DHFR
DHFR is a relatively small water-soluble protein with a molecular weight of 18.000–25.000 Da. DHFR consists of eight sheets, which form a rigid skeleton: seven sheets run parallel and the other runs antiparallel. All the enzyme isoforms contain at least four α-helices intersecting in the long loops of the sheets. The potential of the dihydrofolate reductase (DHFR) enzyme as a therapeutic target for treating infections has been evidenced. DHFR catalyzes the reduction of dihydrofolate to tetrahydrofolate using NADPH, an essential cofactor in the biosynthesis of thymidylate monophosphate (dTMP) and it is involved in the synthesis of raw material for cell proliferation, in both prokaryotic and eukaryotic cells. Inhibition of DHFR leads to a deficiency of dTMP since DHF cannot be recycled, and thus causes inhibition of cell growth.
References
1.Maria Valeria Raimondi,et al. Molecules. 2019 Mar; 24(6): 1140.
2.Gangjee A,et al. Curr Pharm Des. 2007;13(6):609-39.
References
1.Maria Valeria Raimondi,et al. Molecules. 2019 Mar; 24(6): 1140.
2.Gangjee A,et al. Curr Pharm Des. 2007;13(6):609-39.
Cell Cycle/DNA Damage
ABC(12)
AChR(104)
Antifolate(12)
ATM/ATR(26)
Aurora Kinase(51)
CLK(15)
c-Myc(22)
DHFR(16)
DNA Alkylator(34)
DNA gyrase(11)
DNA Repair Protein(21)
DNA/RNA Synthesis(187)
DNA-PK(15)
GPR(97)
HDAC(152)
Hec1/Nek2(9)
Integrin(77)
LIM Kinase (LIMK)(7)
Mps1/TTK(2)
Nucleoside Antimetabolite/Analog(48)
Other Targets(4)
PAK(13)
PARP(67)
PLK(26)
Potassium Channel(146)
RAD51(1)
Rho(16)
ROCK(42)
Telomerase(12)
Topoisomerase(88)
Wee1(7)
DHFR
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P 218
产品货号 : M36513
cas no: 1142407-60-0
P 218 is a novel DHFR inhibitor with antimalarial activity and antifolate effects and can be used to study Buruli ulcer. -
Talotrexin ammonium
产品货号 : M35770
cas no: 648420-92-2
Talotrexin ammonium is a non-polyglutamic acid antifolate. Talotrexin ammonium inhibits tumor growth by targeting dihydrofolate reductase (DHFR), thereby improving anti-tumor activity in a wide range of cancer models, helping to inhibit tumor growth. -
DHFR-IN-4
产品货号 : M35563
cas no: 2820126-49-4
DHFR-IN-4 是一种有效的二氢叶酸还原酶 (DHFR) 抑制剂IC50 为 123 nM。DHFR-IN-4 对 EGFR 和 HER2 也具有抑制活性,IC50 分别为 246 nM 和 357 nM。DHFR-IN-4 对癌细胞具有显著的广谱细胞毒性活性。 -
DS44960156
产品货号 : M34971
cas no: 2361327-08-2
DS44960156 是选择性的亚甲基四氢叶酸脱氢酶 2 (MTHFD2) 的抑制剂,其对 MTHFD2 和 MTHFD1 的 IC50 值分别为 1.6 μM 和 >30 μM。 -
Methotrexate Diglutamate
产品货号 : M34112
cas no: 41600-13-9
Methotrexate Diglutamate Small molecule compound present in the liver that acts as a partially purified human dihydrofolate reductase inhibitor.