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Chemical Structure : P3FI-90
CAS No.: 53995-62-3
Catalog No.: PC-21840Not For Human Use, Lab Use Only.
P3FI-90 is a specific small molecule inhibitor of KDM3B with SPR KD of 7.68 uM, inhibits PAX3-FOXO1 activityand blocks PAX3-FOXO1 downstream target gene expression.
| Packing | Price | Stock | Quantity |
|---|---|---|---|
| 5 mg | $178 | In stock | |
| 10 mg | $288 | In stock | |
| 25 mg | $458 | In stock | |
| 50 mg | Get quote | ||
| 100 mg | Get quote |
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P3FI-90 is a specific small molecule inhibitor of KDM3B with SPR KD of 7.68 uM, inhibits PAX3-FOXO1 activityand blocks PAX3-FOXO1 downstream target gene expression.
P3FI-90 can phenocopies shRNA knockdown of PAX3-FOXO1 when considering the sum of normalized enrichment scores of downregulated PAX3-FOXO1 gene sets.
P3FI-90 does not decrease the amount of PAX3-FOXO1 protein.
P3FI-90 downregulatesthe target genes of PAX3-FOXO1 in fusion-positive rhabdomyosarcoma (FP-RMS) and had broad activity in other pediatric solid tumor cell lines.
P3FI-90 inhibits multiple KDMs including KDM3B, KDM4B, KDM5A, and KDM6B, with highest potency against KDM3B with IC50 of 7 uM.
P3FI-90 shows no inhibitory activity against HDAC1, HDAC2, HDAC3, or PRMT5.
P3FI-90 increases H3K4 and H3K9 methylation.
P3FI-90 shows sub-micromolar EC50 activity in fusion-positive rhabdomyosarcoma (FP-RMS) (RH4, EC50=0.9 uM).
P3FI-90 decreases chromatin loop strength and decreases topologically associating domains (TADs) at PAX3-FOXO1 sites.
P3FI-90 inhibits multiple KDMs with highest selectivity for KDM3B.
P3FI-90 also exerts potent growth inhibitory activity on Ewing's sarcoma and osteosarcoma cell lines.
P3FI-90 effectively inhibits FP-RMS tumor growth in mouse models of RMS without significant weight loss at 25 mg/kg.
| M.Wt | 214.23 | |
| Formula | C11H10N4O | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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| Chemical Name/SMILES |
N'-(pyridin-2-yl)picolinohydrazide |
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1. Kim YY, et al. Nat Commun. 2024 Feb 24;15(1):1703.
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