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KDM5-IN-1

CAS No. : 1628210-26-3

產(chǎn)品活性：KDM5-IN-1 is a potent, selective and orally bioavailable KDM5 inhibitor with an IC₅₀ of 15.1 nM.

研究領(lǐng)域：Epigenetics

作用靶點(diǎn)：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 C_max>15-fold over its cell EC₅₀, thereby providing a robust chemical probe for studying KDM5 biological functions in vivo.

相關(guān)產(chǎn)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  |  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  |  LSD1-IN-14  |  Helenalin acetate  |  KDM2B-IN-2  |  Seclidemstat  |  GSK-LSD1 dihydrochloride  |  LSD1-IN-21  |  KDM4-IN-3  |  LSD1/2-IN-4  |  NCDM-32B  |  Eicosapentaenoic Acid  |  LSD1-IN-15

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