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OTS964 TOPK inhibitor

Name: OTS964
Brand: Selleck Chemicals
SKU: S7648
Availability: InStock
Rating: 5 (8 reviews)

Cat.No.S7648

OTS964 is a potent TOPK inhibitor with high affinity and selectivity and IC50 value is 28 nM. This compound is also a potent inhibitor of the cyclin-dependent kinase CDK11 with Kd of 40 nM. This chemical treatment activates autophagy in glioma cells and induces apoptosis of human lung cancer cells in mouse xenografts.

Chemical Structure

Molecular Weight: 428.97

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Quality Control

Batch: Purity: 99.64%

99.64

Related Targets	ERK p38 MAPK Raf JNK MEK Ras KRas S6 Kinase MAP4K TAK1
Other TOPK Inhibitors	OTS514 hydrochloride HI-TOPK-032

Solubility

In vitro
Batch:

DMSO : 30 mg/mL (69.93 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : Insoluble

Ethanol : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
Mass value Mass unit	Concentration value Concentration unit	Volume value Volume unit	Molecular weight (g/mol)

Dilution Calculator Molecular Weight Calculator

In vivo batch selection In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	1.100mg/ml (2.56mM)
	5% DMSO 1 95% Corn oil Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	0.250mg/ml (0.58mM)

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg

Average weight of animals: g

Dosing volume per animal: μL

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Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO

% Tween 80

% ddH₂O

% DMSO

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Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

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 ddH₂O, 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.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Chemical Information, Storage & Stability

Molecular Weight	428.97	Formula	C₂₃H₂₄N₂O₂S.HCl	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	1338545-07-5	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	N/A			Smiles	CC1=CC(=C(C2=C1NC(=O)C3=C2C=CS3)C4=CC=C(C=C4)C(C)CN(C)C)O.Cl

Mechanism of Action

Targets/IC₅₀/Ki	TOPK (Cell-free assay) 28 nM CDK11B (Cell-free assay) 40 nM(Kd)
In vitro	OTS964 inhibits the growth of TOPK-positive cells with low IC50 values [A549 (31 nM), LU-99 (7.6 nM), DU4475 (53 nM), MDAMB- 231 (73 nM), T47D (72 nM), Daudi (25 nM), UM-UC-3 (32 nM), HCT-116 (33 nM),MKN1 (38 nM), MKN45 (39 nM), HepG2 (19 nM), MIAPaca-2 (30 nM), and 22Rv1 (50 nM)], whereas its growth inhibitory effect against TOPK-negative HT29 cancer cells is significantly weaker, with IC50 of 290nM. Although this compound reveals some suppressive effect on Src family kinases, the response to this chemical in these cancer cells is not correlated with the expression of Src family kinases c-Src, Fyn, and Lyn, supporting the TOPK-dependent growth inhibitory effects of this compound. Time lapse imaging in T47D cells shows that treatment with this agent induces cytokinesis defects followed by apoptosis.
In vivo	Although administration of the free compound induces hematopoietic adverse reactions (leukocytopenia associated with thrombocytosis), the drug delivered in a liposomal formulation effectively causes complete regression of transplanted tumors without showing any adverse reactions in mice. Inhibition of TOPK activity with the liposomal formulation suppresses tumor growth through induction of cytokinesis defects and subsequent apoptosis. Although oral administration of this compound causes some hematopoietic toxicity, this is a transient effect. The spontaneous recovery from leukocytopenia is occured and the anticancer effectiveness of the oral drug is similar to that of the liposomal formulation, oral administration of the drug may prove to be more practical.
References	[1] https://pubmed.ncbi.nlm.nih.gov/25338756/ [2] https://pubmed.ncbi.nlm.nih.gov/31511426/

Applications

Methods	Biomarkers	Images	PMID
Western blot	p62 / LC3-I / LC-3Ⅱ / p-Histone H3 / Histone H3 / TOPK ULK1 / p-ATG13 / ATG13 / p-Beclin-1 / Beclin-1		31378785

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