S8011 |
U73122
|
U73122 is a potent phospholipase C (PLC) inhibitor, which reduces agonist-induced Ca2+ increases in platelets and PMN. U73122 potently inhibits human 5-lipoxygenase (5-LO). |
-
Nat Commun, 2024, 15(1):1300
-
Autophagy, 2024, 10.1080/15548627.2024.2395797
-
Cell Rep, 2024, 43(3):113929
|
|
S7609 |
GW4869
|
GW4869 (GW69A, GW554869A) is a neutral, noncompetitive inhibitor of sphingomyelinase (SMase) with an IC50 of 1 μM. It is selective for N-SMase, and does not inhibit acid SMase at up to at least 150 μM, also is a commonly used exosome inhibitor. |
-
Signal Transduct Target Ther, 2024, 9(1):253
-
ACS Nano, 2024, 18(5):4241-4255
-
J Nanobiotechnology, 2024, 22(1):361
|
|
S1110 |
Varespladib (LY315920)
|
Varespladib (LY315920) is a potent and selective human non-pancreatic secretory phospholipase A2 (hnsPLA) inhibitor with IC50 of 7 nM. Phase 3. |
-
Int J Mol Sci, 2024, 25(19)10649
-
Front Immunol, 2022, 13:824746
-
J Med Chem, 2019, 62(4):1999-2007
|
|
S2364 |
Tanshinone I
|
Tanshinone I, an active principle isolated from Salvia miltiorrhiza (Danshen), is structurally similar to tanshinone IIA and may possess similar cytotoxic effects on tumor cells. |
-
Int J Oncol, 2023, 63(1)76
-
Phytomedicine, 2022, 98:153958
-
Drug Des Devel Ther, 2022, 16:3197-3213
|
|
S7520 |
Darapladib
|
Darapladib is a reversible lipoprotein-associated phospholipase A2 (Lp-PLA2) inhibitor with IC50 of 0.25 nM. Phase 3.
|
-
iScience, 2024, 27(5):109774
-
Nat Commun, 2023, 14(1):5728
-
Nat Commun, 2023, 14(1):5728
|
|
S4107 |
Clofazimine
|
Clofazimine (NSC-141046) is a rhimophenazine dye, originally developed for the treatment of tuberculosis, it has both antimicrobial and antiinflammatory activity, postulated mechanisms of action include intercalation of clofazimine with bacterial DNA and increasing levels of cellular phospholipase A2. |
-
Viruses, 2024, 16(4)640
-
Cell Rep Methods, 2023, 3(10):100599
-
Blood, 2022, blood.2021014304
|
|
S4255 |
Quinacrine 2HCl
|
Quinacrine 2HCl(Quinacrine dihydrochloride) is a lipophilic cationic drug with multiple actions that is commonly used as an anti-protozoal agent. Quinacrine is an effective phospholipase A2 inhibitor. |
-
Molecules, 2022, 27(17)5561
-
Toxicol In Vitro, 2022, 83:105420
-
Mol Oncol, 2020, 10.1002/1878-0261.12853
|
|
S2390 |
Polydatin
|
Polydatin (Piceid) is a crystal component extracted from the root stem of perennial herbage Polygonum Cuspidatum Sieb.et Zucc. |
-
Biochem Biophys Res Commun, 2021, 556:149-155
-
J Med Virol, 2019, 91(8):1440-1447
|
|
S0053 |
CAY10593 (VU0155069)
|
CAY10593 (VU0155069) is a selective phospholipase D1 (PLD1) antagonist that impairs human P2X7 acivation. |
-
Free Radic Biol Med, 2021, S0891-5849(21)00821-2
|
|
S0982 |
m-3M3FBS
|
m-3M3FBS is a potent activator of phospholipase C (PLC) that stimulates a transient intracellular calcium concentration increase in neutrophils. m-3M3FBS induces apoptosis in monocytic leukemia cells. |
-
Pharmaceuticals (Basel), 2022, 15(12)1444
|
|
S9794 |
Melittin
|
Melittin (MLT, Forapin, Forapine) is an activator of phospholipase A2 (PLA2) that stimulates the activity of the low molecular weight PLA2, while it does not the increase the activity of the high molecular weight enzyme. |
-
Nutr Res Pract, 2024, 18(2):210-222
-
EMBO J, 2022, e110439
|
|
S3220 |
Trigonelline
|
Trigonelline (Trigenolline) is a plant alkaloid and a major component of coffee and fenugreek with anti-degranulation, anti-diabetic, antioxidant, anti-inflammatory, and neuroprotective effects. Trigonelline inhibits FcεRI-mediated intracellular signaling pathways, such as phosphorylation of PLCγ1, PI3K, and Akt. Trigonelline (Trigenolline) also inhibits the microtubule formation in RBL-2H3 cells. |
-
Biomed Pharmacother, 2021, 143:112204
|
|
S6522 |
ST 271
|
ST271 is a tyrphostin-like protein tyrosine kinase (PTK) inhibitor which inhibits phospholipase D (PLD) activity. |
|
|
S7321 |
FIPI
|
FIPI (5-Fluoro-2-indolyl deschlorohalopemide), a derivative of halopemide, is a potent and selective inhibitor of phospholipase D with IC50 of 25 nM and 20 nM for PLD1 and PLD2, respectively. |
-
Cell Chem Biol, 2024, S2451-9456(24)00090-4
|
|
S9478 |
Trans-4-Phenyl-3-buten-2-one
|
Trans-4-Phenyl-3-buten-2-one (trans-Benzylideneacetone, trans-Benzalacetone, trans-Benzylideneacetone) is an inhibitor of the enzyme phospholipase A2 (PLA2). Trans-4-Phenyl-3-buten-2-one is used as a flavouring agent, a fragrance and a bacterial metabolite. |
|
|
S6564 |
ML348
|
ML348 (GNF-Pf-1127) is a potent and selective APT1 (Acyl protein thioesterase 1)/lysophospholipase 1 (LYPLA1) inhibitor with Ki values of 280 nM and >10 μM for APT1 and APT2, respectively. |
|
|
S0766 |
RHC 80267
|
RHC 80267 (U-57908) is a potent and selective inhibitor of diacylglycerol lipase (DAGL, DAG lipase) with IC50 of 4 μM for cholinesterase activity. RHC 80267 inhibits cyclooxygenase (COX) activity, phospholipase C (PLC) activity and the hydrolysis of phosphatidylcholine (PC). |
|
|
S5913 |
Cambinol
|
Cambinol is a novel uncompetitive nSMase2 inhibitor with a K i value of 7 μM (IC50 = 5 ± 1 μM). |
|
|
S8011 |
U73122
|
U73122 is a potent phospholipase C (PLC) inhibitor, which reduces agonist-induced Ca2+ increases in platelets and PMN. U73122 potently inhibits human 5-lipoxygenase (5-LO). |
- Nat Commun, 2024, 15(1):1300
- Autophagy, 2024, 10.1080/15548627.2024.2395797
- Cell Rep, 2024, 43(3):113929
|
|
S7609 |
GW4869
|
GW4869 (GW69A, GW554869A) is a neutral, noncompetitive inhibitor of sphingomyelinase (SMase) with an IC50 of 1 μM. It is selective for N-SMase, and does not inhibit acid SMase at up to at least 150 μM, also is a commonly used exosome inhibitor. |
- Signal Transduct Target Ther, 2024, 9(1):253
- ACS Nano, 2024, 18(5):4241-4255
- J Nanobiotechnology, 2024, 22(1):361
|
|
S1110 |
Varespladib (LY315920)
|
Varespladib (LY315920) is a potent and selective human non-pancreatic secretory phospholipase A2 (hnsPLA) inhibitor with IC50 of 7 nM. Phase 3. |
- Int J Mol Sci, 2024, 25(19)10649
- Front Immunol, 2022, 13:824746
- J Med Chem, 2019, 62(4):1999-2007
|
|
S2364 |
Tanshinone I
|
Tanshinone I, an active principle isolated from Salvia miltiorrhiza (Danshen), is structurally similar to tanshinone IIA and may possess similar cytotoxic effects on tumor cells. |
- Int J Oncol, 2023, 63(1)76
- Phytomedicine, 2022, 98:153958
- Drug Des Devel Ther, 2022, 16:3197-3213
|
|
S7520 |
Darapladib
|
Darapladib is a reversible lipoprotein-associated phospholipase A2 (Lp-PLA2) inhibitor with IC50 of 0.25 nM. Phase 3.
|
- iScience, 2024, 27(5):109774
- Nat Commun, 2023, 14(1):5728
- Nat Commun, 2023, 14(1):5728
|
|
S4255 |
Quinacrine 2HCl
|
Quinacrine 2HCl(Quinacrine dihydrochloride) is a lipophilic cationic drug with multiple actions that is commonly used as an anti-protozoal agent. Quinacrine is an effective phospholipase A2 inhibitor. |
- Molecules, 2022, 27(17)5561
- Toxicol In Vitro, 2022, 83:105420
- Mol Oncol, 2020, 10.1002/1878-0261.12853
|
|
S2390 |
Polydatin
|
Polydatin (Piceid) is a crystal component extracted from the root stem of perennial herbage Polygonum Cuspidatum Sieb.et Zucc. |
- Biochem Biophys Res Commun, 2021, 556:149-155
- J Med Virol, 2019, 91(8):1440-1447
|
|
S3220 |
Trigonelline
|
Trigonelline (Trigenolline) is a plant alkaloid and a major component of coffee and fenugreek with anti-degranulation, anti-diabetic, antioxidant, anti-inflammatory, and neuroprotective effects. Trigonelline inhibits FcεRI-mediated intracellular signaling pathways, such as phosphorylation of PLCγ1, PI3K, and Akt. Trigonelline (Trigenolline) also inhibits the microtubule formation in RBL-2H3 cells. |
- Biomed Pharmacother, 2021, 143:112204
|
|
S6522 |
ST 271
|
ST271 is a tyrphostin-like protein tyrosine kinase (PTK) inhibitor which inhibits phospholipase D (PLD) activity. |
|
|
S7321 |
FIPI
|
FIPI (5-Fluoro-2-indolyl deschlorohalopemide), a derivative of halopemide, is a potent and selective inhibitor of phospholipase D with IC50 of 25 nM and 20 nM for PLD1 and PLD2, respectively. |
- Cell Chem Biol, 2024, S2451-9456(24)00090-4
|
|
S9478 |
Trans-4-Phenyl-3-buten-2-one
|
Trans-4-Phenyl-3-buten-2-one (trans-Benzylideneacetone, trans-Benzalacetone, trans-Benzylideneacetone) is an inhibitor of the enzyme phospholipase A2 (PLA2). Trans-4-Phenyl-3-buten-2-one is used as a flavouring agent, a fragrance and a bacterial metabolite. |
|
|
S6564 |
ML348
|
ML348 (GNF-Pf-1127) is a potent and selective APT1 (Acyl protein thioesterase 1)/lysophospholipase 1 (LYPLA1) inhibitor with Ki values of 280 nM and >10 μM for APT1 and APT2, respectively. |
|
|
S0766 |
RHC 80267
|
RHC 80267 (U-57908) is a potent and selective inhibitor of diacylglycerol lipase (DAGL, DAG lipase) with IC50 of 4 μM for cholinesterase activity. RHC 80267 inhibits cyclooxygenase (COX) activity, phospholipase C (PLC) activity and the hydrolysis of phosphatidylcholine (PC). |
|
|
S5913 |
Cambinol
|
Cambinol is a novel uncompetitive nSMase2 inhibitor with a K i value of 7 μM (IC50 = 5 ± 1 μM). |
|
|
S4107 |
Clofazimine
|
Clofazimine (NSC-141046) is a rhimophenazine dye, originally developed for the treatment of tuberculosis, it has both antimicrobial and antiinflammatory activity, postulated mechanisms of action include intercalation of clofazimine with bacterial DNA and increasing levels of cellular phospholipase A2. |
- Viruses, 2024, 16(4)640
- Cell Rep Methods, 2023, 3(10):100599
- Blood, 2022, blood.2021014304
|
|
S0982 |
m-3M3FBS
|
m-3M3FBS is a potent activator of phospholipase C (PLC) that stimulates a transient intracellular calcium concentration increase in neutrophils. m-3M3FBS induces apoptosis in monocytic leukemia cells. |
- Pharmaceuticals (Basel), 2022, 15(12)1444
|
|
S9794 |
Melittin
|
Melittin (MLT, Forapin, Forapine) is an activator of phospholipase A2 (PLA2) that stimulates the activity of the low molecular weight PLA2, while it does not the increase the activity of the high molecular weight enzyme. |
- Nutr Res Pract, 2024, 18(2):210-222
- EMBO J, 2022, e110439
|
|