OTS964 hydrochloride
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 Kd of 40 nM.
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- Pureza: 99.05%
- No. CAS: 1338545-07-5
- Fòrmula: C23H25ClN2O2S
- Peso molecular:428.97
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Almacenamiento:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 2 years; -20°C, 1 year (sealed storage, away from moisture)
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
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Publications Citing Use of MedChemExpress (MCE) OTS964 hydrochloride
More- Nature. 2022 Sep;609(7928):829-834. [Abstract]
- Cell. 2021 Jun 10;184(12):3143-3162.e32. [Abstract]
- Mol Cell. 2025 Sep 4;85(17):3256-3274.e14. [Abstract]
- Adv Sci (Weinh). 2024 Apr;11(14):e2308496. [Abstract]
- Cell Death Dis. 2019 Aug 5;10(8):583. [Abstract]
- J Eur Acad Dermatol Venereol. 2024 May;38(5):851-863. [Abstract]
- Mol Cell Proteomics. 2025 May 12:100991. [Abstract]
- Cancers (Basel). 2026 Jan 14;18(2):261. [Abstract]
- iScience. 2023 Jun 20;26(7):107185. [Abstract]
- bioRxiv. 2026 Mar 26.
- bioRxiv. 2025 Nov 20.
- bioRxiv. 2025 Sep 28.
- SSRN. 2022 Nov 21.
Customer Validation & Images
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Cell Proliferation/Viability Assay
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Flow Cytometry
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WB
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WB
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WB
Actividad biológica
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TOPK 28 nM (IC50) |
CDK11B 40 nM (Kd) |
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.
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Cell Line:LU-99 cells
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Concentration:10 nM
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Incubation Time:48 hours
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Result:Suppressed cancer cell proliferation.
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Cell Line:LU-99 cells
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Concentration:10 nM
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Incubation Time:48 hours
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Result:Increased cancer cell death.
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Cell Line:Hs683 cells, H4 cells
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Concentration:0.1, 1, 2 μM
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Incubation Time:24 and 48 hours
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Result:Increased the expression of LC3-II and decreased the expression of P62, both in a dose-dependent manner.
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.
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Animal Model:Nude mice bearing LU-99 lung cancer cells[1]
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Dosage:40 mg/kg
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Administration:Intravenously; on days 1, 4, 8, 11, 15, and 18
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Result:The tumors continued shrinking even after the treatment and finally revealed complete regression.
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Animal Model:Nude mice bearing LU-99 lung cancer cells[1]
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Dosage:50 or 100 mg/kg
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Administration:Oral administration; once every day for 2 weeks
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Result:Achieved complete tumor regression.
Chemical Information
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No. CAS 1338545-07-5
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Appearance Solid
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Peso molecular 428.97
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Fòrmula C23H25ClN2O2S
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Color Off-white to light yellow
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SMILES
OC1=CC(C)=C2C(C3=C(SC=C3)C(N2)=O)=C1C4=CC=C([C@@H](C)CN(C)C)C=C4.Cl
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
4°C, sealed storage, away from moisture
* In solvent : -80°C, 2 years; -20°C, 1 year (sealed storage, away from moisture)
Publications (13)
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Journal Impact Factor
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Most Recent
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Nature
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 RNAPIICTD phosphorylation at Tyr1, Ser2, Thr4, Ser5 and Ser7 in HCT116 cells.
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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.
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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
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.
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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)
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 -
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Solvente y solubilidad
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.
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- 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.
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.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
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.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%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
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL. * In solvent : -80°C, 2 years; -20°C, 1 year (sealed storage, away from moisture)
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Pureza y Documentación
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Ficha de datos (281 KB)
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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)
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Instrucciones de manejo (2659 KB)
Referencias
[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]
Complete Stock Solution Preparation Table
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.
| 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.
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