KDM5-IN-1

SKU: orb1308159

Description

KDM5-IN-1 is a potent and selective KDM5 histone demethylase inhibitor, exhibiting an IC50 of 15.1 nM. This compound is a valuable chemical probe for epigenetic research, facilitating the study of histone methylation roles in cancer biology and cellular differentiation in both in vitro and in vivo models.

Research Area

Epigenetics & Chromatin

Key Properties

• CAS Number: 1628210-26-3
• MW: 324.38
• Purity: 99.50% (May vary between batches)
• Formula: C₁₇H₂₀N₆O
• SMILES: CC(C)c1c([nH]c2c(cnn2c1=O)C#N)-c1cnn(c1)C(C)(C)C
• Target: Histone Demethylase
• Solubility: DMSO:30 mg/mL (92.48 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (6.17 mM)

Bioactivity

• Target IC50:
  PC9 H3K4Me3 cells:(EC50)0.34 μM|KDM5:15.1 nM
• In Vivo:
  KDM5-IN-1(50 mg/kg; oral) shows an unbound maximal plasma concentration Cmax>15-fold over its cell EC50 in vivo.
• In Vitro:
  KDM5-IN-1 is significantly less potent against other KDM enzymes (1A, 2B, 3B, 4C, 5A, 6A, 7B), inhibiting KDM4C the strongest with an IC50 of 1.9 μM. KDM5-IN-1 potently inhibits KDM5B and KDM5C isoforms (IC50 of 4.7 and 65.5 nM, respectively).
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Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

HistoneDemethylase, Histone Demethylase, Inhibitor, inhibit, KDM5, KDM5 IN 1, KDM5IN1, KDM-5-IN-1, KDM5-IN-1, PC9 H3K4Me3

Compound Identifiers

PubChem CID

118908379