Art. -Nr.: HY-12467

OTS964 hydrochloride

13 Cited Publications

Kundenbewertung

Based on 13 publication(s) in Google Scholar

OTS964 hydrochloride is an orally active, high affinity and selective TOPK (T-lymphokine-activated killer cell-originated protein kinase) inhibitor with an IC₅₀ of 28 nM. OTS964 hydrochloride is also a potent inhibitor of the cyclin-dependent kinase CDK11, which binds to CDK11B with a K_d of 40 nM.

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Reinheit: 99.05%
CAS. Nr.: 1338545-07-5
Formel: C₂₃H₂₅ClN₂O₂S
Molecular Weight:428.97

Speicherung:

4°C, sealed storage, away from moisture

* In solvent : -80°C, 2 years; -20°C, 1 year (sealed storage, away from moisture)

OTS964 hydrochloride Chemical Structure

CAS. Nr.: 1338545-07-5

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Publications (13)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

OTS964 hydrochloride is an orally active, high affinity and selective TOPK (T-lymphokine-activated killer cell-originated protein kinase) inhibitor with an IC₅₀ of 28 nM^[1]. OTS964 hydrochloride is also a potent inhibitor of the cyclin-dependent kinase CDK11, which binds to CDK11B with a K_d of 40 nM^[2].

IC₅₀ & Target^[1]^[2]

TOPK

28 nM (IC₅₀)

CDK11B

40 nM (Kd)

Alle CDK Isoform-spezifische Produkte anzeigen :

In Vitro

OTS964 hydrochloride (10 nM; 48 hours) suppresses cancer cell proliferation^[1].
OTS964 hydrochloride (10 nM; 48 hours) increases cancer cell death^[1].
OTS964 (0.1-2 μM; 24 and 48 hours) increases the expression of LC3-II and decreases the expression of P62, both in a dose-dependent manner^[3].

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

Cell Proliferation Assay^[1]

Cell Line:

LU-99 cells
Concentration:

10 nM
Incubation Time:

48 hours
Result:

Suppressed cancer cell proliferation.

Apoptosis Analysis^[1]

Cell Line:

LU-99 cells
Concentration:

10 nM
Incubation Time:

48 hours
Result:

Increased cancer cell death.

Western Blot Analysis^[3]

Cell Line:

Hs683 cells, H4 cells
Concentration:

0.1, 1, 2 μM
Incubation Time:

24 and 48 hours
Result:

Increased the expression of LC3-II and decreased the expression of P62, both in a dose-dependent manner.

In Vivo

OTS964 hydrochloride (intravenously; 40 mg/kg on days 1, 4, 8, 11, 15, and 18) makes tumors shrinking even after the treatment and finally revealing complete regression^[1].
OTS964 hydrochloride (oral administration; 50 or 100 mg/kg/day for 2 weeks) ultimately achieves complete tumor regression^[1].

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

Animal Model:

Nude mice bearing LU-99 lung cancer cells^[1]
Dosage:

40 mg/kg
Administration:

Intravenously; on days 1, 4, 8, 11, 15, and 18
Result:

The tumors continued shrinking even after the treatment and finally revealed complete regression.

Animal Model:

Nude mice bearing LU-99 lung cancer cells^[1]
Dosage:

50 or 100 mg/kg
Administration:

Oral administration; once every day for 2 weeks
Result:

Achieved complete tumor regression.

Chemical Information

CAS. Nr. 1338545-07-5
Appearance Solid
Molecular Weight 428.97
Formel C₂₃H₂₅ClN₂O₂S
Color Off-white to light yellow
SMILES

OC1=CC(C)=C2C(C3=C(SC=C3)C(N2)=O)=C1C4=CC=C([C@@H](C)CN(C)C)C=C4.Cl
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

4°C, sealed storage, away from moisture

* In solvent : -80°C, 2 years; -20°C, 1 year (sealed storage, away from moisture)

Publications (13)

All WBCell Proliferation/Viability AssayFlow Cytometry

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Journal Impact Factor

Nature

CDK11 regulates pre-mRNA splicing by phosphorylation of SF3B1. [Abstract]

2022 Sep;609(7928):829-834. PMID: 36104565

OTS964 hydrochloride purchased from MedChemExpress. Usage Cited in: Nature. 2022 Sep;609(7928):829-834. [Abstract]

OTS964 hydrochloride (0, 10, 30, 100, 250, 500, 2000 nM; 4 h) decreased the total RNAPII^CTD phosphorylation at Tyr1, Ser2, Thr4, Ser5 and Ser7 in HCT116 cells.
Cell

The PP2A-Integrator-CDK9 axis fine-tunes transcription and can be targeted therapeutically in cancer. [Abstract]

2021 Jun 10;184(12):3143-3162.e32. PMID: 34004147
Mol Cell

A CDK11-dependent RNA polymerase II pause-checkpoint precedes CDK9-mediated transition to transcriptional elongation. [Abstract]

2025 Sep 4;85(17):3256-3274.e14. PMID: 40858114

OTS964 hydrochloride purchased from MedChemExpress. Usage Cited in: Mol Cell. 2025 Sep 4;85(17):3256-3274.e14. [Abstract]

OTS964 hydrochloride (0-1000 nM; 48 h) dose-dependent increases in cell death in THP1 and MV4;11 cells.

OTS964 hydrochloride purchased from MedChemExpress. Usage Cited in: Mol Cell. 2025 Sep 4;85(17):3256-3274.e14. [Abstract]

OTS964 hydrochloride (39 nM; 24 h) induced cell cycle arrest at G1 phase in THP1 FUCCI cells.
Adv Sci (Weinh)

Zygotic Splicing Activation of the Transcriptome is a Crucial Aspect of Maternal-to-Zygotic Transition and Required for the Conversion from Totipotency to Pluripotency. [Abstract]

2024 Apr;11(14):e2308496. PMID: 38308190
Cell Death Dis

TOPK inhibits autophagy by phosphorylating ULK1 and promotes glioma resistance to TMZ. [Abstract]

2019 Aug 5;10(8):583. PMID: 31378785

OTS964 hydrochloride purchased from MedChemExpress. Usage Cited in: Cell Death Dis. 2019 Aug 5;10(8):583. [Abstract]

OTS964 hydrochloride (0, 0.1, 1, 2 μM; 24, 48 h) inhibited cells viability and increased the expression of LC3-II and decreased the expression of P62, and both were in a dose-dependent manner in Hs683 cells.

OTS964 hydrochloride purchased from MedChemExpress. Usage Cited in: Cell Death Dis. 2019 Aug 5;10(8):583. [Abstract]

OTS964 hydrochloride (0, 0.1, 1, 2 μM; 24, 48 h) inhibited cells viability and increased the expression of LC3-II and decreased the expression of P62, and both were in a dose-dependent manner in H4 cells.

OTS964 hydrochloride purchased from MedChemExpress. Usage Cited in: Cell Death Dis. 2019 Aug 5;10(8):583. [Abstract]

OTS964 hydrochloride (1 μM; 48 h) activated autophagy initiation without affecting autophagic flux in Hs683 (left) and H4 (right) cells. Baf A1 (50 nM) was added 5 h before the cells were harvested.

OTS964 hydrochloride purchased from MedChemExpress. Usage Cited in: Cell Death Dis. 2019 Aug 5;10(8):583. [Abstract]

OTS964 hydrochloride (0, 0.1, 1, 2 μM; 48 h) increased the expression of ULK1 and the levels of p-ATG13 and p-Beclin-1 in a dose-dependent manner in Hs683 (left) and H4 (right) cells.
J Eur Acad Dermatol Venereol

TOPK promotes the development of psoriasis and worenine alleviates psoriasiform dermatitis by inhibiting TOPK activity. [Abstract]

2024 May;38(5):851-863. PMID: 38131517
Mol Cell Proteomics

Proteomics and Phosphoproteomics Revealed Dysregulated Kinases and Potential Therapy for Liver Fibrosis. [Abstract]

2025 May 12:100991. PMID: 40368138
Cancers (Basel)

Targeting CDK11 in Rhabdoid Tumor of the Kidney. [Abstract]

2026 Jan 14;18(2):261. PMID: 41595181
iScience

TOPK mediates immune evasion of renal cell carcinoma via upregulating the expression of PD-L1. [Abstract]

2023 Jun 20;26(7):107185. PMID: 37404377
bioRxiv

2026 Mar 26.
bioRxiv

2025 Nov 20.
bioRxiv

2025 Sep 28.
SSRN

2022 Nov 21.

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : ≥ 83.33 mg/mL (194.26 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H₂O : 2 mg/mL (4.66 mM; ultrasonic and warming and heat to 60°C)

* "≥" means soluble, but saturation unknown.

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

2.3312 mL

11.6558 mL

23.3117 mL

5 mM

0.4662 mL

2.3312 mL

4.6623 mL

10 mM

0.2331 mL

1.1656 mL

2.3312 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 (sealed storage, away from moisture). When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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 (5.83 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 (5.83 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 (5.83 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 (281 KB)
SDS (394 KB)
- English - EN (394 KB)
- Français - FR (394 KB)
- Deutsch - DE (394 KB)
- Norwegian - NO (394 KB)
- Español - ES (394 KB)
- Swedish - SV (394 KB)
- Italian - IT (394 KB)
- Korean - KR (394 KB)
- Portuguese - PT (394 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 ofcytokinesis. Sci Transl Med. 2014 Oct 22;6(259):259ra145. [Content Brief]

[2]. Lin A, et al. Off-target toxicity is a common mechanism of action of cancer drugs undergoing clinical trials. Sci Transl Med. 2019 Sep 11;11(509). [Content Brief]

[3]. Lu H, et al. TOPK inhibits autophagy by phosphorylating ULK1 and promotes glioma resistance to TMZ. Cell Death Dis. 2019 Aug 5;10(8):583. [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

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
H₂O / DMSO	1 mM	2.3312 mL	11.6558 mL	23.3117 mL	58.2791 mL
DMSO	5 mM	0.4662 mL	2.3312 mL	4.6623 mL	11.6558 mL
	10 mM	0.2331 mL	1.1656 mL	2.3312 mL	5.8279 mL
	15 mM	0.1554 mL	0.7771 mL	1.5541 mL	3.8853 mL
	20 mM	0.1166 mL	0.5828 mL	1.1656 mL	2.9140 mL
	25 mM	0.0932 mL	0.4662 mL	0.9325 mL	2.3312 mL
	30 mM	0.0777 mL	0.3885 mL	0.7771 mL	1.9426 mL
	40 mM	0.0583 mL	0.2914 mL	0.5828 mL	1.4570 mL
	50 mM	0.0466 mL	0.2331 mL	0.4662 mL	1.1656 mL
	60 mM	0.0389 mL	0.1943 mL	0.3885 mL	0.9713 mL
	80 mM	0.0291 mL	0.1457 mL	0.2914 mL	0.7285 mL
	100 mM	0.0233 mL	0.1166 mL	0.2331 mL	0.5828 mL

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

Keywords

OTS964 hydrochloride

13 Cited Publications

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OTS964 hydrochloride

Apoptosis Compound Library

Cell Cycle/DNA Damage Compound Library

Kinase Inhibitor Library

Anti-Cancer Compound Library

Anti-Aging Compound Library

Orally Active Compound Library

Anti-Breast Cancer Compound Library

Anti-Blood Cancer Compound Library

Targeted Diversity Library

Cancer Stem Cells Compound Library

Heterocyclic Compound Library

Highly Selective Inhibitors Library

Highly Selective Activators Library

Cell Death Library

Serine/Threonine Kinase Inhibitor Library

Anti-Hematopathy Compound Library

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Anti-Aging Compound Library Mini

Kinase Inhibitor Library Mini

MCE Bioactive Compound Library

Bioactive Compound Library

Anti-Brain Cancer Compound Library

Protein Kinase Compound Library

Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library

Cell Proliferation Compound Library

High-Throughput Bioactive Compound Library

Posttranslational Modification Library

High-Efficiency Gene Editing Compound Library

Publications Citing Use of MedChemExpress (MCE) OTS964 hydrochloride

Alle CDK Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (13)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

OTS964 hydrochloride Related Classifications

HY-12467 Related Classifications