1. Signaling Pathways
  2. Cell Cycle/DNA Damage
  3. Antifolate


Antifolates are compounds that antagonise the actions of folic acid (vitamin B9). Folic acid's primary function in the body is as a cofactor to various methyltransferases involved in serine, methionine, thymidine and purine biosynthesis. Consequently antifolates inhibit cell division, DNA/RNA synthesis and repair and protein synthesis. Some such as Proguanil, Pyrimethamine and Trimethoprim selectively inhibit folate's actions in microbial organisms such as bacteria, protozoa and fungi. The majority of antifolates work by inhibiting dihydrofolate reductase (DHFR). Many are primarily DHFR inhibitors, but Raltitrexed is an inhibitor of thymidylate synthase, and Pemetrexed inhibits both and a third enzyme. Antifolates act specifically during DNA and RNA synthesis, and thus are cytotoxic during the S-phase of the cell cycle. Thus, they have a greater toxic effect on rapidly dividing cells.

Antifolate 相关产品 (21):

Cat. No. Product Name Effect Purity
  • HY-14519
    Methotrexate 99.75%
    Methotrexate是一种叶酸拮抗剂,在体外试验中 IC50 为 78 nM。
  • HY-10820A
    Pemetrexed disodium Inhibitor 99.77%
    Pemetrexed disodium是一种叶酸拮抗剂 (antifolate)。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)的Ki 分别为 1.3 nM,7.2 nM 和 65 nM。
  • HY-13664
    Folinic acid Calcium Agonist 99.73%
  • HY-10820
    Pemetrexed Inhibitor 99.30%
    Pemetrexed 是一种叶酸拮抗剂 (antifolate)。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。
  • HY-B0510
    Trimethoprim Inhibitor 99.98%
  • HY-107981
    LSN 3213128 Inhibitor
    LSN 3213128 是一种选择性、非经典、口服有效的抗叶酸剂,能够有效特异性抑制氨基咪唑-4-甲酰胺核糖核苷酸甲酰转移酶 (AICARFT) 的活性,IC50 值为 16 nM,在细胞中对其 IC50 值为 19 nM。
  • HY-108251
    Methotrexate metabolite
    Methotrexate metabolite (DAMPA),是 Methotrexate 的活性代谢产物。 Methotrexate 是一种叶酸 (folic acid) 拮抗剂,广泛用作免疫抑制剂和化学治疗剂。
  • HY-10446
    Pralatrexate Inhibitor 99.23%
    Pralatrexate(Folotyn)是叶酸类似物,对一些细胞株的 IC50< 300 nM。
  • HY-18062
    Pyrimethamine Antagonist 99.90%
  • HY-13781
    Pemetrexed disodium hemipenta hydrate Inhibitor 99.78%
    Pemetrexed disodium hemipenta hydrate 是一种叶酸拮抗剂 (antifolate)。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。
  • HY-13667
    Levoleucovorin Calcium Agonist
    Levoleucovorin Calcium 是folinic acid的活性形式。
  • HY-B0080
    Folinic acid calcium salt pentahydrate Antagonist 99.73%
    Folinic acid (calcium salt pentahydrate) 是还原的叶酸,可与其它化疗药结合使用。
  • HY-12784S
    Cycloguanil D6 Antagonist >98.0%
    Cycloguanil D6是Cycloguanil的氘代化合物标准品。
  • HY-17383
    Levomefolate calcium Agonist
    Levomefolate calcium 是叶酸的人造形式,抗叶酸的作用。
  • HY-17556
    Folinic acid Agonist
    Folinic acid是肿瘤化疗药methotrexate等的佐剂。
  • HY-12784S1
    Cycloguanil D6 Nitrate Antagonist
    Cycloguanil D6硝酸盐是Cycloguanil的氘代化合物标准品。
  • HY-17557
    Calcium N5-methyltetrahydrofolate Agonist
    Calcium N5-methyltetrahydrofolate(NSC173328)是levomefolic acid的钙盐,可作用于心血管疾病和乳腺癌、结直肠癌。
  • HY-114306
    EC0489 Modulator
    EC0489是叶酸和去乙酰长春碱酰肼的偶联物,是叶酸受体 (FR)的高亲和力配体。 有望治疗难治性或转移性肿瘤。 是一种小分子-药物偶联物 (SMDC)。
  • HY-14523
    LY 254155 Inhibitor
    LY 254155 是一种抗叶酸剂。LY 254155 抑制 hGARFT 及与 mFBP 结合,Kis 分别为 2.1±0.2 和 1.7±0.1 nM。
  • HY-B1902
    Diaveridine Inhibitor 98.48%
    Diaveridine (EGIS-5645) 是二氢叶酸还原酶 (DHFR) 的抑制剂,对于野生型 DHFR 的 Ki 值为 11.5 nM,Diaveridine 也是一种抗菌剂。
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