1. Cell Cycle/DNA Damage
    Apoptosis
  2. TOPK
    Apoptosis
  3. OTS514

OTS514 

Cat. No.: HY-18621 Purity: 95.63%
Handling Instructions

OTS514 is a highly potent TOPK inhibitor with an IC50 of 2.6 nM. OTS514 strongly suppresses the growth of TOPK-positive cancer cells. OTS514 induces cell cycle arrest and apoptosis.

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

OTS514 Chemical Structure

OTS514 Chemical Structure

CAS No. : 1338540-63-8

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 212 In-stock
Estimated Time of Arrival: December 31
2 mg USD 132 In-stock
Estimated Time of Arrival: December 31
5 mg USD 264 In-stock
Estimated Time of Arrival: December 31
10 mg USD 432 In-stock
Estimated Time of Arrival: December 31
25 mg USD 912 In-stock
Estimated Time of Arrival: December 31
50 mg USD 1560 In-stock
Estimated Time of Arrival: December 31
100 mg USD 2520 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

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Customer Review

Based on 1 publication(s) in Google Scholar

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Description

OTS514 is a highly potent TOPK inhibitor with an IC50 of 2.6 nM. OTS514 strongly suppresses the growth of TOPK-positive cancer cells[1]. OTS514 induces cell cycle arrest and apoptosis[2].

IC50 & Target

IC50: 2.6 nM (TOPK)[1]

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].

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, is 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].

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

364.46

Formula

C₂₁H₂₀N₂O₂S

CAS No.

1338540-63-8

SMILES

O=C1NC2=C(C(C3=CC=C([[email protected]@H](C)CN)C=C3)=C(O)C=C2C)C4=C1SC=C4

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (274.38 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.7438 mL 13.7189 mL 27.4379 mL
5 mM 0.5488 mL 2.7438 mL 5.4876 mL
10 mM 0.2744 mL 1.3719 mL 2.7438 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (6.86 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.5 mg/mL (6.86 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (6.86 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
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Keywords:

OTS514OTS 514OTS-514TOPKApoptosisT-LAK cell-originated protein kinasepositivecancercellcyclearrestapoptosisHMCLmultiplemyelomaMMInhibitorinhibitorinhibit

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OTS514
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