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 is a potent and highly selective histone lysine demethylases 5 (KDM5) inhibitor, with IC50 values of 71 nM, 19 nM, 69 nM, and 69 nM for KDM5A, KDM5B, KDM5C, and KDM5D, respectively. Multiple myeloma MM1S cells treated with KDOAM-25 citrate show increased global H3K4 methylation at transcriptional start sites and impaired proliferation [1].

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 is an orally available, potent and selective inhibitor of the pan-histidine lysine demethylase 5 KDM5, inhibiting KDM5A, KDM5B, and KDM5C with IC50 values of 45 nM, 56 nM, and 55 nM, respectively.KDM5A-IN-1 inhibits PC9 H3K4Me3, and may be useful in cancer research.

KDM5B ligand 2 is a ligand for the target protein KDM5B. It is utilized in the synthesis of the KDM5B PROTAC degrader GT-653.

KDM5B-IN-4 (compound 11ad) is a novel inhibitor of lysine demethylase 5B (KDM5B), with an IC50 of 0.025 μM for KDM5B. It increases the levels of the substrate H3K4me1/2/3 in PC-3 cells by inhibiting KDM5B. Furthermore, KDM5B-IN-4 induces G2/M phase arrest in PC-3 cells and downregulates proteins in the PI3K/AKT signaling pathway. Additionally, KDM5B-IN-4 reduces tumor volume in mice with minimal organ toxicity.

KDM5B-IN-3 (Compound 5) is an inhibitor of histone lysine-specific demethylase 5B (KDM5B) or JARID1B, with an IC50 value of 9.32 μM, and 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) is a potent and selective inhibitor of KDM5 demethylase. KDM5-C49 HCL(1596348-16-1 Free base) is a candidate compound for the treatment of cancer.

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

PBIT inhibits JARID1B histone demethylase (IC50 of about 3 μM). PBIT also inhibits JARID1A and JARID1C (IC50s of 6 μM and 4.9 μM, respectively). PBIT is a specific inhibitor of the Jumonji AT-rich Interactive Domain 1 (JARID1) enzymes .

YUKA1, a cell-permeable KDM5A inhibitor (IC50=2.66 μM) with a weak effect on KDM5C (IC50=7.12 μM) and no effect on other KDM isoforms, was able to increase the level of H3K4me3 in human cells and inhibit the proliferation of cancer cells, and also prevented the emergence of drug-resistant cells.

GT-653 is a PROTAC degrader targeting lysine-specific demethylase 5B (KDM5B). It induces the degradation of KDM5B via ubiquitin-proteasome pathways, achieving a degradation rate of 68.35% at a concentration of 10 μM. Additionally, GT-653 upregulates H3K4me3 levels and activates type I interferon signaling pathways in prostate cancer cells 22RV1.

YTHu78 is a KDM5B PROTAC-based degrader. It induces the degradation of KDM5B through the ubiquitin-proteasome system and triggers apoptosis in MV-4-11 and MM.1S cell lines. YTHu78 demonstrates significant antiproliferative activity against various hematologic tumor cell lines and is useful for studying hematological malignancies.

TK-129 is an orally active, potent inhibitor of KDM5B with an IC50 of 44 nM and is low-toxicity. TK-129 exhibits cardioprotective effects by inhibiting KDM5B and blocking the KDM5B-associated Wnt pathway. TK-129 can be used in cardiovascular disease studies to reduce isoprenaline-induced myocardial remodelling and fibrosis in vivo, as well as to reduce ang II-induced activation of cardiac fibroblasts in vitro [1].

KDOAM-25 trihydrochloride is a potent and highly selective inhibitor of histone lysine demethylase 5 (KDM5), targeting KDM5A (IC50: 71 nM), KDM5B (IC50: 19 nM), KDM5C (IC50: 69 nM), and KDM5D (IC50: 69 nM). It enhances overall H3K4 methylation at the transcription start site and hinders the proliferation of multiple myeloma [MM1S cells].

Roxadustat-D5 is intended for use as an internal standard for the quantification of roxadustat by GC- or LC-MS. Roxadustat (T2515) 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 (T2515) (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 (T2515) 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 is a potent, selective inhibitor of the KDM5 family of demethylases, with IC50 values of 40 nM for KDM5A, 160 nM for KDM5B, and 100 nM for KDM5C. This compound is utilized in cancer research [1].

Roxadustat-D5 (Standard) is a reference standard of Roxadustat-D5 intended for quantitative analysis, quality control, and related biochemical research applications. 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......