I-BET151 (GSK1210151A)

그림문자(GHS)

• 그림문자(GHS)

  

• 신호 어

  Danger

• 유해·위험 문구

  H301：삼키면 유독함

• 예방조치문구

  P301+P310：삼켰다면 즉시 의료기관(의사)의 진찰을 받으시오.

I-BET151 (GSK1210151A) 화학적 특성, 용도, 생산

• 개요

  The bromodomain and extra terminal domain (BET) family of proteins including BRD2, BRD3, and BRD4 play a key role in many cellular processes, including inflammatory gene expression, mitosis, and viral/host interaction by controlling the assembly of histone acetylation-dependent chromatin complexes. I-BET151 is an isoxazole class pan-BET family inhibitor, blocking BRD2, BRD3, and BRD4 with IC₅₀ values of 0.5, 0.25, and 0.79 μM, respectively. Through this action, it blocks the growth of leukemic cell lines driven by mixed lineage leukemia (MLL) fusions at nanomolar concentrations, whereas tyrosine kinase activated cells were much less sensitive. Specifically, I-BET151 induces apoptosis via reduced expression of BCL2 or triggers G₀/G₁ cell cycle arrest in MLL-fusion cell lines. I-BET151 is effective in vivo, suppressing MLL leukemia progression in two different mouse models.

• 화학적 성질

  Off-White Solid

• 용도

  I-BET 151 is part of a novel series of quinoline isoxazole BET family bromodomain inhibitors, a family of four proteins that selectively bind to aceylated lysine residues in histone. I-BET 151 play ke y roles in many cellular processes, including anti-inflammatory gene expression, mitosis, and viral/host interaction by controlling the conformation of histone acetylation -dependent chromatin complex es. Studies have shown that I-BET 151 increased ApoA1 expression within the nanomolar range in human hepatic cell line HepG2. The upregulation by I-BET 151 suggested potential anti-inflammatory activi ties upon administration.

I-BET151 (GSK1210151A) 준비 용품 및 원자재

I-BET151 (GSK1210151A) 공급 업체

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