DHFR
シグナル伝達経路
研究分野
阻害剤の選択性比較
| カタログ番号 | 製品カタログ | 溶解度(25°C) | ||
|---|---|---|---|---|
| 水 | DMSO | アルコール | ||
| S1135 | Pemetrexed (LY-231514) disodium | 94 mg/mL | <1 mg/mL | ''''<1 mg/mL |
| S1210 | Methotrexate (CL-14377) | <1 mg/mL | 90 mg/mL | ''<1 mg/mL |
| S1497 | Pralatrexate (NSC 754230) | <1 mg/mL | 28 mg/mL | '<1 mg/mL |
| S2006 | Pyrimethamine | <1 mg/mL | 10 mg/mL | <1 mg/mL |
| S5971 | Pemetrexed | <1 mg/mL | 85 mg/mL | ''<1 mg/mL |
| S2588 | Calcium Levofolinate | 9 mg/mL | <1 mg/mL | ''''<1 mg/mL |
| S3129 | Trimethoprim | <1 mg/mL | 58 mg/mL | ''<1 mg/mL |
| S5097 | Methotrexate disodium | 99 mg/mL | <1 mg/mL | -1 mg/mL |
| S7785 | Pemetrexed Disodium Hydrate | 100 mg/mL | <1 mg/mL | <1 mg/mL |
| S5927 | Proguanil | <1 mg/mL | 51 mg/mL | '51 mg/mL |
| S5200 | Diaveridine | -1 mg/mL | 25 mg/mL | -1 mg/mL |
| S5136 | Calcium folinate | 100 mg/mL | <1 mg/mL | -1 mg/mL |
| S0320 | Cycloguanil hydrochloride | ' mg/mL | ||
| S1236 | Leucovorin (NSC -3590) Calcium Pentahydrate | 13 mg/mL | <1 mg/mL | ''<1 mg/mL |
| S0854 | Metoprine | ' mg/mL | ||
DHFR製品
| 製品コード | 製品説明 | 文献中Selleckの製品使用例 | お客様のフィードバック |
|---|---|---|---|
| S1135 |
Pemetrexed (LY-231514) disodiumPemetrexed (LY-231514) disodium is a novel antifolate and antimetabolite for TS, DHFR and GARFT with Ki of 1.3 nM, 7.2 nM and 65 nM in cell-free assays, respectively. Pemetrexed induces autophagy and apoptosis. |
Role of PARP and BER in the synergy between PTX and GMX in A549 cells. Cells were pretreated ±1 umol/L olaparib (2 hours) then sequentially ±150 nmol/L PTX (24 hours), then ± GMX 12 nmol/L (48 hours). PAR modification of proteins and γ-H2AX levels were measured in extracts treated as in A by Western blotting.
|
|
| S1210 |
Methotrexate (CL-14377)Methotrexate (CL14377, MTX, NCI-C04671, Amethopterin, WR19039), analog of folic acid, is a nonspecific inhibitor of the dihydrofolate reductase(DHFR) of bacteria and cancerous cells as well as normal cells. It forms an inactive ternary complex with DHFR and NADPH. Methotrexate (MTX) induces apoptosis. |
Toxicity of MTX (3) and toxic analogues 5 a-e on a) hY1R-expressing MDA-MB-468 and b) non-hYR-expressing HEK293 cells. Cell viability was determined by resazurin assay. Bars represent the mean±SEM of at least three independent experiments performed in triplicate. Measurements were normalized by using only HBSS, pH 7, treated cells (set at 100 %) and ethanol-treated cells (set at 0 %). Statistical significances refer to only HBSS, pH 7, treated cells indicated as a dashed line. |
|
| S1497 |
Pralatrexate (NSC 754230)Pralatrexate (NSC 754230) is an antifolate, and structurally a folate analog. Its IC50 is < 300 nM in some cell lines. Pralatrexate induces tumor cell apoptosis. |
PK parameters for pralatrexate in the study population. Concentration over time for each dose cohort of pralatrexate (A).
|
|
| S2006 |
PyrimethaminePyrimethamine is a dihydrofolate reductase (DHFR) inhibitor, used as an antimalarial drug. |
||
| S5971新 |
PemetrexedPemetrexed (LY231514, Alimta) is a novel antifolate and antimetabolite for thymidylate synthase (TS), dihydrofolate reductase (DHFR) and glycinamide ribonucleotide formyltransferase (GARFT) with Ki of 1.3 nM, 7.2 nM and 65 nM in cell-free assays, respectively. Pemetrexed induces autophagy and apoptosis. |
||
| S2588新 |
Calcium LevofolinateCalcium Levofolinate (Calcium Folinate, Levoleucovorin calcium, CL307782) is a calcium salt of folinic acid that is an adjuvant used in cancer chemotherapy. |
||
| S3129 |
TrimethoprimTrimethoprim (BW 56-72, NIH 204, NSC-106568) is a bacteriostatic antibiotic mainly used in the prophylaxis and treatment of urinary tract infections. |
||
| S5097 |
Methotrexate disodiumMethotrexate sodium, an inhibitor of tetrahydrofolate dehydrogenase, is an antineoplastic antimetabolite with immunosuppressant properties. |
||
| S7785 |
Pemetrexed Disodium HydratePemetrexed Disodium Hydrate (LY-231514) is a novel antifolate and antimetabolite for TS, DHFR and GARFT with Ki of 1.3 nM, 7.2 nM and 65 nM, respectively. Pemetrexed Disodium Hydrate stimulates autophagy and apoptosis. |
Role of PARP and BER in the synergy between PTX and GMX in A549 cells. Cells were pretreated ±1 umol/L olaparib (2 hours) then sequentially ±150 nmol/L PTX (24 hours), then ± GMX 12 nmol/L (48 hours). PAR modification of proteins and γ-H2AX levels were measured in extracts treated as in A by Western blotting.
|
|
| S5927 |
ProguanilProguanil (chlorguanide, chloroguanide) is a prophylactic antimalarial drug. It inhibits the dihydrofolate reductase of plasmodia and thereby blocks the biosynthesis of purines and pyrimidines, which are essential for DNA synthesis and cell multiplication. |
||
| S5200 |
DiaveridineDiaveridine (AI3-23935, CCRIS-3784) is coccidiostat with anti-parasitic activity and also a dihydrofolate reductase (DHFR) inhibitor preventing folic acid synthesis in species of Pneumocystis. |
||
| S5136 |
Calcium folinateCalcium folinate (Leucovorin calcium, Folinic acid calcium salt, Wellcovorin) is a metabolically active, reduced form of folic acid that is rapidly absorbed and extensively metabolized in the liver to other folic acid derivatives. |
||
| S0320 |
Cycloguanil hydrochlorideCycloguanil hydrochloride is an active metabolite of Proguanil. Cycloguanil hydrochloride acts on malaria schizonts in erythrocytes and hepatocytes. |
||
| S1236 |
Leucovorin (NSC -3590) Calcium PentahydrateLeucovorin Calcium Pentahydrate (NSC -3590, Folinic acid) is a derivative of folic acid, which can be used to increase levels of folic acid under conditions favoring folic acid inhibition. |
||
| S0854新 |
MetoprineMetoprine (BW 197U), a diaminopyrimidine derivative, is a potent inhibitor of histamine N-methyltransferase (HMT) that crosses the blood-brain barrier and increases brain histamine levels. Metoprine is an antifolate and antitumor agent. |
| 製品コード | 製品説明 | 文献中Selleckの製品使用例 | お客様のフィードバック |
|---|---|---|---|
| S1135 |
Pemetrexed (LY-231514) disodiumPemetrexed (LY-231514) disodium is a novel antifolate and antimetabolite for TS, DHFR and GARFT with Ki of 1.3 nM, 7.2 nM and 65 nM in cell-free assays, respectively. Pemetrexed induces autophagy and apoptosis. |
Role of PARP and BER in the synergy between PTX and GMX in A549 cells. Cells were pretreated ±1 umol/L olaparib (2 hours) then sequentially ±150 nmol/L PTX (24 hours), then ± GMX 12 nmol/L (48 hours). PAR modification of proteins and γ-H2AX levels were measured in extracts treated as in A by Western blotting.
|
|
| S1210 |
Methotrexate (CL-14377)Methotrexate (CL14377, MTX, NCI-C04671, Amethopterin, WR19039), analog of folic acid, is a nonspecific inhibitor of the dihydrofolate reductase(DHFR) of bacteria and cancerous cells as well as normal cells. It forms an inactive ternary complex with DHFR and NADPH. Methotrexate (MTX) induces apoptosis. |
Toxicity of MTX (3) and toxic analogues 5 a-e on a) hY1R-expressing MDA-MB-468 and b) non-hYR-expressing HEK293 cells. Cell viability was determined by resazurin assay. Bars represent the mean±SEM of at least three independent experiments performed in triplicate. Measurements were normalized by using only HBSS, pH 7, treated cells (set at 100 %) and ethanol-treated cells (set at 0 %). Statistical significances refer to only HBSS, pH 7, treated cells indicated as a dashed line. |
|
| S1497 |
Pralatrexate (NSC 754230)Pralatrexate (NSC 754230) is an antifolate, and structurally a folate analog. Its IC50 is < 300 nM in some cell lines. Pralatrexate induces tumor cell apoptosis. |
PK parameters for pralatrexate in the study population. Concentration over time for each dose cohort of pralatrexate (A).
|
|
| S2006 |
PyrimethaminePyrimethamine is a dihydrofolate reductase (DHFR) inhibitor, used as an antimalarial drug. |
||
| S5971新 |
PemetrexedPemetrexed (LY231514, Alimta) is a novel antifolate and antimetabolite for thymidylate synthase (TS), dihydrofolate reductase (DHFR) and glycinamide ribonucleotide formyltransferase (GARFT) with Ki of 1.3 nM, 7.2 nM and 65 nM in cell-free assays, respectively. Pemetrexed induces autophagy and apoptosis. |
||
| S2588新 |
Calcium LevofolinateCalcium Levofolinate (Calcium Folinate, Levoleucovorin calcium, CL307782) is a calcium salt of folinic acid that is an adjuvant used in cancer chemotherapy. |
||
| S3129 |
TrimethoprimTrimethoprim (BW 56-72, NIH 204, NSC-106568) is a bacteriostatic antibiotic mainly used in the prophylaxis and treatment of urinary tract infections. |
||
| S5097 |
Methotrexate disodiumMethotrexate sodium, an inhibitor of tetrahydrofolate dehydrogenase, is an antineoplastic antimetabolite with immunosuppressant properties. |
||
| S7785 |
Pemetrexed Disodium HydratePemetrexed Disodium Hydrate (LY-231514) is a novel antifolate and antimetabolite for TS, DHFR and GARFT with Ki of 1.3 nM, 7.2 nM and 65 nM, respectively. Pemetrexed Disodium Hydrate stimulates autophagy and apoptosis. |
Role of PARP and BER in the synergy between PTX and GMX in A549 cells. Cells were pretreated ±1 umol/L olaparib (2 hours) then sequentially ±150 nmol/L PTX (24 hours), then ± GMX 12 nmol/L (48 hours). PAR modification of proteins and γ-H2AX levels were measured in extracts treated as in A by Western blotting.
|
|
| S5927 |
ProguanilProguanil (chlorguanide, chloroguanide) is a prophylactic antimalarial drug. It inhibits the dihydrofolate reductase of plasmodia and thereby blocks the biosynthesis of purines and pyrimidines, which are essential for DNA synthesis and cell multiplication. |
||
| S5200 |
DiaveridineDiaveridine (AI3-23935, CCRIS-3784) is coccidiostat with anti-parasitic activity and also a dihydrofolate reductase (DHFR) inhibitor preventing folic acid synthesis in species of Pneumocystis. |
||
| S5136 |
Calcium folinateCalcium folinate (Leucovorin calcium, Folinic acid calcium salt, Wellcovorin) is a metabolically active, reduced form of folic acid that is rapidly absorbed and extensively metabolized in the liver to other folic acid derivatives. |
| 製品コード | 製品説明 | 文献中Selleckの製品使用例 | お客様のフィードバック |
|---|---|---|---|
| S0320 |
Cycloguanil hydrochlorideCycloguanil hydrochloride is an active metabolite of Proguanil. Cycloguanil hydrochloride acts on malaria schizonts in erythrocytes and hepatocytes. |
| 製品コード | 製品説明 | 文献中Selleckの製品使用例 | お客様のフィードバック |
|---|---|---|---|
| S1236 |
Leucovorin (NSC -3590) Calcium PentahydrateLeucovorin Calcium Pentahydrate (NSC -3590, Folinic acid) is a derivative of folic acid, which can be used to increase levels of folic acid under conditions favoring folic acid inhibition. |
2021, e13031 2020, 9(9)E2110 2020, 40(7):3659-3667 |
|
| S0854新 |
MetoprineMetoprine (BW 197U), a diaminopyrimidine derivative, is a potent inhibitor of histamine N-methyltransferase (HMT) that crosses the blood-brain barrier and increases brain histamine levels. Metoprine is an antifolate and antitumor agent. |
