KDM5-IN-1 Inhibitor

Name: KDM5-IN-1 Inhibitor; MyBioSource
Brand: MyBioSource
SKU: MBS5755041
Availability: InStock
Rating: 5 (10 reviews)

For Research Use Only. Not for use in diagnostic procedures. Catalog #: MBS5755041

KDM5-IN-1 is an effective, selective, and orally bioavailable inhibitor of KDM5 (IC50: 15.1nM). More details

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Product Documentation

Sample Manual Insert View PDF

Testing Data View PDF

Certificate of Analysis (COA) View PDF

QC Report View PDF

Material Safety Data Sheet View PDF

Technical Datasheet View PDF

Protocol View PDF

Product Overview

Online Datasheet in PDF

Product Name

KDM5-IN-1, Inhibitor

Full Product Name

KDM5-IN-1

Product Gene Name

KDM5-IN-1, inhibitor

Form/Format

Solid. Powder

Purity/Purification

98.00%

Preparation and Storage

Store at -20 degree C for 3 years powder
-80 degree C for 2 years in solvent

Molecular Weight

324.38

Solubility

DMSO: 30mg/mL (92.48mM)
(<1mg/ml refers to the product slightly soluble or insoluble)

Formula

C17H20N6O

SMILES

N#CC1=C2NC(C3=CN(C(C)(C)C)N=C3)=C(C(C)C)C(N2N=C1)=O

CAS Number

1628210-26-3

Target & IC50

KDM5: ic50 15.1nM
PC9 H3K4Me3: ic50 0.34uM (EC50)

In Vitro

KDM5-IN-1(50mg/kg; orally at twice a day; in mice)treatment, displays an unbound maximal plasma concentration Cmax>15-fold over its cell EC50. Thereby providing a robust chemical probe for studying KDM5 biological functions in vivo[1].

Product Categories/Family for KDM5-IN-1, inhibitor

Chromatin/Epigenetic; Histone Demethylase; Epigenetics

Product References and Citations for KDM5-IN-1, inhibitor

Liang J, et al. Lead optimization of a pyrazolo[1,5-a]pyrimidin-7(4H)-one scaffold to identify potent, selective and orally bioavailable KDM5 inhibitors suitable for in vivo biological studies. Bioorg Med Chem Lett. 2016 Aug 15;26(16):4036-4
Liang J, et al. Lead optimization of a pyrazolo[1,5-a]pyrimidin-7(4H)-one scaffold to identify potent, selective and orally bioavailable KDM5 inhibitors suitable for in vivo biological studies. Bioorg Med Chem Lett. 2016 Aug 15;26(16):4036-41.

Other Notes

Small volumes of KDM5-IN-1, inhibitor vial(s) may occasionally become entrapped in the seal of the product vial during shipment and storage. If necessary, briefly centrifuge the vial on a tabletop centrifuge to dislodge any liquid in the container`s cap. Certain products may require to ship with dry ice and additional dry ice fee may apply.

Searchable Terms for KDM5-IN-1 purchase

MBS5755041 is an inhibitor targeting KDM5-IN-1.