SML4130
PFI-90
≥98% (HPLC)
Synonym(s):
2-Pyridinecarboxylic acid 2-(2-pyridinyl)hydrazide, KDM3B Inhibitor PFI-90, PAX3-FOXO1 transcriptional Inhibitor 90, N′-(Pyridin-2-yl)picolinohydrazide
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About This Item
Quality Level
Assay
≥98% (HPLC)
form
powder
color
white to beige
solubility
DMSO: 2 mg/mL, clear
storage temp.
2-8°C
SMILES string
N(NC(=O)c2ncccc2)c1ncccc1
O=C(C1=NC=CC=C1)NNC2=NC=CC=C2
InChI
1S/C11H10N4O/c16-11(9-5-1-3-7-12-9)15-14-10-6-2-4-8-13-10/h1-8H,(H,13,14)(H,15,16)
InChI key
GCZPXNWBXDWHKM-UHFFFAOYSA-N
Biochem/physiol Actions
PFI-90 directly targets and binds to metal ions in KDMs′ active sites, showing a strong preference for KDM3B (KD = 7.68 μM) while demonstrating minimal effect on other histone demethylases like KDM1A, KDM4B, KDM5A, KDM6B, HDAC1, HDAC2, HDAC3, and PRMT5. This selectivity leads to increased methylation at H3K4 and H3K9, disrupting the transcription of PAX3-FOXO1 oncogene targets in fusion-positive rhabdomyosarcoma (FP-RMS). PFI 90 effectively inhibits growth in PAX3-FOXO1 positive RMS cell lines (SCMC, RH4, RH30) with EC50 = 0.4, 0.9 and 3.2 µM, respectively. PFI-90 suppresses PAX3-FOXO1 function, inducing apoptosis and reducing RNA Pol2 activity without affecting PAX3-FOXO1 protein levels or DNA binding. Its treatment hampers FP-RMS tumor growth in vivo, offering a promising therapeutic avenue by selectively targeting KDM3B to combat FP-RMS.
Storage Class Code
11 - Combustible Solids
WGK
WGK 3
Flash Point(F)
Not applicable
Flash Point(C)
Not applicable
Regulatory Information
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