656222-54-7
中文名称
2-(2-氰基乙酰基)-N-(3,4-二氯苯基)肼基硫代甲酰胺
英文名称
iKIX1
CAS
656222-54-7
分子式
C10H8Cl2N4OS
分子量
303.17
MOL 文件
656222-54-7.mol
更新日期
2024/10/07 18:47:55
656222-54-7 结构式
基本信息
中文别名
化合物IKIX12-(2-氰基乙酰基)-N-(3,4-二氯苯基)肼基硫代甲酰胺
英文别名
iKIX12-Cyano-N-{[(3,4-dichlorophenyl)carbamothioyl]amino}acetamide
物理化学性质
密度1.551±0.06 g/cm3(Predicted)
储存条件-20°C储存
溶解度可溶于DMSO
酸度系数(pKa)3.76±0.10(Predicted)
形态结晶固体
颜色Off-white to light yellow
应用领域
用途一
iKIX1 is an inhibitor of interactions between the transcription co-activator Mediator complex and the pleitropic drug resistance (CgPdr1) transcription factor in the pathogen C. glabrata. It inhibits the interaction between the KIX domain of the Mediator subunit CgGal11A and the activation domain of CgPdr1 (IC50 = 190.2 μM). iKIX1 (10 and 30 μM) inhibits ketoconazole-induced expression of CgPdr1-target genes involved in multidrug resistance and drug efflux in C. glabrata. It increases the sensitivity of azole-resistant C. glabrata strains expressing CgPDR1 gain-of-function mutations to the antifungal compounds fluconazole and ketoconazole in a concentration-dependent manner. iKIX1 (100 mg/kg) decreases fungal burden in the kidney and spleen in a mouse model of infection with azole-sensitive or -resistant C. glabrata when administered in combination with low and high doses of fluconazole, respectively.