1. Epigenetics
  2. Histone Demethylase
  3. KDM5A-IN-1

KDM5A-IN-1 

Cat. No.: HY-100014 Purity: 98.65%
Handling Instructions

KDM5A-IN-1 is a potent, orally bioavailable pan-histone lysine demethylases 5 (KDM5) inhibitor with IC50s of 45 nM, 56 nM and 55 nM for KDM5A, KDM5B and KDM5C, respectively, and with an EC50 value of 960 nM for PC9 H3K4Me3. KDM5A-IN-1 is significantly less potent against other KDM5B enzymes (1A, 2B, 3B, 4C, 6A, 7B).

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

KDM5A-IN-1 Chemical Structure

KDM5A-IN-1 Chemical Structure

CAS No. : 1905481-36-8

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 575 In-stock
Estimated Time of Arrival: December 31
1 mg USD 180 In-stock
Estimated Time of Arrival: December 31
5 mg USD 420 In-stock
Estimated Time of Arrival: December 31
10 mg USD 600 In-stock
Estimated Time of Arrival: December 31
50 mg USD 1800 In-stock
Estimated Time of Arrival: December 31
100 mg USD 2520 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

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Based on 1 publication(s) in Google Scholar

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Description

KDM5A-IN-1 is a potent, orally bioavailable pan-histone lysine demethylases 5 (KDM5) inhibitor with IC50s of 45 nM, 56 nM and 55 nM for KDM5A, KDM5B and KDM5C, respectively, and with an EC50 value of 960 nM for PC9 H3K4Me3. KDM5A-IN-1 is significantly less potent against other KDM5B enzymes (1A, 2B, 3B, 4C, 6A, 7B)[1].

IC50 & Target

IC50: 45 nM (KDM5A), 56 nM (KDM5B) and 55 nM (KDM5C)[1]

In Vivo

KDM5A-IN-1 (Compound 50, 5 mg/kg; oral administration; female CD-1 mice) treatment shows moderate clearance (28 mL/min/kg) in mice with good oral bioavailability (F% 34) and remarkably low plasma protein binding in mice (40%), with t1/2 of 0.4 hours[1].

Animal Model: Female CD-1 mice[1]
Dosage: 5 mg/kg
Administration: Oral administration (Pharmacokinetic study)
Result: Moderate clearance (28 mL/min/kg) in mice with good oral bioavailability (F% 34), and showed remarkably low plasma protein binding in mice (40%).
Molecular Weight

290.36

Formula

C₁₅H₂₂N₄O₂

CAS No.

1905481-36-8

SMILES

O=C(C1CC1)N[[email protected]@H]2CCN(C(C3=CC(C(C)C)=NN3)=O)C2

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 : ≥ 50 mg/mL (172.20 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.4440 mL 17.2200 mL 34.4400 mL
5 mM 0.6888 mL 3.4440 mL 6.8880 mL
10 mM 0.3444 mL 1.7220 mL 3.4440 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: ≥ 2.75 mg/mL (9.47 mM); Clear solution

  • 2.

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

    Solubility: ≥ 2.75 mg/mL (9.47 mM); Clear solution

  • 3.

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

    Solubility: ≥ 2.75 mg/mL (9.47 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
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Product Name:
KDM5A-IN-1
Cat. No.:
HY-100014
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