2. OTS964

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.

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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

IC50: 28 nM (TOPK)[1]
Kd: 40 nM (CDK11B)[2]
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.

OTS964 Related Antibodies

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.
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
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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-964Inhibitorinhibitorinhibit

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