1. Epigenetics
  2. Histone Methyltransferase
  3. OTS186935 hydrochloride

OTS186935 hydrochloride 

Cat. No.: HY-122181B Purity: 99.86%
Handling Instructions

OTS186935 hydrochloride is a potent protein methyltransferase SUV39H2 inhibitor with an IC50 of 6.49 nM. OTS186935 hydrochloride shows significant inhibition of tumor growth in mouse xenograft models without any detectable toxicity. OTS193320 hydrochloride regulates the production of γ-H2AX in cancer cells.

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OTS186935 hydrochloride Chemical Structure

OTS186935 hydrochloride Chemical Structure

Size Price Stock Quantity
10 mM * 1  mL in DMSO USD 345 In-stock
Estimated Time of Arrival: December 31
5 mg USD 300 In-stock
Estimated Time of Arrival: December 31
10 mg USD 500 In-stock
Estimated Time of Arrival: December 31
50 mg USD 1400 In-stock
Estimated Time of Arrival: December 31
100 mg USD 1950 In-stock
Estimated Time of Arrival: December 31
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Based on 1 publication(s) in Google Scholar

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Description

OTS186935 hydrochloride is a potent protein methyltransferase SUV39H2 inhibitor with an IC50 of 6.49 nM. OTS186935 hydrochloride shows significant inhibition of tumor growth in mouse xenograft models without any detectable toxicity. OTS193320 hydrochloride regulates the production of γ-H2AX in cancer cells[1].

IC50 & Target

IC50: 6.49 nM (SUV39H2)[1]

In Vitro

OTS186935 hydrochloride inhibits A549 cell growth with an IC50 of 0.67 μM[1].

In Vivo

OTS186935 hydrochloride (10 mg/kg or 25 mg/kg; intravenously; once daily for 14 days) exhibits growth suppressive effects in human cancer cell line derived xenograft models[1].

Animal Model: Female NOD.CB17-Prkdcscid/J mice (bearing MDA-MB-231 cells )[1]
Dosage: 10 mg/kg
Administration: Intravenously; once daily for 14 days
Result: Tumor growth inhibition of 42.6% on day 14.
Animal Model: Female BALB/cAJcl-nu/nu mice (bearing A549 cells)[1]
Dosage: 25 mg/kg
Administration: Intravenously; once daily for 14 days
Result: Yielded a tumor growth inhibition of 60.8% without significant body weight loss or toxicity.
Molecular Weight

522.31

Formula

C₂₅H₂₆ClN₅O₂. ₈/₅HCl

SMILES

COC1=C(Cl)C=C(C2=CN3C=CC(N4C[[email protected]@H](NCC5=CC=NC=C5)CC4)=CC3=N2)C(OC)=C1.[H]Cl.[8/5]

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 : 25 mg/mL (47.86 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.9146 mL 9.5729 mL 19.1457 mL
5 mM 0.3829 mL 1.9146 mL 3.8291 mL
10 mM 0.1915 mL 0.9573 mL 1.9146 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: 2.08 mg/mL (3.98 mM); Suspended solution; Need ultrasonic

  • 2.

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

    Solubility: ≥ 2.08 mg/mL (3.98 mM); Clear solution

  • 3.

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

    Solubility: ≥ 2.08 mg/mL (3.98 mM); Clear solution

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

OTS186935OTS 186935OTS-186935Histone MethyltransferaseH2AXmethyltransferasetoxicityphosphorylationMDA-MB-231breastcancercellsA549lungInhibitorinhibitorinhibit

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Product Name:
OTS186935 hydrochloride
Cat. No.:
HY-122181B
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