Cat. No. | Product Name | Target | Signaling Pathways |
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T63379 |
DHFR-IN-1
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DHFR-IN-1 是选择性的、有效的 DHFR (二氢叶酸还原酶)抑制剂 (IC50: 40.71 nM)。 DHFR-IN-1 表现出一定的抗真菌效果,并对革兰氏阳性菌和革兰氏阴性菌表现出良好的抗菌活性。DHFR-IN-1 与 Levofloxacin 表现出较好的协同作用,FIC (部分抑菌浓度指数)=0.249。 | |||
T61489 | VEGFR-2/DHFR-IN-1 | ||
VEGFR-2/DHFR-IN-1 (compound 8b) 是 VEGFR-2和DHFR 的抑制剂,其IC50值分别为 0.384 和 7.881 μM。VEGFR-2/DHFR-IN-1 对大肠埃希菌,粪链球菌,肠沙门氏菌,金黄色酿脓葡萄球菌,MSSA 和MRSA 显示了良好的抗菌活性,MIC 值分别为 16,16,16,8 和 16 μg/mL。VEGFR-2/DHFR-IN-1 对 C26,HepG2 和 CF7 癌细胞系具有良好的细胞毒性,IC50值为 2.97-7.12 μM。VEGFR-2/DHFR-IN-1 可用于癌症的研究。 | |||
T61596 | EGFR/HER2/DHFR-IN-1 | ||
EGFR/HER2/DHFR-IN-1 is a highly selective and potent anticancer compound specifically targeting MCF-7 breast cancer cells. It acts as a multi-inhibitor, targeting the EGFR/HER2 kinase and DHFR enzymes, with IC50 values of 0.153 μM, 0.108 μM, and 0.291 μM, respectively. Its mechanism of action involves cell cycle arrest at the G1/S phase and induction of apoptosis in cells [1]. | |||
T82570 |
DHFR-IN-11
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DHFR-IN-11(化合物6b)作为一种DHFR抑制剂,特别针对结核分枝杆菌的DHFR酶表现出抑制效果,其IC50为5.70 μM。 | |||
T82571 |
DHFR-IN-10
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DHFR-IN-10(化合物4c)是针对结核分枝杆菌DHFR的高效抑制剂,其IC50为4.21 μM,显示出卓越的抗结核活性。 | |||
T73328 |
DHFR-IN-5
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DHFR-IN-5 是一种有效且具有口服活性的二氢叶酸还原酶 (DHFR) 抑制剂,对Plasmodiumfalciparum 突变体的Ki 值为 0.54 nM。DHFR-IN-5显示抗疟疾活性[1]。 | |||
T61272 | EGFR/HER2-IN-7 | ||
EGFR/HER2-IN-7 is a highly selective and potent anticancer compound specifically designed to target MCF-7 breast cancer cells. It functions as a dual inhibitor, targeting both EGFR/HER2 kinases and DHFR (dihydrofolate reductase). Its inhibitory activities are measured with IC50 values of 0.18 μM for EGFR, 0.146 μM for HER2, and 0.907 μM for DHFR [1]. | |||
T61229 |
VEGFR-2/DHFR-IN-2
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VEGFR-2/DHFR-IN-2 (compound 5b) is a dual inhibitor targeting VEGFR-2 and DHFR, with respective IC50 values of 0.623 μM and 9.085 μM. It demonstrates potent cytotoxicity against C26, HepG2, and MCF7 cancer cell lines, with IC50 values ranging from 3.59 μM to 8.38 μM. VEGFR-2/DHFR-IN-2 holds promise for cancer research [1]. | |||
T82492 |
EGFR/HER2/DHFR-IN-3
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EGFR | Angiogenesis; JAK/STAT signaling; Tyrosine Kinase/Adaptors |
EGFR/HER2/DHFR-IN-3(compound 4c)是一种针对EGFR和HER2的高效双重抑制剂,其IC50分别为0.138 μM和0.092 μM。该化合物同时对DHFR具有抑制作用,IC50为0.193 M。在生物活性方面,EGFR/HER2/DHFR-IN-3能够导致MCF7乳腺癌细胞周期在S期发生阻滞,并进而诱导细胞凋亡。 | |||
T60938 | EGFR/HER2-IN-8 | ||
EGFR/HER2-IN-8 (compound 34) 是EGFR/HER2和DHFR 的抑制剂,其对 EGFR,HER2 和 DHFR 的IC50值分别为 0.45,0.244 和 5.669 μM。EGFR/HER2-IN-8 可用于癌症研究,它对多种癌细胞系表现出抗癌活性,具有高安全性和选择性指数。 | |||
T61732 | EGFR/HER2-IN-6 | ||
EGFR/HER2-IN-6 (compound 43) is a dual EGFR/HER2 and DHFR inhibitor with potent activity against EGFR kinase, HER2 kinase, and DHFR, characterized by IC50 values of 0.122 μM, 0.078 μM, and 0.585 μM, respectively. This compound displays notable anticancer properties in various cancer cell lines, while demonstrating a favorable safety profile and selectivity indices. Consequently, EGFR/HER2-IN-6 holds promise as a valuable tool in cancer research [1]. | |||
T79735 |
DHFR-IN-9
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DHFR-IN-9(化合物8A)是一种二氢叶酸还原酶(DHFR)抑制剂,通过干扰细胞内嘌呤和胸苷酸的生物合成而影响细胞生长和增殖。该化合物对抗耐甲氧西林金黄色葡萄球菌(MRSA)ATCC 43300展现出显著的抑制效果(IC50=0.25 μg/mL),并在全身及大腿感染的小鼠模型中显示出抗感染能力(剂量:2.5 mg/kg,5 mg/kg;ip)。此外,DHFR-IN-9在乳腺癌小鼠模型中展示了超过紫杉醇(Y-B0015)的抗癌活性(剂量:2.5 mg/kg;ip;每3天1次)。 | |||
T82493 |
EGFR/HER2/DHFR-IN-2
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EGFR | Angiogenesis; JAK/STAT signaling; Tyrosine Kinase/Adaptors |
EGFR/HER2/DHFR-IN-2 (Compound 4b) 是针对EGFR、HER2和DHFR的三重抑制剂,IC50分别为0.248、0.156、0.138 μM。该化合物对包括Hep G2, HeLa, HEp-2, HCT 116, PC-3, MCF7在内的多种癌细胞系展现出显著的抗癌活性(IC50分别为9.14、7.33、14.18、24.87、20.07、6.16 μM),并能有效减缓乳腺癌肿瘤的生长。 | |||
T60286 |
DHFR-IN-2
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DHFR-IN-2 (化合物 4e) 是一种有效且非竞争性的MtDHFR 抑制剂,其IC50值为 7 μM。来自结核分枝杆菌 (MtDHFR) 的二氢叶酸还原酶具有很高的未开发潜力,可以成为抗结核病 (TB) 新药的靶标,因为它对病原体存活很重要。DHFR-IN-2可用于结核病(TB)研究。 | |||
T79734 |
DHFR-IN-8
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DHFR-IN-8 (compound 6r) 是一种抑制二氢叶酸还原酶(DHFR)的化合物,能够阻断嘌呤与胸苷酸的生物合成,从而影响细胞增殖与生长。该化合物对耐甲氧西林金黄色葡萄球菌(MRSA)ATCC 43300表现出高效的抑制活性(IC50=15.6 ng/mL),并在小鼠全身及大腿感染模型中展示了抗感染效果,用药剂量为60 mg/kg,通过腹腔注射(ip)给药。 | |||
T68656 |
Brivudine monophosphate
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Brivudine monophosphate is a phosphate ester of Brivudine. Brivudine, also known as bromovinyl-deoxyuridine, is a uridine derivative and nucleoside analog with pro-apoptotic and chemosensitizing properties. In vitro, bromovinyl-deoxyuridine (BVDU) has been shown to downregulate the multifunctional DNA repair enzyme APEX nuclease 1, resulting in the inhibition of DNA repair and the induction of apoptosis. In addition, this agent may inhibit the expression of STAT3 (signal transducer and activator... |