2. Epigenetics
  3. Histone Methyltransferase
  4. OTS186935

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

At equivalent molar concentrations, both the salt and free forms of a compound exhibit comparable biological activity. Nevertheless, the salt form (OTS186935 hydrochloride) usually boasts enhanced water solubility and stability.

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

OTS186935 Chemical Structure

OTS186935 Chemical Structure

CAS No. : 2093400-18-9

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Description

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

IC50 & Target

IC50: 6.49 nM (SUV39H2)[1]
In Vitro

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

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

OTS186935 Related Antibodies
In Vivo

OTS186935 (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].

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

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

463.96

Formula

C25H26ClN5O2
CAS No.
SMILES

COC1=C(Cl)C=C(C2=CN3C=CC(N4C[C@@H](NCC5=CC=NC=C5)CC4)=CC3=N2)C(OC)=C1
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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OTS186935 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:

OTS1869352093400-18-9OTS 186935OTS-186935Histone MethyltransferaseH2AXmethyltransferasetoxicityanti-cancerphosphorylationMDA-MB-231breastcancercellsA549lungInhibitorinhibitorinhibit

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