1. Epigenetics
  2. Histone Demethylase
  3. KDOAM-25 citrate

KDOAM-25 citrate 

Cat. No.: HY-102047B Purity: 98.04%
Handling Instructions

KDOAM-25 citrate is a potent and highly selective histone lysine demethylases 5 (KDM5) inhibitor with IC50s of 71 nM, 19 nM, 69 nM, 69 nM for KDM5A, KDM5B, KDM5C, KDM5D, respectively. KDOAM-25 citrate increases global H3K4 methylation at transcriptional start sites and impairs proliferation in multiple myeloma MM1S cells.

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

KDOAM-25 citrate Chemical Structure

KDOAM-25 citrate Chemical Structure

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Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO USD 110 In-stock
Estimated Time of Arrival: December 31
5 mg USD 100 In-stock
Estimated Time of Arrival: December 31
10 mg USD 180 In-stock
Estimated Time of Arrival: December 31
50 mg USD 700 In-stock
Estimated Time of Arrival: December 31
100 mg USD 1300 In-stock
Estimated Time of Arrival: December 31
200 mg USD 2400 In-stock
Estimated Time of Arrival: December 31
500 mg USD 4500 In-stock
Estimated Time of Arrival: December 31
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Customer Review

Based on 1 publication(s) in Google Scholar

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Description

KDOAM-25 citrate is a potent and highly selective histone lysine demethylases 5 (KDM5) inhibitor with IC50s of 71 nM, 19 nM, 69 nM, 69 nM for KDM5A, KDM5B, KDM5C, KDM5D, respectively. KDOAM-25 citrate increases global H3K4 methylation at transcriptional start sites and impairs proliferation in multiple myeloma MM1S cells[1].

IC50 & Target

IC50: 71 nM (KDM5A), 19 nM (KDM5B), 69 nM (KDM5C), 69 nM (KDM5D)[1]

In Vitro

KDOAM-25 citrate inhibits most potently KDM5B with an IC50 of ∼50 μM and the other KDM5 family members at concentrations above 100 μM. KDOAM-25 citrate shows no cellular activity on any of the other tested JmjC family members[1].
KDOAM-25 citrate is able to reduce the viability of MM1S cells with an IC50 of ∼30 μM after a delay of 5-7 days[1].
KDOAM-25 citrate treatment results in a G1 cell-cycle arrest with an increased proportion of MM1S in G1 and a decrease of the proportion of cells in G2 without an increase in the proportion of cells in the apoptotic sub-G1 phase[1].
KDOAM-25 citrate (50 μM) increases with approximately twice as much H3K4me3 in in multiple myeloma cells[1].

Molecular Weight

499.51

Formula

C₂₁H₃₃N₅O₉

SMILES

NC(C1=CC=NC(CNCC(N(CC)CCN(C)C)=O)=C1)=O.OC(CC(C(O)=O)(O)CC(O)=O)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, stored under nitrogen

*In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)

Solvent & Solubility
In Vitro: 

DMSO : 200 mg/mL (400.39 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.0020 mL 10.0098 mL 20.0196 mL
5 mM 0.4004 mL 2.0020 mL 4.0039 mL
10 mM 0.2002 mL 1.0010 mL 2.0020 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: ≥ 5 mg/mL (10.01 mM); Clear solution

  • 2.

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

    Solubility: ≥ 5 mg/mL (10.01 mM); Clear solution

  • 3.

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

    Solubility: ≥ 5 mg/mL (10.01 mM); Clear solution

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

KDOAM-25KDOAM25KDOAM 25Histone DemethylaseKDM5KDM5AKDM5BKDM5CKDM5DglobalH3K4methylationtranscriptionalproliferationmultiplemyelomaMM1SInhibitorinhibitorinhibit

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KDOAM-25 citrate
Cat. No.:
HY-102047B
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