1. Cell Cycle/DNA Damage
    Apoptosis
  2. TOPK
    CDK
    Apoptosis
  3. OTS964

OTS964 

Cat. No.: HY-19718
Handling Instructions

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 Kd of 40 nM.

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

OTS964 Chemical Structure

OTS964 Chemical Structure

CAS No. : 1338542-14-5

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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 Kd of 40 nM[2].

IC50 & Target[1][2]

TOPK

28 nM (IC50)

CDK11B

40 nM (Kd)

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].

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].

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([[email protected]@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.

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Keywords:

OTS964OTS 964OTS-964TOPKCDKApoptosisT-LAK cell-originated protein kinaseCyclin dependent kinaseInhibitorinhibitorinhibit

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