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)
カタログ番号	製品カタログ	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
S9478	Trans-4-Phenyl-3-buten-2-one	29 mg/mL	29 mg/mL	''29 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
S0982	m-3M3FBS	<1 mg/mL	69 mg/mL	'''69 mg/mL
S0053	CAY10593 (VU0155069)	<1 mg/mL	30 mg/mL	<1 mg/mL

亜型選択性的な製品

Phospholipase (e.g. PLA)製品

All (19) Phospholipase (e.g. PLA)阻害剤(15) Phospholipase (e.g. PLA)活性剤(3) Phospholipase (e.g. PLA)拮抗剤(1)

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.	J Med Chem, 2019, 62(4):1999-2007 J Med Chem, 2019, 62(4):1999-2007 Nature, 2018, 560(7718):372-376	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 Propionate Halobetasol 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 2HCl Quinacrine 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.	Mol Oncol, 2020, 10.1002/1878-0261.12853 Mol Oncol, 2020, 10.1002/1878-0261.12853 F1000Res, 2016, 5:150
S6522	ST 271 ST271 is a tyrphostin-like protein tyrosine kinase (PTK) inhibitor which inhibits phospholipase D (PLD) activity.
S9478^新	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.
S3220^新	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.
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).	Aging Cell, 2021, e13375 Cell, 2020, 182(3):685-712.e19 Cell, 2020, 182(3):685-712.e19	Effect of U73122 and XC on TFEB phosphorylation
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.
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).
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
S5913	Cambinol Cambinol 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.	Biochem Pharmacol, 2016, 102:78-96
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.	J Clin Invest, 2021, 131(9)142865 Theranostics, 2021, 11(3):1473-1492 Free Radic Biol Med, 2021, 163:220-233	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 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.	Mol Med Rep, 2021, 23(1)40 Int Immunopharmacol, 2019, 10.1016/j.intimp.2019.106040 J Med Virol, 2019, 91(8):1440-1447	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	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.	ACS Infect Dis, 2020, acsinfecdis.0c00486 Hum Mol Genet, 2020, ddaa244
S9794^新	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.
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.
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.	J Med Chem, 2019, 62(4):1999-2007 J Med Chem, 2019, 62(4):1999-2007 Nature, 2018, 560(7718):372-376	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 Propionate Halobetasol 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 2HCl Quinacrine 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.	Mol Oncol, 2020, 10.1002/1878-0261.12853 Mol Oncol, 2020, 10.1002/1878-0261.12853 F1000Res, 2016, 5:150
S6522	ST 271 ST271 is a tyrphostin-like protein tyrosine kinase (PTK) inhibitor which inhibits phospholipase D (PLD) activity.
S9478^新	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.
S3220^新	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.
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).	Aging Cell, 2021, e13375 Cell, 2020, 182(3):685-712.e19 Cell, 2020, 182(3):685-712.e19	Effect of U73122 and XC on TFEB phosphorylation
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.
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).
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
S5913	Cambinol Cambinol 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.	Biochem Pharmacol, 2016, 102:78-96
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.	J Clin Invest, 2021, 131(9)142865 Theranostics, 2021, 11(3):1473-1492 Free Radic Biol Med, 2021, 163:220-233	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 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.	Mol Med Rep, 2021, 23(1)40 Int Immunopharmacol, 2019, 10.1016/j.intimp.2019.106040 J Med Virol, 2019, 91(8):1440-1447	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
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.	ACS Infect Dis, 2020, acsinfecdis.0c00486 Hum Mol Genet, 2020, ddaa244
S9794^新	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.
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.

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

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.

ACS Infect Dis, 2020, acsinfecdis.0c00486

Hum Mol Genet, 2020, ddaa244

S9794^新

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.

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.