human MOLM13 cells assessed as decrease in cell viability after 48 hrs by MTT assay Cytotoxicity against human MOLM13 cells assessed as decrease in cell viability after 48 hrs by MTT assay	[PMID: 30108692]
MV4-11	IC₅₀	10.7 nM Compound: OTS514	Cytotoxicity against human MV4-11 cells assessed as decrease in cell viability after 48 hrs by MTT assay Cytotoxicity against human MV4-11 cells assessed as decrease in cell viability after 48 hrs by MTT assay	[PMID: 30108692]
OV-90	IC₅₀	8.8 nM Compound: OTS514	Cytotoxicity against human OV90 cells assessed as decrease in cell viability after 72 hrs by CCK8 assay Cytotoxicity against human OV90 cells assessed as decrease in cell viability after 72 hrs by CCK8 assay	[PMID: 30108692]
OVCAR-3	IC₅₀	12 nM Compound: OTS514	Cytotoxicity against human OVCAR3 cells assessed as decrease in cell viability after 72 hrs by CCK8 assay Cytotoxicity against human OVCAR3 cells assessed as decrease in cell viability after 72 hrs by CCK8 assay	[PMID: 30108692]
PA-1	IC₅₀	5 nM Compound: OTS514	Cytotoxicity against human PA1 cells assessed as decrease in cell viability after 72 hrs by CCK8 assay Cytotoxicity against human PA1 cells assessed as decrease in cell viability after 72 hrs by CCK8 assay	[PMID: 30108692]
RMG-I	IC₅₀	15 nM Compound: OTS514	Cytotoxicity against human RMG-1 cells assessed as decrease in cell viability after 72 hrs by CCK8 assay Cytotoxicity against human RMG-1 cells assessed as decrease in cell viability after 72 hrs by CCK8 assay	[PMID: 30108692]
SK-OV-3	IC₅₀	6.3 nM Compound: OTS514	Cytotoxicity against human SKOV3 cells assessed as decrease in cell viability after 72 hrs by CCK8 assay Cytotoxicity against human SKOV3 cells assessed as decrease in cell viability after 72 hrs by CCK8 assay	[PMID: 30108692]
SW626	IC₅₀	9.4 nM Compound: OTS514	Cytotoxicity against human SW626 cells assessed as decrease in cell viability after 72 hrs by CCK8 assay Cytotoxicity against human SW626 cells assessed as decrease in cell viability after 72 hrs by CCK8 assay	[PMID: 30108692]
T47D	IC₅₀	8.4 nM Compound: OTS514	Cytotoxicity against human T47D cells assessed as decrease in cell viability after 72 hrs by CCK8 assay Cytotoxicity against human T47D cells assessed as decrease in cell viability after 72 hrs by CCK8 assay	[PMID: 30108692]
THP-1	IC₅₀	23.5 nM Compound: OTS514	Cytotoxicity against human THP1 cells assessed as decrease in cell viability after 48 hrs by MTT assay Cytotoxicity against human THP1 cells assessed as decrease in cell viability after 48 hrs by MTT assay	[PMID: 30108692]
U-937	IC₅₀	19.2 nM Compound: OTS514	Cytotoxicity against human U937 cells assessed as decrease in cell viability after 48 hrs by MTT assay Cytotoxicity against human U937 cells assessed as decrease in cell viability after 48 hrs by MTT assay	[PMID: 30108692]
UMUC3	IC₅₀	5.7 nM Compound: OTS514	Cytotoxicity against human UM-UC-3 cells assessed as decrease in cell viability after 72 hrs by CCK8 assay Cytotoxicity against human UM-UC-3 cells assessed as decrease in cell viability after 72 hrs by CCK8 assay	[PMID: 30108692]

In Vitro

OTS514 (1.5625-100 nM) induces cell cycle arrest and apoptosis at nanomolar concentrations in a series of human myeloma cell lines (HMCL) and prevents outgrowth of a putative CD138⁺ stem cell population from multiple myeloma (MM) patient-derived peripheral blood mononuclear cells^[2].

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

Cell Viability Assay^[2]

Cell Line:

Human myeloma cell lines (MM1.S, MM1.R, RPMI 8226, 8226Dox40, KMS34, KMS34CFZ, KMS11, JJN3, LP-1, NCI H929, U266B1)
Concentration:

1.5625, 3.125, 6.25, 12.5, 25, 50, and 100 nM
Incubation Time:

72 hours
Result:

IC₅₀ values ranged from 11.6 to 29.4 nM in parental cell lines, indicating a potent inhibitory effect. Only the RPMI 8226-Dox40 cell line, which overexpresses the multi-drug resistance transporter gene ABCB1, is resistant.

In Vivo

OTS514 (1-5 mg/kg; once a day for 2 weeks; intravenous administration) induces tumor regression in a xenograft model of A549 cells (TOPK-positive lung cancer cells)^[1].

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

Animal Model:

Female BALB/cSLC-nu/nu mice bearing a xenograft model of A549 cells^[1]
Dosage:

1, 2.5, and 5 mg/kg
Administration:

Intravenously treated; once every day for 2 weeks
Result:

Resulted in tumor growth inhibition (TGI) of 5.7, 43.3, and 65.3% on day 15, respectively, without any body weight loss.

Chemical Information

CAS. Nr. 1338540-63-8
Appearance Solid
Molecular Weight 364.46
Formel C₂₁H₂₀N₂O₂S
Color Off-white to light yellow
SMILES

O=C1NC2=C(C(C3=CC=C([C@@H](C)CN)C=C3)=C(O)C=C2C)C4=C1SC=C4
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Publications (4)

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Autophagy

PBK-Loaded secretory autophagosomes drive radiotherapy-induced systemic adipose depletion via MAPK/ERK-PRKA/PKA-LIPE/HSL signaling: a therapeutic target for esophageal cancer cachexia. [Abstract]

2026 Apr 23:1-26. PMID: 41988986
J Exp Clin Cancer Res

FYN/TOPK/HSPB1 axis facilitates the proliferation and metastasis of gastric cancer. [Abstract]

2023 Apr 4;42(1):80. PMID: 37016377
Bioorg Chem

Identification of FTY720 and COH29 as novel topoisomerase I catalytic inhibitors by experimental and computational studies. [Abstract]

2024 Jun:147:107412. PMID: 38696845
Research Square Print

December 5th, 2022.

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 12 mg/mL (32.93 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.7438 mL

13.7189 mL

27.4379 mL

5 mM

0.5488 mL

2.7438 mL

5.4876 mL

10 mM

0.2744 mL

1.3719 mL

2.7438 mL

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 2.5 mg/mL (6.86 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: ≥ 2.5 mg/mL (6.86 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.5 mg/mL (6.86 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (278 KB)
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Matsuo Y, et al. TOPK inhibitor induces complete tumor regression in xenograft models of human cancer through inhibition of cytokinesis. Sci Transl Med. 2014 Oct 22;6(259):259ra145. [Content Brief]

[2]. Stefka AT, et al. Potent anti-myeloma activity of the TOPK inhibitor OTS514 in pre-clinical models. Cancer Med. 2020 Jan;9(1):324-334. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.7438 mL	13.7189 mL	27.4379 mL	68.5946 mL
	5 mM	0.5488 mL	2.7438 mL	5.4876 mL	13.7189 mL
	10 mM	0.2744 mL	1.3719 mL	2.7438 mL	6.8595 mL
	15 mM	0.1829 mL	0.9146 mL	1.8292 mL	4.5730 mL
	20 mM	0.1372 mL	0.6859 mL	1.3719 mL	3.4297 mL
	25 mM	0.1098 mL	0.5488 mL	1.0975 mL	2.7438 mL
	30 mM	0.0915 mL	0.4573 mL	0.9146 mL	2.2865 mL

Keywords

OTS514

4 Cited Publications

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OTS514

MCE Bioactive Compound Library

Publications Citing Use of MedChemExpress (MCE) OTS514

Biologische Aktivität

Chemical Information

Publications (4)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

OTS514

MCE Bioactive Compound Library

Publications Citing Use of MedChemExpress (MCE) OTS514

Biologische Aktivität

Chemical Information

Publications (4)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

OTS514 Related Classifications

HY-18621 Related Classifications