KDM5A-IN-1 Inhibitor

Name: KDM5A-IN-1 Inhibitor; MyBioSource
Brand: MyBioSource
SKU: MBS5755042
Availability: InStock
Rating: 5 (10 reviews)

For Research Use Only. Not for use in diagnostic procedures. Catalog #: MBS5755042

KDM5A-IN-1 is a potent and orally bioavailable inhibitor of pan-histone lysine demethylases 5 (IC50s: 45nM, 56nM, and 55nM for KDM5A, KDM5B, and KDM5C) and (EC50: 960nM for PC9 H3K4Me3). KDM5A-IN-1 is obviously less effective against other KDM5B enzymes (1A,… 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

KDM5A-IN-1, Inhibitor

Full Product Name

KDM5A-IN-1

Product Gene Name

KDM5A-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

290.36

Solubility

DMSO: 50mg/mL (172.20mM)
(<1mg/ml refers to the product slightly soluble or insoluble)

Formula

C15H22N4O2

SMILES

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

CAS Number

1905481-36-8

Target & IC50

KDM5A: ic50 45nM
KDM5B: ic50 56nM
KDM5C: ic50 55nM

In Vitro

KDM5A-IN-1 (5mg/kg; p.o.; female CD-1 mice) treatment,displays moderate clearance (28mL/min/kg) in mice. It has good oral bioavailability (F% 34) and remarkably low plasma protein binding in mice (40%) (t1/2: 0.4 hours)[1].

Product Categories/Family for KDM5A-IN-1, inhibitor

Chromatin/Epigenetic; Histone Demethylase; Epigenetics

Product References and Citations for KDM5A-IN-1, inhibitor

Liang J, et al. From a novel HTS hit to potent, selective, and orally bioavailable KDM5 inhibitors. Bioorg Med Chem Lett. 2017 Jul 1;27(13):2974-2981.
Liang J, et al. From a novel HTS hit to potent, selective, and orally bioavailable KDM5 inhibitors. Bioorg Med Chem Lett. 2017 Jul 1;27(13):2974-2981.

Other Notes

Small volumes of KDM5A-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 KDM5A-IN-1 purchase

MBS5755042 is an inhibitor targeting KDM5A-IN-1.