2. Cell Cycle/DNA Damage Apoptosis
  3. TOPK Apoptosis
  4. OTS514 hydrochloride

OTS514 hydrochloride is a highly potent TOPK inhibitor, which inhibits TOPK kinase activity with a median inhibitory concentration (IC50) value of 2.6 nM. OTS514 hydrochloride strongly suppresses the growth of TOPK-positive cancer cells. OTS514 hydrochloride induces cell cycle arrest and apoptosis.

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OTS514 hydrochloride

OTS514 hydrochloride Chemical Structure

CAS No. : 2319647-76-0

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OTS514 hydrochloride Related Antibodies

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Description

OTS514 hydrochloride is a highly potent TOPK inhibitor, which inhibits TOPK kinase activity with a median inhibitory concentration (IC50) value of 2.6 nM. OTS514 hydrochloride strongly suppresses the growth of TOPK-positive cancer cells[1]. OTS514 hydrochloride induces cell cycle arrest and apoptosis[2].

IC50 & Target

IC50: 2.6 nM (TOPK)[1]
Cellular Effect
Cell Line Type Value Description References
A549 IC50
19.52 nM
Compound: OTS514
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]
HCT-116 IC50
18.89 nM
Compound: OTS514
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
187.1 nM
Compound: OTS514
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]
In Vitro

OTS514 (1.5625-100 nM) induces cell cycle arrest and apoptosis at nanomolar concentrations in a series of human myeloma cell lines (HMCL) and prevents outgrowth of a putative CD138+ stem cell population from multiple myeloma (MM) patient-derived peripheral blood mononuclear cells[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

OTS514 hydrochloride Related Antibodies

Cell Viability Assay[2]

Cell Line: Human myeloma cell lines (MM1.S, MM1.R, RPMI 8226, 8226Dox40, KMS34, KMS34CFZ, KMS11, JJN3, LP-1, NCI H929, U266B1)
Concentration: 1.5625, 3.125, 6.25, 12.5, 25, 50, and 100 nM
Incubation Time: 72 hours
Result: IC50 values ranged from 11.6 to 29.4 nM in parental cell lines, indicating a potent inhibitory effect. Only the RPMI 8226-Dox40 cell line, which overexpresses the multi-drug resistance transporter gene ABCB1, was resistant.
In Vivo

OTS514 (1-5 mg/kg; once a day for 2 weeks; intravenous administration) induces tumor regression in a xenograft model of A549 cells (TOPK-positive lung cancer cells)[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Female BALB/cSLC-nu/nu mice bearing a xenograft model of A549 cells[1]
Dosage: 1, 2.5, and 5 mg/kg
Administration: Intravenously treated; once every day for 2 weeks
Result: Resulted in tumor growth inhibition (TGI) of 5.7, 43.3, and 65.3% on day 15, respectively, without any body weight loss.
Molecular Weight

400.92

Formula

C21H21ClN2O2S
CAS No.
SMILES

O=C1NC2=C(C(C3=CC=C([C@@H](C)CN)C=C3)=C(O)C=C2C)C4=C1SC=C4.[H]Cl
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
References
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OTS514 hydrochloride 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:

OTS5142319647-76-0OTS 514OTS-514TOPKApoptosisT-LAK cell-originated protein kinasepositivecancercellcyclearrestapoptosisHMCLmultiplemyelomaMMInhibitorinhibitorinhibit

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