OTS964

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OTS964 is an orally active, high affinity and selective TOPK inhibitor with an IC₅₀ of 28 nM. OTS964 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. : 1338542-14-5

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Other In-stock Forms of OTS964:

OTS964 hydrochloride

Other Forms of OTS964:

OTS964 hydrochloride In-stock

13 Publications Citing Use of MCE OTS964

Cell Proliferation/Viability Assay

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: OTS964 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 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 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 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 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 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 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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Description

OTS964 is an orally active, high affinity and selective TOPK inhibitor with an IC₅₀ of 28 nM^[1]. OTS964 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)

Cellular Effect

Cell Line	Type	Value	Description	References
A549	IC₅₀	20.41 nM Compound: OTS964	Antiproliferative activity against human A549 cells after 72 hrs by MTT assay Antiproliferative activity against human A549 cells after 72 hrs by MTT assay	[PMID: 30453248]
A549	IC₅₀	31 nM Compound: OTS964	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]
CWR22R	IC₅₀	50 nM Compound: OTS964	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]
DU-4475	IC₅₀	53 nM Compound: OTS964	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]
Daudi	IC₅₀	25 nM Compound: OTS964	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]
HCT-116	IC₅₀	33 nM Compound: OTS964	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]
HCT-116	IC₅₀	45 nM Compound: OTS964	Antiproliferative activity against human HCT116 cells after 72 hrs by MTT assay Antiproliferative activity against human HCT116 cells after 72 hrs by MTT assay	[PMID: 30453248]
HCT-15	IC₅₀	73.08 nM Compound: OTS964	Antiproliferative activity against human HCT15 cells after 72 hrs by MTT assay Antiproliferative activity against human HCT15 cells after 72 hrs by MTT assay	[PMID: 30453248]
HepG2	IC₅₀	19 nM Compound: OTS964	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]
MDA-MB-231	IC₅₀	73 nM Compound: OTS964	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	30 nM Compound: OTS964	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	38 nM Compound: OTS964	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	39 nM Compound: OTS964	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]
T47D	IC₅₀	72 nM Compound: OTS964	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]
UMUC3	IC₅₀	32 nM Compound: OTS964	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

OTS964 (10 nM; 48 hours) suppresses cancer cell proliferation^[1].
OTS964 (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 (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 (oral administration; 50 or 100 mg/kg/day for 2 weeks) 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

392.51

Formula

C₂₃H₂₄N₂O₂S

CAS No.

1338542-14-5

SMILES

O=C(N1)C2=C(C=CS2)C3=C1C(C)=CC(O)=C3C4=CC=C([C@@H](C)CN(C)C)C=C4

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation

Handling Instructions (2659 KB)

References

[1]. Matsuo Y , et al. TOPK inhibitor induces complete tumor regression in xenograft models of human cancerthrough inhibition of cytokinesis. 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]

OTS964 Related Classifications

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Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

OTS9641338542-14-5OTS 964OTS-964TOPKCDKApoptosisT-LAK cell-originated protein kinaseCyclin dependent kinaseInhibitorinhibitorinhibit

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