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KDM5-C70 Sale

(Synonyms: KDOAM-21) 目录号 : GC39394

An inhibitor of JARID1B

KDM5-C70 Chemical Structure

Cas No.:1596348-32-1

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25mg
¥1,575.00
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100mg
¥5,805.00
现货
250mg
¥11,655.00
现货

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Sample solution is provided at 25 µL, 10mM.

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产品描述

KDM5-C70 is an inhibitor of Jumonji AT rich interactive domain 1B (JARID1B), also known as lysine-specific demethylase 5B (KDM5B; IC50 = 49 nM).1 It is selective for JARID1B over KDM4C (IC50 = 2,400 nM).

1.Tumber, A., Nuzzi, A., Hookway, E.S., et al.Potent and selective KDM5 inhibitor stops cellular demethylation of H3K4me3 at transcription start sites and proliferation of MM1S myeloma cellsCell Chem. Biol.24(3)371-380(2017)

Chemical Properties

Cas No. 1596348-32-1 SDF
别名 KDOAM-21
Canonical SMILES O=C(C1=CC(CNCC(N(CCN(C)C)CC)=O)=NC=C1)OCC
分子式 C17H28N4O3 分子量 336.43
溶解度 DMSO: 250 mg/mL (743.10 mM) 储存条件 Store at -20°C
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1 mM 2.9724 mL 14.8619 mL 29.7239 mL
5 mM 0.5945 mL 2.9724 mL 5.9448 mL
10 mM 0.2972 mL 1.4862 mL 2.9724 mL
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Research Update

The KDM5 Inhibitor KDM5-C70 Induces Astrocyte Differentiation in Rat Neural Stem Cells

ACS Chem Neurosci 2021 Feb 3;12(3):441-446.PMID:33482060DOI:10.1021/acschemneuro.0c00613.

Members of the lysine-specific histone demethylase 5 (KDM5/JARID1) family are known to play important roles in stem cell fate determination. Here, using the KDM5 inhibitor C70 (KDM5-C70), we demonstrated that the histone demethylase activity of the KDM5 enzyme is essential for the repression of astrocytic differentiation of neural stem cells (NSCs). KDM5-C70 treatment activated the glial fibrillary acidic protein (Gfap) gene by increasing the trimethylation of histone H3 lysine 4 in the promoter regions and subsequently induced astrocytogenesis in NSCs. In addition, treatment of NSCs with KDM5-C70 activated Janus kinase-signal transducer and activator of transcription (JAK-STAT3) signaling and increased the mRNA expression of transforming growth factor-beta 1 (Tgf-β1). Our data provide evidence that KDM5 is a promising target for NSC fate modulation and suggest that epigenetic regulation is important for NSC fate determination.

Structural analysis of human KDM5B guides histone demethylase inhibitor development

Nat Chem Biol 2016 Jul;12(7):539-45.PMID:27214403DOI:10.1038/nchembio.2087.

Members of the KDM5 (also known as JARID1) family are 2-oxoglutarate- and Fe(2+)-dependent oxygenases that act as histone H3K4 demethylases, thereby regulating cell proliferation and stem cell self-renewal and differentiation. Here we report crystal structures of the catalytic core of the human KDM5B enzyme in complex with three inhibitor chemotypes. These scaffolds exploit several aspects of the KDM5 active site, and their selectivity profiles reflect their hybrid features with respect to the KDM4 and KDM6 families. Whereas GSK-J1, a previously identified KDM6 inhibitor, showed about sevenfold less inhibitory activity toward KDM5B than toward KDM6 proteins, KDM5-C49 displayed 25-100-fold selectivity between KDM5B and KDM6B. The cell-permeable derivative KDM5-C70 had an antiproliferative effect in myeloma cells, leading to genome-wide elevation of H3K4me3 levels. The selective inhibitor GSK467 exploited unique binding modes, but it lacked cellular potency in the myeloma system. Taken together, these structural leads deliver multiple starting points for further rational and selective inhibitor design.