656222-54-7
中文名稱
2-(2-氰基乙?；?-N-(3,4-二氯苯基)肼基硫代甲酰胺
英文名稱
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
2024/12/15 19:35:19
656222-54-7 結(jié)構(gòu)式
基本信息
中文別名
化合物IKIX12-(2-氰基乙?；?-N-(3,4-二氯苯基)肼基硫代甲酰胺
英文別名
iKIX12-Cyano-N-{[(3,4-dichlorophenyl)carbamothioyl]amino}acetamide
物理化學(xué)性質(zhì)
密度1.551±0.06 g/cm3(Predicted)
儲存條件-20°C儲存
溶解度可溶于DMSO
酸度系數(shù)(pKa)3.76±0.10(Predicted)
形態(tài)結(jié)晶固體
顏色Off-white to light yellow
應(yīng)用領(lǐng)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.