P3FI-90 | KDM3B inhibitor | Probechem Biochemicals

Chemical Structure : P3FI-90

CAS No.: 53995-62-3

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P3FI-90 (PAX3-FOXO1 transcriptional Inhibitor 63)

货号: 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 activity and blocks PAX3-FOXO1 downstream target gene expression.

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5 mg	￥1780	In stock
10 mg	￥2880	In stock
25 mg	￥4580	In stock
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100 mg		Get quote

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生物&药学活性

P3FI-90 is a specific small molecule inhibitor of KDM3B with SPR KD of 7.68 uM, inhibits PAX3-FOXO1 activity and 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.

物理化学性质&存储条件

分子量	214.23
分子式	C11H10N4O
外观性状	Solid
CAS No.
储存条件	固体粉末 -20°C 12 个月; 4°C 6 个月	配置液 -80°C 6 个月; -20°C 6 个月
Shipping
Solubility	10 mM in DMSO
Chemical Name/SMILES	N'-(pyridin-2-yl)picolinohydrazide

参考文献

1. Kim YY, et al. Nat Commun. 2024 Feb 24;15(1):1703.

P3FI-90 (PAX3-FOXO1 transcriptional Inhibitor 63)

生物&药学活性

物理化学性质&存储条件

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P3FI-90 (PAX3-FOXO1 transcriptional Inhibitor 63)

生物&药学活性

物理化学性质&存储条件

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