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首页-抗体药物偶连体和PROTACs-PROTAC-KTX-545
KTX-545

Chemical Structure : KTX-545

CAS No.: 2432992-21-5

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KTX-545 (KTX545)

货号: PC-26875Not For Human Use, Lab Use Only.

KTX-545 (KTX545) is a potent, selective IRAK4-targeting degrader with DC50 of 0.9 nM determined in in vitro assays with human monocytes.

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纯度 & COA & 质检文件 纯度: >98% (HPLC)

生物&药学活性

KTX-545 (KTX545) is a potent, selective IRAK4-targeting degrader with DC50 of 0.9 nM determined in in vitro assays with human monocytes.
IRAK4 is the only protein degraded of over 10,000 different proteins in human peripheral blood mononuclear cells (PBMCs) incubated with a concentration of KTX-545 ten-fold over its DC90.
KTX-545 specifically links the Cereblon (CRBN) domain binding the E3 ligase to IRAK4, induces ubiquitination and degradation by the 26S proteasome with IC50 of 60 nM (CRBN) and 11 nM (IRAK4).
KTX-545 induces impairment of myddosome formation and a significant reduction of NF-kB-driven gene expression in isolated primary mouse kSFCs.
KTX-545 significantly reduces the expression of the myofibroblast marker gene Acta2 encoding myofibroblast smooth muscle actin (Sma), the extracellular matrix protein encoding genes Col1a1, Fn1 and Fbn1 and the cytokines Tgfb and Ctgf.
KTX-545 shows increased efficacy compared to the small molecule IRAK4 kinase inhibitor CA-4948 in ameliorating fibrosis following ischemia/reperfusion injury. 

物理化学性质&存储条件

分子量 843.95
分子式 C44H52F3N9O5
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

2-Pyridinecarboxamide, N-[2-[trans-4-[[[1-[[1-(2,6-dioxo-3-piperidinyl)-2,3-dihydro-3-methyl-2-oxo-1H-benzimidazol-4-yl]methyl]-4-piperidinyl]methylamino]methyl]cyclohexyl]-6-(1-hydroxy-1-methylethyl)-2H-indazol-5-yl]-6-(trifluoromethyl)-

参考文献

1. Lopez-Marfil M, et al. Commun Biol. 2026 May 25. doi: 10.1038/s42003-026-10271-3.

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