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CAS No. : 1628210-26-3
MCE 国际站:KDM5-IN-1
产品活性:KDM5-IN-1是高效选择,有口服活性的KDM5抑制剂,IC50值为15.1 nM。
研究领域:Epigenetics
作用靶点:Histone Demethylase
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.
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.
相关产品:Bioactive Compound Library Plus | Epigenetics Compound Library | Histone Modification Research Compound Library | Anti-Cancer Compound Library | Orally Active Compound Library | Anti-Cancer Metabolism Compound Library | Targeted Diversity Library | Heterocyclic Compound Library | Highly Selective Inhibitors Library | GSK2879552 dihydrochloride | KDM2B-IN-3 | KDM4-IN-2 | LSD1/ER-IN-1 | GSK-J4 hydrochloride | Bomedemstat hydrochloride | LSD1-IN-18 | KDM4-IN-4 | (1S,2R)-Tranylcypromine hydrochloride | Pulrodemstat benzenesulfonate | GSK-J1 lithium salt | CPI-4203 | JQKD82 | Corin | Tranylcypromine hemisulfate | KDM2B-IN-4 | (1R,2S)-NCD38 TFA | LSD1-IN-14 | LSD1-IN-26 | Helenalin acetate | KDM2B-IN-2 | JHDM-IN-1 | Seclidemstat | GSK-LSD1 dihydrochloride | LSD1-IN-21 | Arborinine | KDM4-IN-3
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货号: HY-100422
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