1. Cell Cycle/DNA Damage
  2. Antifolate

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 (19):

Cat. No. Product Name Effect Purity
  • HY-14519
    Methotrexate Antagonist 99.75%
    Methotrexate 是一种传统叶酸拮抗剂,在使用磺酰罗丹明 B 测定的六个小儿白血病和淋巴瘤细胞系中,平均 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),Ki 分别为 1.3 nM,7.2 nM 和 65 nM。
  • HY-14781
    Levomefolic acid Agonist >98.0%
    Levomefolic acid (5-MTHF)是天然的叶酸活性形式。
  • HY-10446
    Pralatrexate Inhibitor 98.99%
    Pralatrexate(Folotyn)是叶酸类似物,对一些细胞株的 IC50< 300 nM。
  • HY-18062
    Pyrimethamine Antagonist 99.90%
    Pyrimethamine(RP4753)可通过抑制二氢叶酸还原酶(DHFR)干扰四氢叶酸的合成,可作用于原生动物的感染。
  • 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-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。
  • HY-B0510
    Trimethoprim Inhibitor 99.98%
    Trimethoprim是抗菌素,可作用于泌尿系统感染。
  • HY-13664
    Folinic acid Calcium Agonist 99.52%
    Leucovorin钙盐是还原的叶酸。
  • HY-13667
    Levoleucovorin Calcium Agonist
    Levoleucovorin钙盐是folinic acid的活性形式。
  • 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-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-12784S
    Cycloguanil D6 Antagonist >98.0%
    Cycloguanil D6是Cycloguanil的氘代化合物标准品。
  • 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-17556
    Folinic acid Agonist
    Folinic acid是肿瘤化疗药methotrexate等的佐剂。
  • HY-17383
    Levomefolate calcium Agonist
    Levomefolate是叶酸的人造形式,抗叶酸的作用。
  • 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-B1902
    Diaveridine Inhibitor 98.48%
    Diaveridine 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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