OTS964 hydrochloride

Name: OTS964 hydrochloride
Brand: MedChemExpress
SKU: HY-12467
Rating: 5.0 (13 reviews)

Cat. No.: HY-12467 Purity: 99.05%: Data Sheet
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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.

For research use only. We do not sell to patients.

CAS No. : 1338545-07-5

Size	Stock	Quantity

Free Sample (0.1 - 0.2 mg)	Apply Now
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	In-stock	Estimated Time of Arrival: December 31
10 mg	In-stock	Estimated Time of Arrival: December 31
25 mg	In-stock	Estimated Time of Arrival: December 31
50 mg	In-stock	Estimated Time of Arrival: December 31
100 mg	In-stock	Estimated Time of Arrival: December 31
200 mg	Get quote
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Customer Review

Based on 13 publication(s) in Google Scholar

Other Forms of OTS964 hydrochloride:

OTS964 Get quote

13 Publications Citing Use of MCE OTS964 hydrochloride

Cell Proliferation/Viability Assay

Flow Cytometry

: 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.

: 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.

: 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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Biological Activity
Purity & Documentation
References
Customer Review

Description

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)

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.

Molecular Weight

428.97

Formula

C₂₃H₂₅ClN₂O₂S

CAS No.

1338545-07-5

Appearance

Solid

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, sealed storage, away from moisture

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

Solvent & Solubility

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.

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

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

View the 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.

* 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.

Molarity Calculator
Dilution Calculator

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

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

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.

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.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
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.
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.
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

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

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

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

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).

Calculation results:

Working solution concentration: 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)

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

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.

Purity & Documentation

Purity: 99.74%

Select Batch:

Data Sheet (281 KB) SDS (394 KB)

COA (253 KB) HNMR (269 KB) LCMS (94 KB)

Handling Instructions (2659 KB)

References

[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

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.