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KDM5-IN-1

CAS No. : 1628210-26-3

MCE 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 C_max>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  |  GSK-J4  |  JIB-04  |  IOX1  |  Corin  |  Tranylcypromine hemisulfate  |  KDOAM-25 citrate  |  NCGC00244536  |  L-2-Hydroxyglutaric acid disodium  |  Daminozide  |  PBIT  |  AS8351  |  Procaine  |  CBB1007 trihydrochloride  |  α-Hydroxyglutaric acid  |  (rel)-Tranylcypromine D5 hydrochloride  |  KDM2A/7A-IN-1

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