Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T3693 |
DHFR-IN-3
7-bromoquinazoline-2,4-diamine,7-溴-2,4-二氨基喹唑啉 |
Others | Others |
DHFR-IN-3 (7-bromoquinazoline-2,4-diamine) 是一种活性生化剂。 | |||
T4197 |
HZ-1157
HZ1157,DHFR-inhibitor |
HCV Protease | Microbiology/Virology; Proteases/Proteasome |
HZ-1157 (DHFR-inhibitor) 是一种丙型肝炎病毒抑制剂,对 HCV NS3/4A 蛋白酶具有抑制活性。 | |||
T61486 | DHFR-IN-4 | DHFR | Cell Cycle/Checkpoint; DNA Damage/DNA Repair; Metabolism |
DHFR-IN-4 是一种高效的二氢叶酸还原酶 (DHFR) 抑制剂,具有抗肿瘤活性,抑制 EGFR 和 HER2 ,可用于研究胰腺癌。 | |||
T63379 |
DHFR-IN-1
|
||
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。 | |||
T79735 |
DHFR-IN-9
|
||
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)。 | |||
T82570 | DHFR-IN-11 | ||
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。 | |||
T79734 |
DHFR-IN-8
|
||
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。 | |||
T60286 | DHFR-IN-2 | ||
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。 | |||
T73328 |
DHFR-IN-5
|
||
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]。 | |||
T82571 |
DHFR-IN-10
|
||
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。 | |||
T82492 | EGFR/HER2/DHFR-IN-3 | 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。 | |||
T82493 | EGFR/HER2/DHFR-IN-2 | 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。 | |||
T61229 | VEGFR-2/DHFR-IN-2 | ||
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]. | |||
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。 | |||
T36692 |
Fanotaprim
|
DHFR | Cell Cycle/Checkpoint; DNA Damage/DNA Repair; Metabolism |
Fanotaprim 是二氢叶酸还原酶的有效抑制剂,抑制 tgDHFR (Toxoplasma gondiiDHFR) 和 hDHFR (human DHFR)的 IC50分别为 1.57 和 308 nM。Fanotaprim 在研究弓形虫病方面具有价值。 | |||
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]. | |||
T81381 |
PROTAC eDHFR Degrader-1
|
PROTACs | PROTAC |
PROTACeDHFR Degrader-1是一种高效的PROTAC,针对eDHFR-YFP和多种POI(如YFP、荧光素酶)具有显著的降解作用。 | |||
T0849 |
Pyrimethamine
Pirimecidan,RP 4753,Pirimetamin,乙胺嘧啶 |
DHFR; Antifolate; Parasite | Cell Cycle/Checkpoint; DNA Damage/DNA Repair; Metabolism; Microbiology/Virology |
Pyrimethamine (Pirimecidan) 是一种二氢叶酸还原酶的竞争性抑制剂,用作抗疟药。 | |||
T1485 |
Methotrexate
NCI-C04671,WR19039,Amethopterin,甲氨蝶呤,CL14377 |
Apoptosis; Dehydrogenase; DNA/RNA Synthesis; Antifolate | Apoptosis; Cell Cycle/Checkpoint; DNA Damage/DNA Repair; Metabolism |
Methotrexate (WR19039) 是一种叶酸类似物,一种二氢叶酸还原酶 DHFR 的抑制剂。Methotrexate 具有抗代谢、抗肿瘤和免疫抑制等活性,常用于类风湿关节炎和多种肿瘤的研究。 | |||
T6226 |
Pemetrexed disodium hemipenta hydrate
培美曲塞二钠一水合物,Pemetrexed Disodium Hydrate,LY-231514 Disodium Hydrate,Pemetrexed sodium hydrate,培美曲塞二钠水合物 |
Apoptosis; DHFR; DNA/RNA Synthesis; Antifolate; Autophagy | Apoptosis; Autophagy; Cell Cycle/Checkpoint; DNA Damage/DNA Repair; Metabolism |
Pemetrexed disodium hemipenta hydrate (LY-231514 Disodium Hydrate) 是一种叶酸拮抗剂。抑制胸苷酸合成酶 (TS),二氢叶酸还原酶 (DHFR) 和甘氨酰胺核苷酸甲酰转移酶 (GARFT),Ki 分别为 1.3 nM,7.2 nM 和 65 nM。 | |||
T61159 |
Antibacterial agent 26
|
Antibacterial | Microbiology/Virology |
Antibacterial agent 26 是一种抗菌化合物,是有效的DHFR 抑制剂(金黄色葡萄球菌DHFR Ki 为0.020 nM)。 | |||
T19858 |
Brodimoprim
|
DHFR; Antibacterial | Cell Cycle/Checkpoint; DNA Damage/DNA Repair; Metabolism; Microbiology/Virology |
Brodimoprim 是甲氧苄啶的一种类似物,是口服有效的二氢叶酸还原酶抑制剂,对广谱革兰氏阴性和革兰氏阳性细菌具有高度的抑制作用。 | |||
T64295 |
Talotrexin ammonium
|
DHFR | Cell Cycle/Checkpoint; DNA Damage/DNA Repair; Metabolism |
Talotrexin ammonium 是一种不可多聚谷氨酸抗叶酸类药物。Talotrexin ammonium 通过针对二氢叶酸还原酶(DHFR)来抑制肿瘤生长,从而提高了在广泛癌症模型中的抗肿瘤活性,有助于抑制肿瘤的增长。 | |||
T2204 |
Diaveridine
二氨藜芦啶,EGIS-5645,敌菌净,CCRIS-3784,AI3-23935 |
DHFR; Antifolate; Antibacterial | Cell Cycle/Checkpoint; DNA Damage/DNA Repair; Metabolism; Microbiology/Virology |
Diaveridine (AI3-23935) 是二氢叶酸还原酶的抑制剂,对于野生型 DHFR 的Ki 值为 11.5 nM。它也是一种抗菌剂。 | |||
T6120 |
Pralatrexate
Folotyn,10-炔丙基-10-去氮杂氨基蝶呤,10-Propargyl-10-deazaaminopterin,普拉曲沙 |
Apoptosis; DHFR; Antifolate; TAM Receptor | Apoptosis; Cell Cycle/Checkpoint; DNA Damage/DNA Repair; Metabolism; Tyrosine Kinase/Adaptors |
Pralatrexate (10-Propargyl-10-deazaaminopterin) 是一种抗叶酸剂,也是二氢叶酸还原酶抑制剂,Ki 值为 13.4 pM。它具有抗肿瘤活性,可研究复发/难治性 T 细胞淋巴瘤。它是叶酰聚谷氨酸合成酶的底物,具有改善的细胞摄取和保留能力。 | |||
T17257 |
WR99210
|
DHFR; Antifolate; Antibacterial | Cell Cycle/Checkpoint; DNA Damage/DNA Repair; Metabolism; Microbiology/Virology |
WR99210 是一种有效的、可口服的且毒性较低的二氢叶酸还原酶 (DHFR) 抑制剂 (IC50<0.075 nM)。WR99210 具有较好的抗寄生虫活性,对间日疟原虫和恶性疟原虫株 (包括耐 Pyrimethamine 的恶性疟原虫株) 以及弓形虫有良好的抑制作用。 | |||
T79192 |
DQn-1
|
||
DQn-1作为高效的抗叶酸剂,对结核分枝杆菌(Mtb)展现出显著活性(MIC90=0.03 µM),能够直接抑制DHFR enzyme的功能。其对Mtb DHFR enzyme的IC50值为8.7 nM,而对人DHFR enzyme的IC50值则为7.6 nM。 | |||
T27002 |
CH-1504
CH 1504,MobileTrex |
||
CH-1504, dihydrofolate reductase (DHFR) inhibitor, is used potentially for the treatment of rheumatoid arthritis. | |||
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]. | |||
T40619 |
Tetroxoprim
HE 781,Tetroxoprim |
||
Tetroxoprim is an antimicrobial DHFR inhibitor. | |||
T24966 |
11-Oxahomoaminopterin
NSC-325304,NSC 325304,NSC325304 |
||
11-Oxahomoaminopterin exhibits antifolate activity against two folate-requiring microorganisms and inhibited Lactobacillus casei DHFR. | |||
T25981 | Pralatrexate, (S)- | ||
Pralatrexate, (S)- is a folate analog dihydrofolate reductase (DHFR) inhibitor exhibiting high affinity for reduced folate carrier-1 (RFC-1) with antineoplastic and immunosuppressive activities. Pralatrexate selectively enters cells expressing RFC-1; intr | |||
T60726 |
OYYF-175
|
||
OYYF-175 是一种抗菌抗叶酸剂。OYYF-175具有有效的广谱抗菌活性,尤其是针对多重耐药革兰氏阴性菌株。OYYF-175是一种二氢叶酸还原酶 (DHFR) 抑制剂,其对大肠杆菌 DHFR 的 IC50为 2.36 nM。 | |||
T25980 |
Pralatrexate, (R)-
|
||
Pralatrexate, (R)- is a folate analog dihydrofolate reductase (DHFR) inhibitor exhibiting high affinity for reduced folate carrier-1 (RFC-1) with antineoplastic and immunosuppressive activities. Pralatrexate selectively enters cells expressing RFC-1; intr | |||
T78238 |
4′-DTMP
4-Demethyltrimethoprim |
DHFR; Antifungal | Cell Cycle/Checkpoint; DNA Damage/DNA Repair; Metabolism; Microbiology/Virology |
4′-DTMP (4-Demethyltrimethoprim) 是一种有效的 DHFR 抑制剂,具有抗菌活性,诱导与酶的额外局部相互作用,对大肠杆菌具有抑制作用。 | |||
T70304 |
CI-898 HCl
|
||
CI-898 HCl is a lipophilic antifolate inhibitor of dihydrofolate reductase (DHFR). It has enhanced binding to DHFR in the presence of the cofactor NADPH. Cl-898 HCl inhibits cell growth and halts the cell cycle at the G1/S phase in L1210 mouse lymphocytic leukemia cells and is active against methotrexate-resistant cancer cell lines. It also enhances the activity of doxorubicin, cyclophosphamide, and 6-thioguanine (6-TG) in mice with advanced stage P338 leukemia. | |||
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。 | |||
T60699 | Aditoprime | ||
Aditoprime (Aditoprim) 是细菌二氢叶酸还原酶(DHFR)的选择性抑制剂。Aditoprime 抑制二氢叶酸向四氢叶酸的转化。Aditoprime 显示出良好的抗菌活性,具有广谱抗菌性,并且显示出良好的药代动力学。Aditoprime 抑制干酪乳杆菌和大肠杆菌 DHFR 的 IC50分别为520和47 nM。 | |||
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]. | |||
T68684 |
Piritrexim isethionate
|
||
Piritrexim isethionate is a lipid-soluble inhibitor of dihydrofolate reductase (DHFR) that appears to be an active agent in patients with metastatic urothelial cancer when administered as a 5-day, low-dose oral schedule. | |||
T73085 |
Talotrexin
PT523 |
||
Talotrexin (PT523) 是一种 Aminopterin 的类似物,是一种非聚谷氨酸化的经典抗叶酸剂 (antifolate)。 Talotrexin 是一种 RFC(还原型叶酸载体)的特异性抑制剂,可选择性地抑制 RFC 转运。Talotrexin 通过靶向 DHFR 抑制肿瘤生长显示出抗肿瘤活性。 | |||
T0189 |
Pemetrexed
Pemetrexed acid,培美曲塞,LY231514,培美曲唑,LY-231514 Disodium Hydrate |
DHFR; DNA/RNA Synthesis; Antifolate; Autophagy | Autophagy; Cell Cycle/Checkpoint; DNA Damage/DNA Repair; Metabolism |
Pemetrexed (LY-231514 Disodium Hydrate) acid 是一种鸟嘌呤衍生的抗肿瘤药物,可结合并抑制胸苷酸合酶、二氢叶酸还原酶和甘氨酰胺核苷酸甲酰转移酶的 Ki 分别为 1.3 nM、7.2 nM 和 65 nM。 | |||
T0189L |
Pemetrexed disodium
培美曲塞二钠盐,LY-231514,LY231514 disodium,培美曲塞二钠,Pemetrexed |
Apoptosis; DHFR; DNA/RNA Synthesis; Antifolate; Autophagy | Apoptosis; Autophagy; Cell Cycle/Checkpoint; DNA Damage/DNA Repair; Metabolism |
Pemetrexed disodium (LY-231514) 是一种叶酸拮抗剂,用于治疗非小细胞肺癌和恶性间皮瘤。它抑制胸苷酸合成酶,二氢叶酸还原酶和甘氨酰胺核苷酸甲酰转移酶的Ki 分别为 1.3 nM,7.2 nM 和 65 nM。 | |||
T41148 |
Phototrexate
|
||
Phototrexate is a photoswitchable potent inhibitor of human dihydrofolate reductase (DHFR). Phototrexate is a photochromic analog of Methotrexate. Antifolate activity is switched on (cis-Phototrexate) by UVA (375 nm) light; it can be switched off (trans-Phototrexate) by blue or white light and by thermal relaxation in the dark.cis-Phototrexate (IC50 = 6 nM) significantly reduces the viability of HeLa cells compared withtrans-Phototrexate (IC50 = 34 μM). | |||
T68656 |
Brivudine monophosphate
|
||
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... | |||
T81639 |
NSC309401 dihydrochloride
|
||
NSC309401为大肠杆菌DHFR抑制剂,具有IC50值为189 nM和KD值为14.57 nM。 | |||
T79912 |
NSC309401
|
||
NSC309401 是一种针对大肠杆菌DHFR的抑制剂,具有IC50值为189 nM和KD值为14.57 nM。 | |||
T78964 | Antileishmanial agent-17 | Parasite | Microbiology/Virology |
Antileishmanial agent-17是香豆素杂化化合物,展现出优越的抗利什曼原虫活性(IC50<0.78 μM),同时对VERO细胞具备安全性。该化合物通过抑制叶酸代谢途径发挥效用,且在对抗利什曼原虫不同生长阶段表现显著,其IC50值分别对前鞭毛体为0.40 μM,对无鞭毛体为0.68 μM。 |