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KDM5-IN-1

  Cat. No.:  DC10285   Featured
Chemical Structure
1628210-26-3
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More than 5000 active chemicals with high quality for research!
Field of application
KDM5-IN-1 is a potent, selective and orally bioavailable KDM5 inhibitor with an IC50 of 15.1 nM.
Chemicals PropertiesBiological activity COA & MSDSRelated productsDatasheet
Cas No.: 1628210-26-3
SMILES: N#CC1=C2NC(C3=CN(C(C)(C)C)N=C3)=C(C(C)C)C(N2N=C1)=O
Formula: C17H20N6O
M.Wt: 324.38
Purity: >98%
Sotrage: 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
Description: KDM5-IN-1 is a potent, selective and orally bioavailable KDM5 inhibitor with an IC50 of 15.1 nM.
Target: IC50: 15.1 nM (KDM5); EC50: 0.34 μM (PC9 H3K4Me3)[1]
In Vivo: When dosed orally in mice at 50 mg/kg twice a day, KDM5-IN-1 shows 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].
In Vitro: KDM5-IN-1 is found to potently inhibit KDM5B and KDM5C isoforms (IC50 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 IC50 of 1.9 μM. KDM5-IN-1 still displays more than 100-fold selectivity for KDM4C vs. KDM5A[1].
References: [1]. 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
MSDS
COA
LOT NO. DOWNLOAD
2018-0101
2018-0101
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