KDM5-IN-1 - ≥99% , CAS No.1628210-26-3

CAS: 1628210-26-3 Cat. No.: K647839 Molecular Weight: 324.38

GRADE & PURITY ≥99%

Storage

Store at -20°C

Shipped In

Ice chest + Ice pads

Overview

KDM5-IN-1 is a potent, selective and orally bioavailable KDM5 inhibitor with an IC 50 of 15.1 nM.

In Vitro

KDM5-IN-1 is found to potently inhibit KDM5B and KDM5C isoforms (IC 50 of 4.7 and 65.5 nM, respectively). It is significantly less potent against other KDM enzymes (1A, 2B, 3B, 4C, 5A, 6A, 7B), inhibiting KDM4C the strongest with an IC 50 of 1.9 μM. KDM5-IN-1 still displays more than 100-fold selectivity for KDM4C vs. KDM5A. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

When dosed orally in mice at 50 mg/kg twice a day, KDM5-IN-1 shows an unbound maximal plasma concentration C max >15-fold over its cell EC 50 , thereby providing a robust chemical probe for studying KDM5 biological functions in vivo . MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Form:Solid

IC50& Target:IC50: 15.1 nM (KDM5),EC50: 0.34 μM (PC9 H3K4Me3)

Specifications

Specifications & Purity

≥99%

Biochemical and Physiological Mechanisms

KDM5-IN-1 is a potent, selective and orally bioavailable KDM5 inhibitor with an IC 50 of 15.1 nM.

Storage

Store at -20°C

Shipped In

Ice chest + Ice pads

This product requires cold chain shipping. Ground and other economy services are not available.

Action Type

INHIBITOR

Purity

≥99%

Names and Identifiers

• Molecular Weight: 324.38

Chemical and Physical Properties

• Solubility: DMSO : ≥ 30 mg/mL (92.48 mM)