登录并加购，请在购物车里查看协议价、货期和发货地。
选择规格
变更视图
关于此项目
经验公式（希尔记法）:
C11H10N4O
化学文摘社编号:
分子量:
214.22
MDL number:
NACRES:
NA.21
UNSPSC Code:
12352200
Assay:
≥98% (HPLC)
Form:
powder
Quality Segment
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
selective KDM3B inhibitor, disrupts PAX3-FOXO1 mediated transcription in FP-RMS.
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.
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.
存储类别
11 - Combustible Solids
怎么回事？
WGK 3
闪点 (F)
Not applicable
闪点 (°C)
Not applicable