kdm5b

KDM4-IN-2 is a potent and selective KDM4 KDM5 dual inhibitor with Kis of 4 and 7 nM for KDM4A and KDM5B, respectively.

KDOAM-25 citrate 是有效且具有高选择性的组蛋白赖氨酸脱甲基酶 5 (KDM5) 抑制剂，对 KDM5A，KDM5B，KDM5C，KDM5D 的IC50分别为 71 nM，19 nM，69 nM，69 nM。用KDOAM-25 citrate 处理的多发性骨髓瘤 MM1S 细胞显示转录起始位点的整体 H3K4 甲基化增加，增殖受损。

KDOAM-25 trihydrochloride increases global H3K4 methylation at transcriptional start sites and impairs proliferation in multiple myeloma MM1S cells. KDOAM-25 trihydrochloride is a potent and highly selective histone lysine demethylases 5 (KDM5) inhibitor

KDOAM-25, a potent and highly selective inhibitor of histone lysine demethylases 5 (KDM5) with IC50 values of 71 nM for KDM5A, 19 nM for KDM5B, 69 nM for KDM5C, and 69 nM for KDM5D, enhances global H3K4 methylation at transcriptional start sites and reduces proliferation in multiple myeloma MM1S cells.

KDM5A-IN-1 是一种可口服且具有高效性和选择性的泛组氨酸赖氨酸脱甲基酶 5 KDM5 抑制剂，抑制 KDM5A，KDM5B，KDM5C，IC50 值分别为 45 nM，56 nM 和 55 nM。KDM5A-IN-1 抑制 PC9 H3K4Me3，可用于研究癌症。

KDM5B-IN-3 (Compound 5) is an inhibitor of histone lysine-specific demethylase 5B (KDM5B) or JARID1B. It effectively inhibits the activity of KDM5B with an IC50 value of 9.32 μM. Consequently, KDM5B-IN-3 serves as a valuable tool in gastric cancer research [1].

QC6352 is a selective and effective KDM4C inhibitor (IC50: 35 nM).

KDM5-C49 HCl (KDOAM-20 hydrochloride)KDM5-C49 HCl 是一种有效的和具有选择性的 去甲基化酶 KDM5抑制剂。KDM5-C49 HCl 是治疗癌症的候选化合物。

PBIT 是一种特异性 Jumonji AT 富集互作结构域 1 抑制剂，抑制JARID1A 和JARID1C，IC50分别为 6 和 4.9 μM。它抑制JARID1B(KDM5B 或PLU1) 组蛋白去甲基化酶，IC50值约为 3 μM。

YUKA1是一种具有细胞渗透性的KDM5A 抑制剂(IC50=2.66 μM)，对 KDM5C 的作用较弱（IC50=7.12 μM）而对其他KDM亚型无作用，能够增加人细胞中 H3K4me3 的水平和抑制癌细胞增殖，还能阻止药物耐受细胞的出现。

TK-129 是具有口服活性的 KDM5B 的有效抑制剂，IC50值为44 nM，并且具有低毒性。TK-129 发挥心脏保护作用，通过抑制 KDM5B 和阻断 KDM5B 相关的 Wnt 通路。TK-129 可用于研究心血管疾病，它能在体内减少异丙肾上腺素诱导的心肌重塑和纤维化，并且在体外减少 Ang II 诱导的心脏成纤维细胞活化。

KDOAM-25 trihydrochloride 是一种有效的、高度选择性的组蛋白赖氨酸脱甲基酶 5 (KDM5) 抑制剂，能够作用于 KDM5A (IC50: 71 nM)、KDM5B (IC50: 19 nM)、KDM5C (IC50: 69 nM)、KDM5D (IC50: 69 nM)。KDOAM-25 trihydrochloride 能够提高转录起始位点的整体 H3K4 甲基化，可阻碍多发性骨髓瘤 MM1S 细胞的增殖。

Roxadustat-d5 is intended for use as an internal standard for the quantification of roxadustat by GC- or LC-MS. Roxadustat is an inhibitor of hypoxia-inducible factor prolyl hydroxylase (HIF-PH; IC50s = 1.4, 1.26, and 1.32 µM for HIF-PH1, HIF-PH2, and HIF-PH3, respectively). It is selective for HIF-PH over other 2-oxoglutarate-dependent dioxygenases, including lysine-specific demethylase 5A (KDM5A), KDM5B, -5C, -5D, and -6B (IC50s = >100 µM for all). Roxadustat (10-200 µM) stabilizes HIF-1α and HIF-2α in Hep3B hepatocellular carcinoma cells. It increases levels of secreted erythropoietin in Hep3B cells in a concentration-dependent manner and increases erythropoiesis in rats when administered at doses of 25 and 50 mg kg. Roxadustat reverses anemia in a rat model of chronic inflammation induced by peptidoglycan-polysaccharide, as well as a rat model of chronic kidney disease induced by 5 6 nephrectomy. It reduces tumor growth and increases survival in a murine Lewis lung carcin......

KDM5-C49 (KDOAM-20) hydrochloride 是一种有效和选择性的KDM5去甲基化酶抑制剂，抑制KDM5A，KDM5B 和KDM5C 的IC50值分别为 40 nM，160 nM 和 100 nM。KDM5-C49 hydrochloride 可用于癌症的研究。