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KDM5-C70
CAS No. 1596348-32-1
KDM5-C70( KDM5 inhibitor C70 )
Catalog No. M12280 CAS No. 1596348-32-1
KDM5-C70 is the cell-permeable derivative of KDM5-C49, potent, selective and cell permeable KDM5 inhibitor with IC50 of 0.3, 0.3 and 0.58 uM for KDM5A, B and C, respectively.
Purity : >98% (HPLC)
COA
Datasheet
HNMR
HPLC
MSDS
Handing Instructions
| Size | Price / USD | Stock | Quantity |
| 2MG | 33 | In Stock |
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| 5MG | 50 | In Stock |
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| 10MG | 73 | In Stock |
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| 25MG | 129 | In Stock |
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| 50MG | 232 | In Stock |
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| 100MG | 464 | In Stock |
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| 200MG | 663 | In Stock |
|
| 500MG | 1017 | In Stock |
|
| 1G | Get Quote | In Stock |
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Biological Information
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Product NameKDM5-C70
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NoteResearch use only, not for human use.
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Brief DescriptionKDM5-C70 is the cell-permeable derivative of KDM5-C49, potent, selective and cell permeable KDM5 inhibitor with IC50 of 0.3, 0.3 and 0.58 uM for KDM5A, B and C, respectively.
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DescriptionKDM5-C70 is the cell-permeable derivative of KDM5-C49, potent, selective and cell permeable KDM5 inhibitor with IC50 of 0.3, 0.3 and 0.58 uM for KDM5A, B and C, respectively; significantly increases global levels of H3K4me3, while having little impact on H3K4me2/me1, or modifications regulated by other histone lysine demethylases, such as H3K27me3 (substrate for the KDM6 family) and H3K9me3/H3K36me3 (substrates for the KDM4 family).
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In VitroKDM5-C70 (10-9-10-5 M; 7 days; MM.1S myeloma cells) treatment shows antiproliferative effects after 7 days of treatment at elevated concentrations (estimated 50% reduction of viability/proliferation for KDM5-C70 at ~20 μM).KDM5-C70 (50 μM; 7 days; MM.1S myeloma cells)treatment decreases the level of phosphorylation of retinoblastoma protein (Rb), while leaving the total level of phosphorylated Rb (pRb) unchanged, indicating impairment of cell cycle progression.Chromatin immunoprecipitation followed by next-generation sequencing shows an increase in H3K4me3 levels around transcription start sites with KDM5-C70 but little change with GSK467A at 50 μM inhibitor concentrations. Cell Viability Assay Cell Line:MM.1S myeloma cells Concentration:10-9-10-5 M Incubation Time:7 days Result:Showed antiproliferative effects after 7 days of treatment at elevated concentrations.Western Blot Analysis Cell Line:MM.1S myeloma cells Concentration:50 μM Incubation Time:7 days Result:Decreased the level of phosphorylation of retinoblastoma protein (Rb).
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In Vivo——
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SynonymsKDM5 inhibitor C70
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PathwayChromatin/Epigenetic
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TargetHistone Demethylase
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RecptorHistone Demethylase
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Research Area——
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Indication——
Chemical Information
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CAS Number1596348-32-1
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Formula Weight336.43
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Molecular FormulaC17H28N4O3
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Purity>98% (HPLC)
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SolubilityIn Vitro:?DMSO : 100 mg/mL (297.24 mM)
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SMILESO=C(OCC)C1=CC=NC(CNCC(N(CCN(C)C)CC)=O)=C1
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Chemical NameEthyl 2-(((2-((2-(dimethylamino)ethyl)(ethyl)amino)-2-oxoethyl)amino)methyl)isonicotinate
Shipping & Storage Information
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Storage(-20℃)
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ShippingWith Ice Pack
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Stability≥ 2 years
Reference
1. Johansson C, et. Nat Chem Biol. 2016 Jul;12(7):539-45.
2. Horton JR, et al. Cell Chem Biol. 2016 Jul 21;23(7):769-81.
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