ホスホリパーゼ(e.g. PLA)
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 | ||
| S1110 | Varespladib (LY315920) | <1 mg/mL | 76 mg/mL | <1 mg/mL |
| S4089 | Halobetasol Propionate | <1 mg/mL | 97 mg/mL | 38 mg/mL |
| S4255 | Quinacrine 2HCl | 53 mg/mL | 14 mg/mL | 28 mg/mL |
| S6522 | ST 271 | <1 mg/mL | 54 mg/mL | 54 mg/mL |
| S3220 | Trigonelline | -1 mg/mL | 50 mg/mL | -1 mg/mL |
| S8011 | U73122 | <1 mg/mL | 0.01 mg/mL | <1 mg/mL |
| S7321 | FIPI | <1 mg/mL | 45 mg/mL | <1 mg/mL |
| S6564 | ML348 | <1 mg/mL | 83 mg/mL | '10 mg/mL |
| S0766 | RHC 80267 | <1 mg/mL | 79 mg/mL | ''''79 mg/mL |
| S2390 | Polydatin | <1 mg/mL | 78 mg/mL | <1 mg/mL |
| S5913 | Cambinol | <1 mg/mL | 21 mg/mL | '<1 mg/mL |
| S7520 | Darapladib (SB-480848) | <1 mg/mL | 100 mg/mL | 100 mg/mL |
| S7609 | GW4869 | <1 mg/mL | <1 mg/mL | ''<1 mg/mL |
| S2364 | Tanshinone I | <1 mg/mL | 23 mg/mL | <1 mg/mL |
| S4107 | Clofazimine | <1 mg/mL | 5 mg/mL | <1 mg/mL |
| S9794 | Melittin | 100 mg/mL | -1 mg/mL | '-1 mg/mL |
| S0053 | CAY10593 (VU0155069) | <1 mg/mL | 30 mg/mL | <1 mg/mL |
Phospholipase (e.g. PLA)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 |
|---|---|---|---|
| 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. |
Hepatic immune cell infiltration in Mmp2 −/− mice administered the pan-sPLA 2 inhibitor varespladib (10 mg/kg per day, gavage, for 5 days). Collagenase-treated and liberated cells were surface-stained for indicated markers (A) and quantitated. n=3 WT and n=5 Mmp2 −/−. *P≤0.05 vs WT untreated. † P≤0.05 vs Mmp2 −/− untreated. MHC II, major histocompatibility complex II; sPLA2, secreted phospholipase A2; SSC, Side-scattered light (a magnitude proportional to cell granularity or internal complexity); WT, wild type. |
|
| S4089 |
Halobetasol PropionateHalobetasol Propionate (BMY-30056, CGP-14458) is an anti-inflammatory and a dermatologic agent commonly used to treat psoriasis. Halobetasol propionate is thought to act by the induction of phospholipase A2 (PLA2) inhibitory proteins. |
||
| S4255 |
Quinacrine 2HClQuinacrine 2HCl is a lipophilic cationic drug with multiple actions that is commonly used as an anti-protozoal agent. Quinacrine is an effective phospholipase A2 inhibitor. |
||
| S6522 |
ST 271ST271 is a tyrphostin-like protein tyrosine kinase (PTK) inhibitor which inhibits phospholipase D (PLD) activity. |
||
| S3220新 |
TrigonellineTrigonelline (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. |
||
| S8011 |
U73122U73122 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). |
Effect of U73122 and XC on TFEB phosphorylation |
|
| S7321 |
FIPIFIPI (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. |
||
| S6564 |
ML348ML348 (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 80267RHC 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). |
||
| S2390 |
PolydatinPolydatin (Piceid) is a crystal component extracted from the root stem of perennial herbage Polygonum Cuspidatum Sieb.et Zucc. |
||
| S5913 |
CambinolCambinol is a novel uncompetitive nSMase2 inhibitor with a K i value of 7 μM (IC50 = 5 ± 1 μM). |
||
| S7520 |
Darapladib (SB-480848)Darapladib (SB-480848) is a reversible lipoprotein-associated phospholipase A2 (Lp-PLA2) inhibitor with IC50 of 0.25 nM. Phase 3. |
||
| S7609 |
GW4869GW4869 (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. |
U87 and SG2 cells cultured in the indicated conditions for 48 h were exposed to TMZ for 12 h and then were stained with γ-H2AX immediately. Scale bar: 5 μm
|
|
| S2364 |
Tanshinone ITanshinone I, an active principle isolated from Salvia miltiorrhiza (Danshen), is structurally similar to tanshinone IIA and may possess similar cytotoxic effects on tumor cells. |
Tan-1 inhibited the migration of HMEC-1 cells (F). Cells were treated with vehicle (a), or Tan-1 12.5 μM (b), 25 μM (c) or 50 μM (d) in the corresponding left panel for 6 h. Magnification: 10×. The data from three independent experiments were expressed as mean ± SD in the corresponding right panel. *p < 0.05; **p < 0.01.
|
|
| S4107 |
ClofazimineClofazimine (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. |
||
| S9794新 |
MelittinMelittin (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. |
||
| S0053新 |
CAY10593 (VU0155069)CAY10593 (VU0155069) is a selective phospholipase D1 (PLD1) antagonist that impairs human P2X7 acivation. |
| 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 |
|---|---|---|---|
| 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. |
Hepatic immune cell infiltration in Mmp2 −/− mice administered the pan-sPLA 2 inhibitor varespladib (10 mg/kg per day, gavage, for 5 days). Collagenase-treated and liberated cells were surface-stained for indicated markers (A) and quantitated. n=3 WT and n=5 Mmp2 −/−. *P≤0.05 vs WT untreated. † P≤0.05 vs Mmp2 −/− untreated. MHC II, major histocompatibility complex II; sPLA2, secreted phospholipase A2; SSC, Side-scattered light (a magnitude proportional to cell granularity or internal complexity); WT, wild type. |
|
| S4089 |
Halobetasol PropionateHalobetasol Propionate (BMY-30056, CGP-14458) is an anti-inflammatory and a dermatologic agent commonly used to treat psoriasis. Halobetasol propionate is thought to act by the induction of phospholipase A2 (PLA2) inhibitory proteins. |
||
| S4255 |
Quinacrine 2HClQuinacrine 2HCl is a lipophilic cationic drug with multiple actions that is commonly used as an anti-protozoal agent. Quinacrine is an effective phospholipase A2 inhibitor. |
||
| S6522 |
ST 271ST271 is a tyrphostin-like protein tyrosine kinase (PTK) inhibitor which inhibits phospholipase D (PLD) activity. |
||
| S3220新 |
TrigonellineTrigonelline (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. |
||
| S8011 |
U73122U73122 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). |
Effect of U73122 and XC on TFEB phosphorylation |
|
| S7321 |
FIPIFIPI (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. |
||
| S6564 |
ML348ML348 (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 80267RHC 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). |
||
| S2390 |
PolydatinPolydatin (Piceid) is a crystal component extracted from the root stem of perennial herbage Polygonum Cuspidatum Sieb.et Zucc. |
||
| S5913 |
CambinolCambinol is a novel uncompetitive nSMase2 inhibitor with a K i value of 7 μM (IC50 = 5 ± 1 μM). |
||
| S7520 |
Darapladib (SB-480848)Darapladib (SB-480848) is a reversible lipoprotein-associated phospholipase A2 (Lp-PLA2) inhibitor with IC50 of 0.25 nM. Phase 3. |
||
| S7609 |
GW4869GW4869 (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. |
U87 and SG2 cells cultured in the indicated conditions for 48 h were exposed to TMZ for 12 h and then were stained with γ-H2AX immediately. Scale bar: 5 μm
|
|
| S2364 |
Tanshinone ITanshinone I, an active principle isolated from Salvia miltiorrhiza (Danshen), is structurally similar to tanshinone IIA and may possess similar cytotoxic effects on tumor cells. |
Tan-1 inhibited the migration of HMEC-1 cells (F). Cells were treated with vehicle (a), or Tan-1 12.5 μM (b), 25 μM (c) or 50 μM (d) in the corresponding left panel for 6 h. Magnification: 10×. The data from three independent experiments were expressed as mean ± SD in the corresponding right panel. *p < 0.05; **p < 0.01.
|
| 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 |
|---|---|---|---|
| S4107 |
ClofazimineClofazimine (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. |
2020, acsinfecdis.0c00486 2020, ddaa244 |
|
| S9794新 |
MelittinMelittin (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. |
| 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 |
|---|---|---|---|
| S0053新 |
CAY10593 (VU0155069)CAY10593 (VU0155069) is a selective phospholipase D1 (PLD1) antagonist that impairs human P2X7 acivation. |
