1. Epigenetics
  2. Histone Demethylase
  3. KDM5-C70

KDM5-C70 

Cat. No.: HY-120400 Purity: >98.0%
Handling Instructions

KDM5-C70 is an ethyl ester derivative of KDM5-C49 and a potent, cell-permeable and pan-KDM5 histone demethylase inhibitor. KDM5-C70 has an antiproliferative effect in myeloma cells, leading to genome-wide elevation of H3K4me3 levels.

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

KDM5-C70 Chemical Structure

KDM5-C70 Chemical Structure

CAS No. : 1596348-32-1

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Based on 1 publication(s) in Google Scholar

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Description

KDM5-C70 is an ethyl ester derivative of KDM5-C49 and a potent, cell-permeable and pan-KDM5 histone demethylase inhibitor. KDM5-C70 has an antiproliferative effect in myeloma cells, leading to genome-wide elevation of H3K4me3 levels[1][2].

IC50 & Target

KDM5 histone demethylase[1][2]

In Vitro

KDM5-C70 (10-9-10-5 M; 7 days; MM.1S myeloma cells) treatment shows antiproliferative effects after 7 days of treatment at elevated concentrations (estimated 50% reduction of viability/proliferation for KDM5-C70 at ~20 μM)[1].
KDM5-C70 (50 μM; 7 days; MM.1S myeloma cells) treatment decreases the level of phosphorylation of retinoblastoma protein (Rb), while leaving the total level of phosphorylated Rb (pRb) unchanged, indicating impairment of cell cycle progression[1].
Chromatin immunoprecipitation followed by next-generation sequencing shows an increase in H3K4me3 levels around transcription start sites with KDM5-C70 but little change with GSK467A at 50 μM inhibitor concentrations[1].

Cell Viability Assay[1]

Cell Line: MM.1S myeloma cells
Concentration: 10-9-10-5 M
Incubation Time: 7 days
Result: Showed antiproliferative effects after 7 days of treatment at elevated concentrations.

Western Blot Analysis[1]

Cell Line: MM.1S myeloma cells
Concentration: 50 μM
Incubation Time: 7 days
Result: Decreased the level of phosphorylation of retinoblastoma protein (Rb).
Molecular Weight

336.43

Formula

C₁₇H₂₈N₄O₃

CAS No.

1596348-32-1

SMILES

O=C(C1=CC(CNCC(N(CCN(C)C)CC)=O)=NC=C1)OCC

Shipping

Room temperature in continental US; may vary elsewhere.

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

DMSO : 250 mg/mL (743.10 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.9724 mL 14.8619 mL 29.7239 mL
5 mM 0.5945 mL 2.9724 mL 5.9448 mL
10 mM 0.2972 mL 1.4862 mL 2.9724 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: ≥ 6.25 mg/mL (18.58 mM); Clear solution

  • 2.

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

    Solubility: ≥ 6.25 mg/mL (18.58 mM); Clear solution

  • 3.

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

    Solubility: ≥ 6.25 mg/mL (18.58 mM); Clear solution

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

KDM5-C70Histone DemethylaseKDM5JARID1antiproliferativephosphorylationretinoblastomaH3K4me3KDM5-C49Inhibitorinhibitorinhibit

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Product Name:
KDM5-C70
Cat. No.:
HY-120400
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