1. Epigenetics
  2. Histone Methyltransferase
  3. OTS186935 trihydrochloride

OTS186935 trihydrochloride 

Cat. No.: HY-122181A
Handling Instructions

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

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OTS186935 trihydrochloride Chemical Structure

OTS186935 trihydrochloride Chemical Structure

CAS No. : 2093401-85-3

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Description

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

IC50 & Target

IC50: 6.49 nM (SUV39H2)[1]

In Vitro

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

In Vivo

OTS186935 trihydrochloride (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

573.34

Formula

C₂₅H₂₉Cl₄N₅O₂

CAS No.

2093401-85-3

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.[H]Cl.[H]Cl

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Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

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Keywords:

OTS186935 trihydrochlorideHistone MethyltransferaseMDA-MB-231breastcancercellsA549lungtoxicityproliferationtumorInhibitorinhibitorinhibit

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OTS186935 trihydrochloride
Cat. No.:
HY-122181A
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