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KDM5-IN-48
CAS No. 1628210-26-3
KDM5-IN-48( KDM5-IN-48 | KDM5 IN 48 | KDM5IN48 | KDM5 inhibitor-48 | KDM5 inhibitor 48 )
Catalog No. M12424 CAS No. 1628210-26-3
A potent, selective and orally bioavailable KDM5 inhibitor with biochemical IC50 of 15.1, 4.7 and 65.5 nM for KDM5A, KDM5B and KDM5C, respectively.
Purity : >98% (HPLC)
COA
Datasheet
HNMR
HPLC
MSDS
Handing Instructions
| Size | Price / USD | Stock | Quantity |
| 5MG | 294 | Get Quote |
|
| 10MG | 447 | Get Quote |
|
| 25MG | 714 | Get Quote |
|
| 50MG | 1017 | Get Quote |
|
| 100MG | 1368 | Get Quote |
|
| 500MG | 2673 | Get Quote |
|
| 1G | Get Quote | Get Quote |
|
Biological Information
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Product NameKDM5-IN-48
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NoteResearch use only, not for human use.
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Brief DescriptionA potent, selective and orally bioavailable KDM5 inhibitor with biochemical IC50 of 15.1, 4.7 and 65.5 nM for KDM5A, KDM5B and KDM5C, respectively.
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DescriptionA potent, selective and orally bioavailable KDM5 inhibitor with biochemical IC50 of 15.1, 4.7 and 65.5 nM for KDM5A, KDM5B and KDM5C, respectively; displays significantly less potent against other KDM enzymes (KDM4C IC50=1.9 uM); increases H3K4Me3 level in PC9 cells with EC50 of 0.34 uM; possesses suitable physiochemical properties and displays excellent PK profile in mice.
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In VitroKDM5-IN-1 is found to potently inhibit KDM5B and KDM5C isoforms (IC50 of 4.7 and 65.5 nM, respectively). It is significantly less potent against other KDM enzymes (1A, 2B, 3B, 4C, 5A, 6A, 7B), inhibiting KDM4C the strongest with an IC50 of 1.9 μM. KDM5-IN-1 still displays more than 100-fold selectivity for KDM4C vs. KDM5A.
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In VivoWhen dosed orally in mice at 50 mg/kg twice a day, KDM5-IN-1 shows an unbound maximal plasma concentration Cmax>15-fold over its cell EC50, thereby providing a robust chemical probe for studying KDM5 biological functions in vivo.
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SynonymsKDM5-IN-48 | KDM5 IN 48 | KDM5IN48 | KDM5 inhibitor-48 | KDM5 inhibitor 48
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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 Number1628210-26-3
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Formula Weight324.3803
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Molecular FormulaC17H20N6O
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Purity>98% (HPLC)
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SolubilityDMSO: ≥ 30 mg/mL
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SMILESN#CC1=C2NC(C3=CN(C(C)(C)C)N=C3)=C(C(C)C)C(N2N=C1)=O
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Chemical NamePyrazolo[1,5-a]pyrimidine-3-carbonitrile, 5-[1-(1,1-dimethylethyl)-1H-pyrazol-4-yl]-4,7-dihydro-6-(1-methylethyl)-7-oxo-
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. Liang J, et al. Bioorg Med Chem Lett. 2016 Aug 15;26(16):4036-41.
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