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KDM5-C70

Catalog No. T15648 CAS 1596348-32-1

KDM5-C70 is an ethyl ester derivative of KDM5-C49. KDM5-C70 is an effective, cell-permeable, and pan-KDM5 histone demethylase inhibitor. KDM5-C70 has an antiproliferative effect in myeloma cells, inducing a genome-wide elevation of H3K4me3 levels.

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KDM5-C70, CAS 1596348-32-1

Pack Size	Availability	Price/USD
2 mg	In stock	$ 37.00
5 mg	In stock	$ 56.00
10 mg	In stock	$ 81.00
25 mg	In stock	$ 143.00
50 mg	In stock	$ 258.00
100 mg	In stock	$ 515.00
200 mg	In stock	$ 737.00
500 mg	In stock	$ 1,130.00
1 mL * 10 mM (in DMSO)	In stock	$ 67.00

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Biological Description

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Description

In vitro

KDM5-C70 (50 μM; 7 days; MM.1S myeloma cells) treatment reduces the level of phosphorylation of retinoblastoma protein (Rb) while leaving the total level of phosphorylated Rb (pRb) unchanged, indicating impairment of cell cycle progression. KDM5-C70 (1 nM-10 μM; 7 days; MM.1S myeloma cells) treatment displays antiproliferative effects after 7 days of treatment at elevated concentrations (estimated 50% reduction of viability/proliferation for KDM5-C70 at ~20 μM). Chromatin immunoprecipitation followed by next-generation sequencing displays an enhanced H3K4me3 level around transcription start sites with KDM5-C70 but little change with GSK467A at 50 μM inhibitor concentrations [1].

Molecular Weight	336.43
Formula	C17H28N4O3
CAS No.	1596348-32-1

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 250 mg/mL (743.10 mM), Sonication is recommended.

References and Literature

1. Johansson C, et al. Structural analysis of human KDM5B guides histone demethylase inhibitor development. Nat Chem Biol. 2016 Jul;12(7):539-45. 2. Blair LP, et al. KDM5 lysine demethylases are involved in maintenance of 3'UTR length. Sci Adv. 2016 Nov 18;2(11):e1501662. 3. Xia L, Zheng Z, Liu J, et al. Targeting triple-negative breast cancer with combination therapy of EGFR CAR-T cells and CDK7 inhibition[J]. Cancer Immunology Research. 2021

Citations

1. Xia L, Zheng Z, Liu J, et al. Targeting triple-negative breast cancer with combination therapy of EGFR CAR T cells and CDK7 inhibition. Cancer Immunology Research. 2021, 9(6): 707-722.

Related compound libraries

This product is contained In the following compound libraries：

Inhibitor Library Bioactive Compounds Library Max Epigenetics Compound Library NO PAINS Compound Library Bioactive Compound Library Histone Modification Compound Library

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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

KDM5-C70 1596348-32-1 Chromatin/Epigenetic Histone Demethylase KDM5-C49 JARID1 retinoblastoma inhibit KDM5 C70 KDM-5-C70 phosphorylation KDM5C70 KDM5 Inhibitor H3K4me3 antiproliferative inhibitor

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