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    1. Cell Cycle/DNA Damage
    2. 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 (20):

    Cat. No. Product Name Effect Purity
    • HY-14519
      Methotrexate Antagonist 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 99.52%
    • HY-14781
      Levomefolic acid Agonist >98.0%
      Levomefolic acid (5-MTHF)是天然的叶酸活性形式。
    • HY-B0510
      Trimethoprim Inhibitor 99.98%
    • 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-10446
      Pralatrexate Inhibitor 99.23%
      Pralatrexate(Folotyn)是叶酸类似物,对一些细胞株的 IC50< 300 nM。
    • 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-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钙盐是folinic acid的活性形式。
    • HY-B0080
      Folinic acid calcium salt pentahydrate Antagonist 99.73%
      Folinic Acid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
    • 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-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。
    • HY-10818
      LY309887 Inhibitor
      LY309887 是一种有效的二氢叶酸还原酶 (GARFT) 抑制剂,Ki 值为 6.5 nM,具有抗肿瘤活性。
    Isoform Specific Products

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