SML4083
TJ-M2010-5
≥98% (HPLC)
别名:
3-(4-Benzyl-piperazin-1-yl)-N-(4-phenylthiazol-2-yl)propionamide, 3-(4-Benzylpiperazin-1-yl)-N-(4-phenylthiazol-2-yl)propanamide, 4-(Phenylmethyl)-N-(4-phenyl-2-thiazolyl)-1-piperazinepropanamide, TJ-5, TJM2010-5
质量水平
方案
≥98% (HPLC)
表单
powder
颜色
white to beige
溶解性
DMSO: 2 mg/mL, clear
储存温度
2-8°C
SMILES字符串
O=C(CCN1CCN(CC1)CC2=CC=CC=C2)NC3=NC(C4=CC=CC=C4)=CS3
生化/生理作用
TIR domain-targeting MyD88 homodimerization inhibitor that blocks MyD88 signaling and prevents colitis-associated cancer (CAC) development in vivo.
TJ-M2010-5 (TJ-5) is a TIR domain-targeting MyD88 homodimerization inhibitor (67% inhibition of HEK293 cellular MyD88 interaction at 20 µM) that blocks IRAK4, ERK and p38 phosphorylation induction by LPS stimulation (100 ng/mL for 6h with or without 40 µM TJ-5) in RAW 264.7 cells. TJ-5 (50 mg/kg/d i.p.) significantly reduces AOM/DSS-induced colitis and completely prevents colitis-associated cancer (CAC) development and death (53% mortality of control mice) in mice in vivo.
TJ-M2010-5 (TJ-5) is a TIR domain-targeting MyD88 homodimerization inhibitor (67% inhibition of HEK293 cellular MyD88 interaction at 20 µM) that blocks IRAK4, ERK and p38 phosphorylation induction by LPS stimulation (100 ng/mL for 6h with or without 40 µM TJ-5) in RAW 264.7 cells. TJ-5 (50 mg/kg/d i.p.) significantly reduces AOM/DSS-induced colitis and completely prevents colitis-associated cancer (CAC) development and death (53% mortality of control mice) in mice in vivo.
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