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首页-小分子抑制剂&激动剂-Epigenetics-Histone Methyltransferase (HMTase)-BCOR-PCGF1 inhibitor iBP
BCOR-PCGF1 inhibitor iBP

Chemical Structure : BCOR-PCGF1 inhibitor iBP

CAS No.: 879790-53-1

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BCOR-PCGF1 inhibitor iBP (Inhibitor of BCOR-PCGF1)

货号: PC-24609Not For Human Use, Lab Use Only.

BCOR-PCGF1 inhibitor iBP is a selective PRC1.1 inhibitor, specifically inhibits the interaction between BCOR and PCGF1 with IC50 of 12.21 uM in AlphaScreen assays, limits H2AK119ub1 activity and activates Wnt signaling pathway.

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纯度 & COA & 质检文件 纯度: >98% (HPLC)

生物&药学活性

BCOR-PCGF1 inhibitor iBP is a selective PRC1.1 inhibitor, specifically inhibits the interaction between BCOR and PCGF1 with IC50 of 12.21 uM in AlphaScreen assays, limits H2AK119ub1 activity and activates Wnt signaling pathway.
iBP has affinity for PCGF1RAWUL L238A/F242A with a dissociation constant (Kd) of 6.42 uM.
iBP (5-10 uM) is sufficient to inhibit the interaction between PCGF1 and BCOR, without disrupting PRC2 or PRC1.4 integrity.
iBP (10 uM) reduces total H2AK119ub1 levels in 293 T cells, reduces the enrichment of PCGF1, RING1B and H2AK119ub1 levels specifically at target promoter regions.
iBP treatment (20 mg/kg daily, i.p.) enhances OB functions and reverses bone loss in OVX models, enhances upregulation in the expression of osteogenic marker genes and Wnt/β-catenin target genes, effectively activates Wnt signaling and prevents osteoporosis.
iBP enhances osteogenic functions in mouse models of osteoporosis and acute trauma, promotes new bone formation in vivo.

物理化学性质&存储条件

分子量 332.36
分子式 C20H16N2O3
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

3-(hydroxyimino)-1-(2-(naphthalen-1-yloxy)ethyl)indolin-2-one

参考文献

1. Xing L, et al. Nat Commun. 2025 May 8;16(1):4294.

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