KDM5-C49 (KDOAM-20) HCl is a potent and specific KDM5 demethylase inhibitor (antagonist) with IC50s of 40 nM, 160 nM and 100 nM for KDM5A, KDM5B and KDM5C respectively. KDM5-C49 HCl may be utilized in cancer research.

Physicochemical Properties

Molecular Formula	C15H25CLN4O3
Molecular Weight	344.84
CAS #	3026728-26-4
Related CAS #	KDM5-C49;1596348-16-1
Appearance	Colorless to light yellow solid-liquid Mixture
HS Tariff Code	2934.99.9001
Storage	Powder-20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture.
Shipping Condition	Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)

Biological Activity

ln Vitro	KDM5-C49 hydrochloride has a low permeability. A cell-permeable prodrug (KDM5-C70) was created by converting the carboxyl group of KDM5-C49 into an ethyl ester.
References	[1]. Structural Basis for KDM5A Histone Lysine Demethylase Inhibition by Diverse Compounds. Cell Chem Biol. 2016 Jul 21;23(7):769-781. [2]. The role and prospect of lysine-specific demethylases in cancer chemoresistance. Med Res Rev. 2023 Apr 3.

Solubility Data

Solubility (In Vitro)

DMSO :~125 mg/mL (~362.49 mM)

Solubility (In Vivo)

Solubility in Formulation 1: ≥ 2.08 mg/mL (6.03 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.08 mg/mL (6.03 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution.  (Please use freshly prepared in vivo formulations for optimal results.)

Preparing Stock Solutions		1 mg	5 mg	10 mg
	1 mM	2.8999 mL	14.4995 mL	28.9990 mL
	5 mM	0.5800 mL	2.8999 mL	5.7998 mL
	10 mM	0.2900 mL	1.4499 mL	2.8999 mL

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.