Home MAPK TOPK inhibitor - Apoptosis related activator OTS514 hydrochloride For research use only.

OTS514 hydrochloride

OTS514 is a highly potent TOPK(T-LAK cell-originated protein kinase) inhibitor with an IC50 value of 2.6 nM. OTS514 induces cell cycle arrest and apoptosis.

OTS514 hydrochloride Chemical Structure

OTS514 hydrochloride Chemical Structure

CAS: 2319647-76-0

Selleck's OTS514 hydrochloride has been cited by 11 publications

Purity & Quality Control

Batch: S765201 DMSO] 80 mg/mL] false] Water] 80 mg/mL] false] Ethanol] 5 mg/mL] false Purity: 99.42%
99.42

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Biological Activity

Description OTS514 is a highly potent TOPK(T-LAK cell-originated protein kinase) inhibitor with an IC50 value of 2.6 nM. OTS514 induces cell cycle arrest and apoptosis.
Targets
TOPK [2]
(Cell-free assay)
2.6 nM
In vitro
In vitro OTS514 has growth inhibitory effect on five kidney cancer cell lines, VMRC-RCW, Caki-1, Caki-2, 769-P and 786-O, in which TOPK was highly expressed. The IC50 values range from 19.9 to 44.1 nM[1]. OTS514 strongly suppressed the growth of TOPK-positive cancer cells. It also shows significant growth-inhibitory effect on ovarian cancer cell lines with IC50 values of 3.0 to 46 nM[3].
Cell Research Cell lines CD34+ HSCs
Concentrations 20 or 40 nM
Incubation Time 48 h
Method Cells were cultured in RPMI supplemented with 20% fetal bovine serum and 1×StemSpan CC100. Cells were treated with OTS514 (20 or 40 nM) or OTS964 (100 or 200 nM) for 48 hours. Collected cells were washed with PBS and resuspended in 100 ml of PBS followed by staining with CD41a antibody for 20 min at room temperature. Finally, the cells were washed with PBS again and then analyzed for CD41a staining by flow cytometry. Expression of STAT5 was examined by Western blot with an anti-STAT5 antibody.
Experimental Result Images Methods Biomarkers Images PMID
Western blot TOPK p-FOXM1 / FOXM1 28075524
Growth inhibition assay Cell viability 28075524
In Vivo
In vivo Mouse xenograft studies with human lung cancer cells demonstrated the in vivo efficacy of OTS514 but found that the compound also caused severe hematopoietic toxicity [reduction of red blood cells (RBCs) and white blood cells (WBCs) associated with marked increase in platelets][2]. Oral administration of OTS514 significantly elongated overall survival in the ES-2 abdominal dissemination xenograft model, compared with vehicle control (P < 0.001)[3].
Animal Research Animal Models BALB/cSLC-nu/nu mice
Dosages 1, 2.5, and 5 mg/kg
Administration IV or oral gavage

Chemical Information & Solubility

Molecular Weight 400.92 Formula

C21H20N2O2S.HCl
CAS No. 2319647-76-0 SDF Download OTS514 hydrochloride SDF
Smiles Cl.CC(CN)C1=CC=C(C=C1)C2=C3C(=C(C)C=C2O)NC(=O)C4=C3C=CS4
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 80 mg/mL ( (199.54 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : 80 mg/mL

Ethanol : 5 mg/mL


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Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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