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62

抑制剂 & 化合物

3

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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。
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。
T29460 5-Methyldihydrofolate

5-Methyldihydrofolate is the primary biologically active form of folate used for DNA reproduction, the cysteine cycle, and the regulation of homocysteine.
T20340 10-Formyldihydrofolate

10-Formyldihydrofolate is a Methotrexate metabolite. It inhibits thymidylate synthetase and glycinamide ribotide transformylase.
T24962 10-Formylfolic acid

DHFR Cell Cycle/Checkpoint; DNA Damage/DNA Repair; Metabolism
10-Formylfolic acid 是一种新型有效的二氢叶酸还原酶 (dihydrofolate reductase) 抑制剂,可用于研究白血病。
T17257L WR99210 hydrochloride(47326-86-3 free base)

WR99210 hydrochloride(47326-86-3 free base),6,6-Dimethyl-1-[3-(2,4,5-trichlorophenoxy)propoxy]-1,6-dihydro-1,3,5-triazine-2,4-diamine

Others Others
WR99210 hydrochloride 是恶性疟原虫二氢叶酸还原酶 (pfDHFR) 的有效抑制剂,pfDHFR 是主要的疟疾药物靶点。它对野生型、双突变体和四突变体二氢叶酸还原酶具有亚纳摩尔效力。
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。
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。
TQ0113 Iclaprim

艾拉普林,AR-100

Antibacterial; Antibiotic Microbiology/Virology
Iclaprim (AR-100) 是一种细菌二氢叶酸的选择性新型抑制剂, 可抑制金黄色葡萄球菌的生长, 其 MIC90值为 0.06 μg/mL。
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。
T25886 Methotrexate Diglutamate

NSC-269401,NSC 269401,NSC269401

DHFR Cell Cycle/Checkpoint; DNA Damage/DNA Repair; Metabolism
Methotrexate Diglutamate 存在于肝脏中的小分子化合物,可作为部分纯化的人二氢叶酸还原酶抑制剂。
T24644 Piritrexim

BW 301U

DHFR Cell Cycle/Checkpoint; DNA Damage/DNA Repair; Metabolism
Piritrexim (BW 301U) 是一种可口服的脂溶性二氢叶酸还原酶抑制剂,具有肺毒性,用于研究尿路上皮癌和转移性乳腺癌。
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。
T20339 7-Hydroxymethotrexate

NSC 380963,NSC-380963,NSC380962,NSC380963,NSC 380962,NSC-380962

Drug Metabolite Metabolism
7-Hydroxymethotrexate 是 Methotrexate 主要的代谢产物。Methotrexate 对叶酸具有抑制作用,抑制二氢叶酸还原酶,从而防止叶酸转化为四氢叶酸,并抑制 DNA 合成。Methotrexate 对代谢也具有抑制作用。
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。
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。
T5420 Cycloguanil hydrochloride

Chloroguanide Triazine,环氯胍盐酸盐

Parasite; Drug Metabolite Metabolism; Microbiology/Virology
Cycloguanil hydrochloride (Chloroguanide Triazine) 是抗疟化合物氯胍的活性代谢物。 它作为二氢叶酸还原酶的抑制剂,对于疟原虫和人类形式的 Kis 值分别为 0.3 和 1.5 nM。
T4382 Proguanil hydrochloride

Paludrine hydrochloride,盐酸氯胍,Chlorguanide hydrochloride,Chloroquanil

Others; Dehydrogenase; DNA/RNA Synthesis; Antifolate; Parasite Cell Cycle/Checkpoint; DNA Damage/DNA Repair; Metabolism; Microbiology/Virology; Others
Proguanil hydrochloride (Chloroquanil) 是一种双胍类抗疟疾剂,在体内代谢形成环胍。它还是一种二氢叶酸还原酶抑制剂。
T30761 CB 3703

CB3703,NSC 289522,CB-3703

CB 3703 is an inhibitor of dihydrofolate reductase and thymidylate synthase.
T17164 Trimetrexate

三甲曲沙,CI-898

Others Others
Trimetrexate is an effective competitive inhibitor of bacterial, protozoan, and mammalian dihydrofolate reductase.
T29003 TRC-19

TRC-19 is a potent and selective inhibitor of Toxoplasma gondii dihydrofolate reductase. TRC-19 shows an IC50 of 9 nM and 89-fold selectivity in favor of Toxoplasma gondii dihydrofolate reductase.
T24459 Metioprim

Ro126995,Ro 126995,He 909,He909,Ro 12-6995

Metioprim is a competitive bacterial dihydrofolate reductases inhibitor.
T24571 Ornithine-methotrexate

ADMPO

Ornithine-methotrexate is a ornithine analog of methotrexate. It is an inhibitors of dihydrofolate reductase.
T23883 Chlorasquin

Ccnsc-529,861,Ccnsc 529,861,SK 29861,Ccnsc529,861,SK-29861

Chlorasquin is a dihydrofolate reductase inhibitor.
T25079 Aminopterin N-hydroxysuccinimide ester

Nhs-aminopterin,N-Hydroxysuccinimide aminopterin

Aminopterin N-hydroxysuccinimide ester is an antineoplastic agent with immunosuppressive properties. Aminopterin works as an enzyme inhibitor by competing for the folate binding site of the enzyme dihydrofolate reductase. Its binding affinity for dihydrof
T24427 Lysine-methotrexate

ADMPL

Lysine-methotrexate is an anticancer drug. It is an inhibitor of dihydrofolate reductase.
T7730L Aminopterin sodium

NSC739,NSC 739 [as the base],NSC-739

Aminopterin sodium is an antineoplastic agent with immunosuppressive properties. Aminopterin works as an enzyme inhibitor by competing for the folate binding site of the enzyme dihydrofolate reductase. Its binding affinity for dihydrofolate reductase effe
T25381 Epiroprim

Epiroprime,Ro11-8958,Ro 11-8958,Ro-11-8958

Epiroprim is an analog of trimethoprim and a dihydrofolate reductase inhibitor.
T10916 Cycloguanil D6

Chlorguanide triazine D6

Others Others
Cycloguanil D6 is a dihydrofolate reductase inhibitor, deuterium-labeled Cycloguanil.
T25332 Dihydrohomofolic acid

Dihydrohomofolic acid is a substrate for dihydrofolate reductase that produces tetrahydro-homo folate which in turn suppresses thymidylate synthetase and then DNA synthesis.
T70080 Methasquin

Methasquin is a folic acid antagonist that has been used in the treatment of experimental leukemia; acts by inhibiting the dihydrofolate reductase in the cell.
T27002 CH-1504

CH 1504,MobileTrex

CH-1504, dihydrofolate reductase (DHFR) inhibitor, is used potentially for the treatment of rheumatoid arthritis.
T25324 Dichloromethotrexate

NSC 29630,3988-B-129-4,NSC29630,Dichloroamethopterin,NSC-29630

Dichloromethotrexate is an enzyme dihydrofolate reductase inhibitor, thus preventing the synthesis of purine nucleotides and thymidylates and inhibiting DNA and RNA synthesis. This agent is metabolized and excreted by the liver.
T69591 Cycloguanil nitrate

Cycloguanil nitrate is a dihydrofolate reductase inhibitor and is a metabolite of the antimalarial drug proguanil.
T10915 Cycloguanil D6 Nitrate

Chlorguanide triazine D6 Nitrate

Others Others
Cycloguanil D6 Nitrate is a dihydrofolate reductase inhibitor, deuterium-labeled Cycloguanil.
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
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.
T22409 Proguanil

氯胍,chloroguanide,chlorguanide

Others Others
Proguanil, a prophylactic antimalarial drug, inhibits the dihydrofolate reductase of plasmodia and thereby blocks the biosynthesis of pyrimidines and purines, which are essential for DNA synthesis and cell multiplication.
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
T39862 Trimethoprim lactate

Trimethoprim lactic is a bacteriostatic antibiotic and an orally active dihydrofolate reductase inhibitor. Trimethoprim lactic is active against a wide range of Gram-positive and Gram-negative aerobic bacteria . Trimethoprim lactic has the potential for urinary tract infections, Shigellosis and Pneumocystis pneumonia treatment.
T12742 Ro 20-0657/000

Others Others
Ro 20-0657/000 is a Trimethoprim metabolite. Trimethoprim is an inhibitor of dihydrofolate reductase, used as an antibacterial agent in human and veterinary medicine.
T25374 Emofolin sodium

NSC139490,MeTHHF disodium,NSC-139490,NSC 139490

Emofolin sodium is the sodium salt of a synthetic antimetabolite analogue of folate with antineoplastic activity,which competes for the folate binding site of the enzyme dihydrofolate reductase, resulting in inhibition of tetrahydrofolate synthesis, deple
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。
T63985 Trimetrexate glucuronate

Trimetrexate glucuronate (NSC 352122) 是一种叶酸拮抗剂,能够抑制二氢叶酸还原酶 (dihydrofolate reductase),进而阻断嘌呤核苷酸和胸苷酸的合成,影响 DNA 和 RNA 合成,表现出潜在的抗肿瘤效果。
T69089 Trimethoprim sulfate

Trimethoprim sulfate is a pyrimidine inhibitor of dihydrofolate reductase, it is an antibacterial related to PYRIMETHAMINE. The interference with folic acid metabolism may cause a depression of hematopoiesis. It is potentiated by SULFONAMIDES and the TRIMETHOPRIM-SULFAMETHOXAZOLE COMBINATION is the form most often used. It is sometimes used alone as an antimalarial. TRIMETHOPRIM RESISTANCE has been reported.
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。
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。
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).
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]。
T75259 Baquiloprim

Baquiloprim为一种抗生素,作为细菌二氢叶酸还原酶的选择性抑制剂,对革兰氏阴性及革兰氏阳性细菌展现体外抑菌活性。

化合物

DHFR-IN-3
Cat.No: T3693
Synonym: 7-bromoquinazoline-2,4-diamine,7-溴-2,4-二氨基喹唑啉
Target: Others
Pralatrexate
Cat.No: T6120
Synonym: Folotyn,10-炔丙基-10-去氮杂氨基蝶呤,10-Propargyl-10-deazaaminopterin,普拉曲沙
Target: Apoptosis, DHFR, Antifolate, TAM Receptor
5-Methyldihydrofolate
Cat.No: T29460
Synonym:
Target:
10-Formyldihydrofolate
Cat.No: T20340
Synonym:
Target:
10-Formylfolic acid
Cat.No: T24962
Synonym:
Target: DHFR
WR99210 hydrochloride(47326-86-3 free base)
Cat.No: T17257L
Synonym: WR99210 hydrochloride(47326-86-3 free base),6,6-Dimethyl-1-[3-(2,4,5-trichlorophenoxy)propoxy]-1,6-dihydro-1,3,5-triazine-2,4-diamine
Target: Others
Brodimoprim
Cat.No: T19858
Synonym:
Target: DHFR, Antibacterial
Pyrimethamine
Cat.No: T0849
Synonym: Pirimecidan,RP 4753,Pirimetamin,乙胺嘧啶
Target: DHFR, Antifolate, Parasite
Iclaprim
Cat.No: TQ0113
Synonym: 艾拉普林,AR-100
Target: Antibacterial, Antibiotic
DHFR-IN-4
Cat.No: T61486
Synonym:
Target: DHFR
Methotrexate Diglutamate
Cat.No: T25886
Synonym: NSC-269401,NSC 269401,NSC269401
Target: DHFR
Piritrexim
Cat.No: T24644
Synonym: BW 301U
Target: DHFR
Methotrexate
Cat.No: T1485
Synonym: NCI-C04671,WR19039,Amethopterin,甲氨蝶呤,CL14377
Target: Apoptosis, Dehydrogenase, DNA/RNA Synthesis, Antifolate
7-Hydroxymethotrexate
Cat.No: T20339
Synonym: NSC 380963,NSC-380963,NSC380962,NSC380963,NSC 380962,NSC-380962
Target: Drug Metabolite
Fanotaprim
Cat.No: T36692
Synonym:
Target: DHFR
Talotrexin ammonium
Cat.No: T64295
Synonym:
Target: DHFR
Cycloguanil hydrochloride
Cat.No: T5420
Synonym: Chloroguanide Triazine,环氯胍盐酸盐
Target: Parasite, Drug Metabolite
Proguanil hydrochloride
Cat.No: T4382
Synonym: Paludrine hydrochloride,盐酸氯胍,Chlorguanide hydrochloride,Chloroquanil
Target: Others, Dehydrogenase, DNA/RNA Synthesis, Antifolate, Parasite
CB 3703
Cat.No: T30761
Synonym: CB3703,NSC 289522,CB-3703
Target:
Trimetrexate
Cat.No: T17164
Synonym: 三甲曲沙,CI-898
Target: Others
TRC-19
Cat.No: T29003
Synonym:
Target:
Metioprim
Cat.No: T24459
Synonym: Ro126995,Ro 126995,He 909,He909,Ro 12-6995
Target:
Ornithine-methotrexate
Cat.No: T24571
Synonym: ADMPO
Target:
Chlorasquin
Cat.No: T23883
Synonym: Ccnsc-529,861,Ccnsc 529,861,SK 29861,Ccnsc529,861,SK-29861
Target:
Aminopterin N-hydroxysuccinimide ester
Cat.No: T25079
Synonym: Nhs-aminopterin,N-Hydroxysuccinimide aminopterin
Target:
Lysine-methotrexate
Cat.No: T24427
Synonym: ADMPL
Target:
Aminopterin sodium
Cat.No: T7730L
Synonym: NSC739,NSC 739 [as the base],NSC-739
Target:
Epiroprim
Cat.No: T25381
Synonym: Epiroprime,Ro11-8958,Ro 11-8958,Ro-11-8958
Target:
Cycloguanil D6
Cat.No: T10916
Synonym: Chlorguanide triazine D6
Target: Others
Dihydrohomofolic acid
Cat.No: T25332
Synonym:
Target:
Methasquin
Cat.No: T70080
Synonym:
Target:
CH-1504
Cat.No: T27002
Synonym: CH 1504,MobileTrex
Target:
Dichloromethotrexate
Cat.No: T25324
Synonym: NSC 29630,3988-B-129-4,NSC29630,Dichloroamethopterin,NSC-29630
Target:
Cycloguanil nitrate
Cat.No: T69591
Synonym:
Target:
Cycloguanil D6 Nitrate
Cat.No: T10915
Synonym: Chlorguanide triazine D6 Nitrate
Target: Others
Pralatrexate, (R)-
Cat.No: T25980
Synonym:
Target:
Piritrexim isethionate
Cat.No: T68684
Synonym:
Target:
Proguanil
Cat.No: T22409
Synonym: 氯胍,chloroguanide,chlorguanide
Target: Others
Pralatrexate, (S)-
Cat.No: T25981
Synonym:
Target:
Trimethoprim lactate
Cat.No: T39862
Synonym:
Target:
Ro 20-0657/000
Cat.No: T12742
Synonym:
Target: Others
Emofolin sodium
Cat.No: T25374
Synonym: NSC139490,MeTHHF disodium,NSC-139490,NSC 139490
Target:
NSC309401 dihydrochloride
Cat.No: T81639
Synonym:
Target:
Trimetrexate glucuronate
Cat.No: T63985
Synonym:
Target:
Trimethoprim sulfate
Cat.No: T69089
Synonym:
Target:
NSC309401
Cat.No: T79912
Synonym:
Target:
DHFR-IN-10
Cat.No: T82571
Synonym:
Target:
Phototrexate
Cat.No: T41148
Synonym:
Target:
DHFR-IN-5
Cat.No: T73328
Synonym:
Target:
Baquiloprim
Cat.No: T75259
Synonym:
Target:
Cat. No. Product Name Target Signaling Pathways
T15128 Dihydrofolic acid

7,8-Dihydrofolic acid,Dihydrofolate

Others Others
Dihydrofolic acid (7,8-Dihydrofolic acid) 是一种叶酸衍生物,在二氢叶酸还原酶的作用下生成四氢叶酸。
T1153 Trimethoprim

NIH 204,BW 56-72,甲氧苄啶,NSC-106568

DHFR; DNA/RNA Synthesis; Antifolate; Antibacterial; Antibiotic Cell Cycle/Checkpoint; DNA Damage/DNA Repair; Metabolism; Microbiology/Virology
Trimethoprim (NSC-106568) 是抑菌抗生素,也是具有口服活性的二氢叶酸还原酶抑制剂。它对多种革兰氏阳性和革兰氏阴性需氧细菌具有活性,可用于尿路感染,肺孢子菌肺炎和志贺氏菌病的研究。
T7730 Aminopterin

APGA,氨基蝶呤,4-Aminofolic acid

Antifolate Cell Cycle/Checkpoint
Aminopterin (4-Aminofolic acid) 是叶酸的 4-氨基衍生物,是叶酸拮抗剂,具有抗癌和免疫抑制活性,用于研究儿童白血病。它催化叶酸还原为四氢叶酸,竞争性抑制二氢叶酸还原酶,Ki 值为 3.7 pM。

天然产物

Dihydrofolic acid
Cat.No: T15128
Synonym: 7,8-Dihydrofolic acid,Dihydrofolate
Target: Others
Trimethoprim
Cat.No: T1153
Synonym: NIH 204,BW 56-72,甲氧苄啶,NSC-106568
Target: DHFR, DNA/RNA Synthesis, Antifolate, Antibacterial, Antibiotic
Aminopterin
Cat.No: T7730
Synonym: APGA,氨基蝶呤,4-Aminofolic acid
Target: Antifolate
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