Formycin B
Formycin B is an orally active PNP and PARP inhibitor. Formycin B inhibits influenza A virus proliferation and the replication of intracellular Trypanosoma cruzi, Leishmania, and pathogenic trypanosomes by competitively inhibiting PNP (Ki = 68-100 μM) and PARP (quail Ki = 68.9-75.0 μM), and by inhibiting DNA, RNA, and protein synthesis and cell proliferation. Formycin B can be used for research on influenza, PNP deficiency, leukemia, Chagas disease, leishmaniasis, and trypanosomiasis.
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- CAS 番号: 13877-76-4
- 分子式: C10H12N4O5
- 分子量:268.23
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
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生物活性
製品説明
Formycin B is an orally active PNP and PARP inhibitor. Formycin B inhibits influenza A virus proliferation and the replication of intracellular Trypanosoma cruzi, Leishmania, and pathogenic trypanosomes by competitively inhibiting PNP (Ki = 68-100 μM) and PARP (quail Ki = 68.9-75.0 μM), and by inhibiting DNA, RNA, and protein synthesis and cell proliferation. Formycin B can be used for research on influenza, PNP deficiency, leukemia, Chagas disease, leishmaniasis, and trypanosomiasis[1][2][3][4][5][6][7][8].
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PNP 68 μM (Ki, extracts of human T lymphocytes) |
PNP 100 μM (Ki, extracts from dialyzed cells) |
PARP 68.9 μM (Ki, chromatin-bound) |
PARP 75.0 μM (Ki, soluble) |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| L5178Y | ED50 |
16.0 μM
|
Antiproliferative activity against mouse L5178Y leukemia cells assessed as cell proliferation inhibition after 72 hrs incubation by cell concentration and doubling count.
Antiproliferative activity against mouse L5178Y leukemia cells assessed as cell proliferation inhibition after 72 hrs incubation by cell concentration and doubling count.
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172231 |
| L5178Y | ED50 |
31 μM
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Antiproliferative activity against mouse L5178Y leukemia cells assessed as cell proliferation inhibition after 24 hrs incubation by cell concentration and doubling count.
Antiproliferative activity against mouse L5178Y leukemia cells assessed as cell proliferation inhibition after 24 hrs incubation by cell concentration and doubling count.
|
172231 |
| L5178Y | ED50 |
21.6 μM
|
Antiproliferative activity against mouse L5178Y leukemia cells assessed as cell proliferation inhibition after 72 hrs incubation in the presence of 0.75 μM NAD+ by cell concentration and doubling count.
Antiproliferative activity against mouse L5178Y leukemia cells assessed as cell proliferation inhibition after 72 hrs incubation in the presence of 0.75 μM NAD+ by cell concentration and doubling count.
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172231 |
| L5178Y | ED50 |
23.8 μM
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Antiproliferative activity against mouse L5178Y leukemia cells assessed as cell proliferation inhibition after 72 hrs incubation in the presence of 1.51 μM NAD+ by cell concentration and doubling count.
Antiproliferative activity against mouse L5178Y leukemia cells assessed as cell proliferation inhibition after 72 hrs incubation in the presence of 1.51 μM NAD+ by cell concentration and doubling count.
|
172231 |
| L5178Y | ED50 |
33.1 μM
|
Antiproliferative activity against mouse L5178Y leukemia cells assessed as cell proliferation inhibition after 72 hrs incubation in the presence of 4.52 μM NAD+ by cell concentration and doubling count.
Antiproliferative activity against mouse L5178Y leukemia cells assessed as cell proliferation inhibition after 72 hrs incubation in the presence of 4.52 μM NAD+ by cell concentration and doubling count.
|
172231 |
体外実験
Anti-cancerNucleotide MetabolismProtein/Amino Acid MetabolismParasitic InfectionInnate ImmunityViral InfectionOthers
Anti-cancer
Formycin B (16.0-31 μM; 24-72 h) inhibits the proliferation of L5178Y mouse leukemia cells, with an ED50 value of 16.0 μM at 72 h and 31 μM at 24 h, exhibiting cytostatic effects at the ED50 and cytotoxic effects above 2× ED50[4].
Anti-cancer
Nucleotide Metabolism
Formycin B (7.2-36 μM; 24 h) inhibits macromolecule synthesis in L5178Y mouse leukemia cells, reducing [3H]thymidine, [3H]uridine, and [3H]phenylalanine incorporation to 40%, 51%, and 25% of control at 36 μM[4].
Anti-cancer
Nucleotide Metabolism
Protein/Amino Acid Metabolism
Formycin B (20-40 μM; 12 h) inhibits poly (ADP-Rib) synthesis in intact L5178Y mouse leukemia cells, reducing [14C]ribose incorporation into HCl extracts to 42% of control at 40 μM, and decreases histone H1 ADP-ribosylation[4].
Nucleotide Metabolism
Formycin B (0.03 mM-1.0 μM; 10 min) inhibits human purine nucleoside phosphorylase (PNP) in dialyzed cell extracts with a Ki of 100 μM[3].
Formycin B (40-200 μg/mL; 24 hr) does not significantly inhibit DNA or RNA synthesis and shows no obvious cytotoxicity in PRK cells[8].
Formycin B (40-200 μg/mL; 24 hr) does not significantly inhibit DNA or RNA synthesis and shows no obvious cytotoxicity in PRK cells[8].
Parasitic Infection
Formycin B (0.2-60 μg/mL) inhibits the replication of epimastigotes of T. cruzi Y strain in brain heart infusion medium only at 60 μg/mL[5].
Formycin B (0.1-10 μg/mL; 3-9 days) significantly inhibits the intracellular replication of T. cruzi Y strain amastigotes in normal mouse peritoneal macrophage monolayers at 0.1 μg/mL[5].
Formycin B (0.1-10 μg/mL; 48 h) reduces intracellular amastigotes of the T. cruzi Y strain in L929 cells by 91% at 1 and 10 μg/mL[5].
Formycin B (1-10 μg/mL; 2 h) pre-exposure slightly reduces subsequent intracellular replication of T. cruzi Y strain amastigotes in mouse peritoneal macrophages[5].
Formycin B (2.5 mM) is phosphorylated to formycin B monophosphate by cell-free extracts of L. mexicana or L. donovani promastigotes at a rate of 0.75 mmol/h/mg protein when p-nitrophenyl phosphate serves as the phosphate donor[6].
Formycin B (1-10 μM; 72 h) inhibits the proliferation of L. donovani and L. mexicana promastigotes, reducing L. donovani parasite counts to 14% or less of the control and L. mexicana to 16% or less[6].
Formycin B (100 μM; 24 h) accumulates as formycin B monophosphate in intact L. mexicana promastigotes, reaching 2.76 μmol/mg protein, with no formycin A monophosphate detected[6].
Formycin B (0.1-10 μg/mL; 3-9 days) significantly inhibits the intracellular replication of T. cruzi Y strain amastigotes in normal mouse peritoneal macrophage monolayers at 0.1 μg/mL[5].
Formycin B (0.1-10 μg/mL; 48 h) reduces intracellular amastigotes of the T. cruzi Y strain in L929 cells by 91% at 1 and 10 μg/mL[5].
Formycin B (1-10 μg/mL; 2 h) pre-exposure slightly reduces subsequent intracellular replication of T. cruzi Y strain amastigotes in mouse peritoneal macrophages[5].
Formycin B (2.5 mM) is phosphorylated to formycin B monophosphate by cell-free extracts of L. mexicana or L. donovani promastigotes at a rate of 0.75 mmol/h/mg protein when p-nitrophenyl phosphate serves as the phosphate donor[6].
Formycin B (1-10 μM; 72 h) inhibits the proliferation of L. donovani and L. mexicana promastigotes, reducing L. donovani parasite counts to 14% or less of the control and L. mexicana to 16% or less[6].
Formycin B (100 μM; 24 h) accumulates as formycin B monophosphate in intact L. mexicana promastigotes, reaching 2.76 μmol/mg protein, with no formycin A monophosphate detected[6].
Parasitic Infection
Innate Immunity
Formycin B (1-10 μM; 72 h) reduces L. mexicana amastigote infection in J774G8 macrophages, decreasing parasite numbers to 0.48 × 106 at 1 μM and to 0.09 × 106 at 10 μM[6].
Protein/Amino Acid Metabolism
Formycin B (2000 μM; days 6-7) inhibits DNA synthesis in PHA-stimulated human PBL by approximately 90%, but protein synthesis by only approximately 60%[2].
Formycin B (500 μM; day 6; 24 h; combined with deoxycytidine 500 μM) does not have its inhibition of cell number or protein synthesis in PHA-stimulated human PBL blocked by deoxycytidine[2].
Formycin B (500 μM; day 6; 24 h; combined with deoxycytidine 500 μM) does not have its inhibition of cell number or protein synthesis in PHA-stimulated human PBL blocked by deoxycytidine[2].
Viral Infection
Formycin B (0.004-40 μg/mL; administered 24 hours before challenge, immediately after viral adsorption, or both) exhibits no activity against vaccinia, herpes simplex, and vesicular stomatitis viruses in PRK cells, with an MIC of > 40 μg/mL for each virus[8].
Others
Formycin B (1000 μM or higher) competitively inhibits human T lymphocyte PNP in the extract, with a Ki of 68 μM when deoxyguanosine is used as the substrate[2].
Formycin B (10-75 μM; day 0) inhibits DNA synthesis in PHA-stimulated human PBL, with 10 μM causing 90% inhibition and 75 μM or higher causing complete inhibition[2].
Formycin B (10-75 μM; days 0-6) inhibits DNA synthesis in PHA-stimulated human PBL in a time-dependent manner; addition on day 6 shifts the dose-response curve by approximately 1 log unit, and 75 μM causes only 50% inhibition[2].
Formycin B (500-2000 μM; 6 h on day 6) does not reduce the number of viable cells in PHA-stimulated human PBLs, but significantly inhibits DNA synthesis per viable cell[2].
Formycin B (100-2000 μM; day 6; combined with deoxyguanosine 10-500 μM) shows no consistent synergistic effect with deoxyguanosine in inhibiting DNA synthesis in PHA-stimulated human PBL[2].
Formycin B (10 min) competitively inhibits quail oviduct chromatin-bound and soluble poly (ADP-Rib) polymerase, with Ki values of 68.9 and 75.0 μM[4].
Formycin B (10-75 μM; day 0) inhibits DNA synthesis in PHA-stimulated human PBL, with 10 μM causing 90% inhibition and 75 μM or higher causing complete inhibition[2].
Formycin B (10-75 μM; days 0-6) inhibits DNA synthesis in PHA-stimulated human PBL in a time-dependent manner; addition on day 6 shifts the dose-response curve by approximately 1 log unit, and 75 μM causes only 50% inhibition[2].
Formycin B (500-2000 μM; 6 h on day 6) does not reduce the number of viable cells in PHA-stimulated human PBLs, but significantly inhibits DNA synthesis per viable cell[2].
Formycin B (100-2000 μM; day 6; combined with deoxyguanosine 10-500 μM) shows no consistent synergistic effect with deoxyguanosine in inhibiting DNA synthesis in PHA-stimulated human PBL[2].
Formycin B (10 min) competitively inhibits quail oviduct chromatin-bound and soluble poly (ADP-Rib) polymerase, with Ki values of 68.9 and 75.0 μM[4].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Cell Proliferation Assay[5]
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Cell Line:L929 cell monolayers infected with Trypanosoma cruzi Y strain amastigotes
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Concentration:0.1, 1, 10 μg/mL
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Incubation Time:48 h
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Result:Infected L929 cells treated with 0.1, 1, or 10 μg/mL formycin B had 27, 91, and 91% fewer intracellular amastigotes, respectively, than controls after 48 h of incubation.
体内実験
Anti-cancerParasitic Infection
Anti-cancer
Formycin B (2.5-80 mg/kg; daily) does not inhibit L-1210 leukemia in mice[1].
Parasitic Infection
Formycin B (5.9-11.8 mg/kg; intraperitoneal injection; once daily; for 19 days) completely protects mice infected with the Y strain from acute death and significantly reduces parasitemia, but does not achieve parasitological cure[5].
Formycin B (11.8 mg/kg; intragastric oral administration; once daily; for 19 days) prevents death and reduces parasitemia in mice infected with the Tulahuen strain of T. cruzi[5].
Formycin B (11.8 mg/kg; intraperitoneal injection; once daily; for 3 weeks) exhibits activity against multiple T. cruzi strains but fails to clear the infection[5].
Formycin B (5.9-100 mg/kg; intraperitoneal injection; once daily; for 5-10 weeks) inhibits but does not eliminate T. cruzi in mice[5].
Formycin B (11.8 mg/kg; intragastric oral administration; once daily; for 19 days) prevents death and reduces parasitemia in mice infected with the Tulahuen strain of T. cruzi[5].
Formycin B (11.8 mg/kg; intraperitoneal injection; once daily; for 3 weeks) exhibits activity against multiple T. cruzi strains but fails to clear the infection[5].
Formycin B (5.9-100 mg/kg; intraperitoneal injection; once daily; for 5-10 weeks) inhibits but does not eliminate T. cruzi in mice[5].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Swiss Webster (female, 18-22 g)[5]
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Dosage:11.8 mg/kg
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Administration:p.o. by gavage; once daily; for 19 days
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Result:There were 0/7 deaths and 0 mortality.
Only rare organisms were detected on day 7.
Parasitemia was lower than in controls.
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Animal Model:Swiss Webster (female, 18-22 g)[5]
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Dosage:11.8 mg/kg
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Administration:i.p.; once daily; for 3 weeks
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Result:Mice infected with MR, CL, or Tulahuen strains responded as did Y strain-infected mice.
Survivors were not cured, as hemocultures and subinoculations revealed organisms after administration completion.
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Animal Model:Swiss Webster (female, 18-22 g)[5]
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Dosage:11.8 or 5.9 mg/kg (105 inoculation; 10 weeks); 50 mg/kg (103 inoculation; 9 weeks); 100 mg/kg (103 inoculation; 5 weeks)
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Administration:i.p.; once daily; for 10 weeks, 9 weeks, or 5 weeks
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Result:After 10 weeks of administration with 11.8 or 5.9 mg/kg, serology and hemocultures were positive at completion.
After 103 inoculum and 50 or 100 mg/kg for 9 or 5 weeks, circulating parasites were still present at completion by subinoculation.
No parasitological cure was achieved.
Related Protocols :
- BrdU Incorporation Assay
- Somatic Cell Culture
- CFSE Dye Dilution Proliferation Assay
- Dye-dilution cell tracking and proliferation staining
- CCK-8/WST-8 Cell Proliferation Assay
- Protocol for Cell Cycle
- Cell Counting-Based Growth Curve Assay
- Colony Formation (Clonogenic) Assay
- Cell Viability Determination by MTT Colorimetric Assay
- EdU Incorporation Assay (Click Chemistry-Based DNA Synthesis Measurement)
- Ki-67 Immunostaining Proliferation Assay
- PCNA Immunodetection Proliferation Assay
- Protocol for Cell Counting and Cell Density Analysis
- MTT Cell Proliferation Assay
化学情報
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CAS 番号 13877-76-4
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分子量 268.23
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分子式 C10H12N4O5
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SMILES
O[C@H]1[C@@H](O)[C@H](C2=NNC3=C2NC=NC3=O)O[C@@H]1CO
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Structure Classification
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Initial Source
Nocardia interforma
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
純度とドキュメンテーション
バッチを選択:
純度:
99.98%
Assay:
99.98%
ee.:
99.98%
参考文献
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Formycin B 関連分類
HY-124210 関連分類
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