Phospholipase is a member of a very complex group of enzymes that break down phospholipids into fatty acids and other compounds. Phospholipases are defined by the enzymatic reaction they catalyze. The classes are phospholipase A, which has members A1 and A2; phospholipase B, which can carry out the reactions of both A1 and A2; phospholipase C; and phospholipase D. Phospholipase A2 (PLA2) catalyses the hydrolysis of the sn-2 position of glycerophospholipids to yield fatty acids and lysophospholipids. Phospholipase C (PLC) converts phosphatidylinositol 4,5-bisphosphate (PIP2) to inositol 1,4,5-trisphosphate (IP3) and diacylglycerol (DAG). DAG and IP3 each control diverse cellular processes and are also substrates for synthesis of other important signaling molecules. PLC is thus central to many important interlocking regulatory networks. Phospholipase D (PLD) is an essential enzyme responsible for the production of the lipid second messenger phosphatidic acid (PA), which is involved in fundamental cellular processes, including membrane trafficking, actin cytoskeleton remodeling, cell proliferation and cell survival.


Anti-infection >
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Antibody-drug Conjugate >
ADC Cytotoxin ADC Linker Drug-Linker Conjugates for ADC PROTAC-linker Conjugate for PAC
Apoptosis >
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Autophagy >
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Antifolate APC ATM/ATR Aurora Kinase Casein Kinase CDK Checkpoint Kinase (Chk) CRISPR/Cas9 Deubiquitinase DNA Alkylator/Crosslinker DNA-PK DNA/RNA Synthesis Eukaryotic Initiation Factor (eIF) G-quadruplex Haspin Kinase HDAC HSP IRE1 Kinesin LIM Kinase (LIMK) Microtubule/Tubulin Mps1 Nucleoside Antimetabolite/Analog p97 PAK PARP PERK Polo-like Kinase (PLK) PPAR RAD51 ROCK Sirtuin SRPK Telomerase TOPK Topoisomerase Wee1
Cytoskeleton >
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Epigenetics >
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GPCR/G Protein >
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Immunology/Inflammation >
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JAK/STAT Signaling >
EGFR JAK Pim STAT
MAPK/ERK Pathway >
ERK JNK KLF MAP3K MAP4K MAPKAPK2 (MK2) MEK Mixed Lineage Kinase MNK p38 MAPK Raf Ribosomal S6 Kinase (RSK)
Membrane Transporter/Ion Channel >
ATP Synthase BCRP Calcium Channel CFTR Chloride Channel CRAC Channel CRM1 EAAT2 GABA Receptor GlyT HCN Channel iGluR Monoamine Transporter Monocarboxylate Transporter Na+/Ca2+ Exchanger Na+/HCO3- Cotransporter Na+/K+ ATPase nAChR NKCC P-glycoprotein P2X Receptor Potassium Channel Proton Pump SGLT Sodium Channel TRP Channel URAT1
Metabolic Enzyme/Protease >
15-PGDH 5 alpha Reductase 5-Lipoxygenase Acetyl-CoA Carboxylase Acyltransferase Adenosine Deaminase Adenosine Kinase Aldehyde Dehydrogenase (ALDH) Aldose Reductase Aminopeptidase Angiotensin-converting Enzyme (ACE) ATGL ATP Citrate Lyase Carbonic Anhydrase Carboxypeptidase Cathepsin CETP COMT Cytochrome P450 Dipeptidyl Peptidase Dopamine β-hydroxylase E1/E2/E3 Enzyme Elastase Enolase FAAH FABP Factor Xa Farnesyl Transferase Fatty Acid Synthase (FAS) FXR Glucokinase GSNOR Gutathione S-transferase HCV Protease Hexokinase HIF/HIF Prolyl-Hydroxylase HIV Integrase HIV Protease HMG-CoA Reductase (HMGCR) HSP Indoleamine 2,3-Dioxygenase (IDO) Isocitrate Dehydrogenase (IDH) Lactate Dehydrogenase LXR MAGL Mineralocorticoid Receptor Mitochondrial Metabolism MMP Nampt NEDD8-activating Enzyme Neprilysin PAI-1 PDHK PGC-1α Phosphatase Phosphodiesterase (PDE) Phospholipase Procollagen C Proteinase Proteasome Pyruvate Kinase RAR/RXR Renin ROR Ser/Thr Protease SGK Stearoyl-CoA Desaturase (SCD) Thrombin Tryptophan Hydroxylase Tyrosinase Xanthine Oxidase
Neuronal Signaling >
5-HT Receptor AChE Adenosine Kinase Amyloid-β Beta-secretase CaMK CGRP Receptor COMT Dopamine Receptor Dopamine Transporter FAAH GABA Receptor GlyT iGluR Imidazoline Receptor mAChR Melatonin Receptor Monoamine Oxidase nAChR Neurokinin Receptor Opioid Receptor Serotonin Transporter γ-secretase
NF-κB >
NF-κB IKK Keap1-Nrf2 MALT1
PI3K/Akt/mTOR >
Akt AMPK ATM/ATR DNA-PK GSK-3 MELK mTOR PDK-1 PI3K PI4K PIKfyve PTEN
PROTAC >
PROTAC E3 Ligase Ligand-Linker Conjugate Ligand for E3 Ligase PROTAC Linker PROTAC-linker Conjugate for PAC
Protein Tyrosine Kinase/RTK >
Ack1 ALK Bcr-Abl BMX Kinase Btk c-Fms c-Kit c-Met/HGFR Discoidin Domain Receptor DYRK EGFR Ephrin Receptor FAK FGFR FLT3 IGF-1R Insulin Receptor IRAK Itk PDGFR PKA Pyk2 ROS Src Syk TAM Receptor Trk Receptor VEGFR
Stem Cell/Wnt >
Casein Kinase ERK Gli GSK-3 Hedgehog Hippo (MST) JAK Notch Oct3/4 PKA Porcupine ROCK sFRP-1 Smo STAT TGF-beta/Smad Wnt YAP β-catenin γ-secretase
TGF-beta/Smad >
TGF-beta/Smad PKC ROCK TGF-β Receptor
Vitamin D Related >
VD/VDR
Others >
Androgen Receptor Aromatase Estrogen Receptor/ERR Progesterone Receptor Thyroid Hormone Receptor Others

WH-15

WH-15 is a fluorogenic PLC reporter with Km value of 49; 30, 86.1 µM for PLC-γ1, PLC-δ1, PLC-β2, respectively. WH-15 can be cleaved in a cascade reaction to generate fluorescent 6-aminoquinoline. WH-15 can be used to respond to imaging PLC activity in live cells[1].

  • CAS Number: 1264748-47-1
  • MF: C31H43N2O18P3
  • MW: 824.60
  • Catalog: Phospholipase
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

MJ33 lithium

MJ33 lithium is an active-site-directed, specific, competitive, and reversible phospholipase A2 (PLA2) inhibitor. MJ33 lithium blocks the calcium-independent phospholipase A2 (iPLA2) activity of Prdx6[1]. MJ33 lithium has a critical effect on inflammatory brain damage[2].

  • CAS Number: 1135306-36-3
  • MF: C22H43F3LiO7P
  • MW: 514.48
  • Catalog: Phospholipase
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

ML211

ML-211 is a carbamate-based dual inhibitor of acyl-protein thioesterase 1 (APT1)/lysophospholipase 1 (LYPLA1) (IC50=17 nM) and LYPLA2 (IC50=30 nM). ML-211 also inhibits theserine hydrolase ABHD11 with an IC50 value of 10 nM but is ≥ 50-fold selective for LYPLA in a panel of 20 additional serine hydrolases[1].

  • CAS Number: 2205032-89-7
  • MF: C25H30N4O2
  • MW: 418.531
  • Catalog: MAGL
  • Density: 1.2±0.1 g/cm3
  • Boiling Point: 583.9±42.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 306.9±27.9 °C

2-Amino-1,3-octadecanediol

D-Erythro-dihydrosphingosin directly inhibits cytosolic phospholipase A2α (cPLA2α) activity.

  • CAS Number: 764-22-7
  • MF: C18H39NO2
  • MW: 301.508
  • Catalog: Phospholipase
  • Density: 0.9±0.1 g/cm3
  • Boiling Point: 446.2±25.0 °C at 760 mmHg
  • Melting Point: 70-72ºC
  • Flash Point: 223.7±23.2 °C

Tanshinone I

Tanshinone I is an inhibitor of type IIA human recombinant sPLA2 (IC50=11 μM) and rabbit recombinant cPLA2 (IC50=82 μM).

  • CAS Number: 568-73-0
  • MF: C18H12O3
  • MW: 276.286
  • Catalog: Phospholipase
  • Density: 1.3±0.1 g/cm3
  • Boiling Point: 498.0±24.0 °C at 760 mmHg
  • Melting Point: 233-234ºC
  • Flash Point: 245.9±15.6 °C

C12 NBD-SPHINGOMYELIN

C12 NBD sphingomyelin is an active derivative of sphingomyelin (HY-113498) that is tagged with fluorescent C12 nitrobenzoxadiazole (C12 NBD). C12 NBD sphingomyelin can be used as a sphingomyelinase substrate for studying the metabolism and transport of sphingomyelins (Ex=470 nm, Em=525 nm)[1].

  • CAS Number: 254117-01-6
  • MF: C41H73N6O9P
  • MW: 825.027
  • Catalog: Phospholipase
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

BAPTA tetrasodium

BAPTA tetrasodium is a selective chelator for calcium. BAPTA tetrasodium, as calcium indicator, has high selectivity against magnesium and calcium. BAPTA tetrasodium is widely used as an intracellular buffer for investigating the effects of Ca2+ release from intracellular stores or influx via Ca2+-permeable channels in the plasma membrane. BAPTA tetrasodium can also inhibit phospholipase C activity independently of their role as Ca2+ chelators[1][2][3].

  • CAS Number: 126824-24-6
  • MF: C22H20N2Na4O10
  • MW: 564.361
  • Catalog: Phospholipase
  • Density: N/A
  • Boiling Point: 766.6ºC at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 417.4ºC

Methyl Arachidonyl Fluorophosphonate

MAFP (Methyl Arachidonyl Fluorophosphonate) is an selective, active-site directed and irreversible inhibitor of cPLA2 and iPLA2. MAFP is also a potent irreversible inhibitor of anandamide amidase.

  • CAS Number: 188404-10-6
  • MF: C21H36FO2P
  • MW: 370.482
  • Catalog: Phospholipase
  • Density: 1.0±0.1 g/cm3
  • Boiling Point: 455.3±34.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 229.1±25.7 °C

SB-435495 hydrochloride

SB-435495 hydrochloride is a potent, selective, reversible, non-covalent and orally active Lp-PLA2 inhibitor with an IC50 of 0.06 nM[1][3].

  • CAS Number: 304694-41-5
  • MF: C38H41ClF4N6O2S
  • MW: 757.28
  • Catalog: Phospholipase
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

CCT129957

CCT129957 is an indole derivative and a potent phospholipase C-γ (PLC-γ) inhibitor with an IC50 of ~3 μM and a GC50 of 15 μM. CCT129957 inhibits Ca2+ release in squamous carcinoma cells at ~15 μM[1][2].

  • CAS Number: 883098-58-6
  • MF: C17H15N3O3
  • MW: 309.32
  • Catalog: Phospholipase
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

SB-435495 ditartrate

SB-435495 ditartrate is a potent, selective, reversible, non-covalent and orally active Lp-PLA2 inhibitor with an IC50 of 0.06 nM[1][3].

  • CAS Number: 304694-43-7
  • MF: C46H52F4N6O14S
  • MW: 1021.00
  • Catalog: Phospholipase
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

EA4

EA4, a derivative of quinone, is an inhibitor for both rPLA and cPLA. EA4 can inhibit rPLA2 with a Ki value of 130 μM. EA4 can be used for the research of hemostasis, thrombosis, and erythropoiesis[1].

  • CAS Number: 389614-94-2
  • MF: C19H17ClN2O2
  • MW: 340.803
  • Catalog: Phospholipase
  • Density: 1.3±0.1 g/cm3
  • Boiling Point: 508.3±50.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 261.2±30.1 °C

FIPI

FIPI is a derivative of halopemide which potently inhibits both PLD1 and PLD2 with IC50s of 25 nM and 20 nM, respectively.

  • CAS Number: 939055-18-2
  • MF: C23H24FN5O2
  • MW: 421.467
  • Catalog: Autophagy
  • Density: 1.4±0.1 g/cm3
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

2-(4-(2-Amino-2-oxoethoxy)-1-benzyl-2-ethyl-1H-indol-3-yl)-2-oxoacetamide

hnps-PLA-IN-1 (compound 5aa), a indole-3-acetamide, is a hnps-PLA2 inhibitor (IC50=0.124 μM)[1].

  • CAS Number: 185298-58-2
  • MF: C21H21N3O4
  • MW: 379.41
  • Catalog: Phospholipase
  • Density: 1.3±0.1 g/cm3
  • Boiling Point: 709.0±70.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 382.6±35.7 °C

Giripladib

Giripladib (PLA-695) is a indole-based inhibitor of cytosolic phospholipase A2 (cPLA2). Giripladib can be used for osteoarthritis and breast cancer research[1][2].

  • CAS Number: 865200-20-0
  • MF: C41H36ClF3N2O4S
  • MW: 745.25
  • Catalog: Phospholipase
  • Density: 1.29g/cm3
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Efipladib

Efipladib is a potent, selective and orally active cPLA2α inhibitor with an IC50 of 0.04 μM and a Kd of 0.067 μM[1].

  • CAS Number: 381683-94-9
  • MF: C40H35Cl3N2O4S
  • MW: 746.14
  • Catalog: Phospholipase
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

ROC-0929

ROC-0929 (compound 13a) is a potent and selective inhibitor of secreted phospholipases A2 (sPLA2s) with an IC50 of 80 nM, specially targeting hGX. ROC-0929 inhibits the phosphorylation of ERK1/2 and p-38. Secreted phospholipases A2 (sPLA2s) are a family of disulfide-rich, Ca2+-dependent enzymes that hydrolyze the sn-2 position of glycero-phospholipids to release a fatty acid and a lysophospholipid. ROC-0929 has the potential for the treatment of inflammation related diseases[1].

  • CAS Number: 1048660-43-0
  • MF: C30H31N3O6S
  • MW: 561.65
  • Catalog: Phospholipase
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Melittin (free acid) trifluoroacetate salt

Melittin free acid is a basic 26-amino-acid polypeptide, the major active ingredient of honeybee venom. Melittin free acid is an activator of phospholipase A2 (PLA2). Melittin free acid has broad-spectrum antifungal activity with MIC values of 0.4-60 μM. Melittin free acid hinders fungal growth by inducing cell apoptosis, repressing (1,3)-β-D-glucan synthase and participating in other pathways[1][2].

  • CAS Number: 123168-46-7
  • MF: C131H228N38O32
  • MW: 2847.448
  • Catalog: Fungal
  • Density: 1.4±0.1 g/cm3
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

sPLA2 inhibitor 1

sPLA2 inhibitor 1, a D-tyrosine derivative, is an orally active, potent secretory phospholipase A2 (sPLA2) inhibitor with an IC50 of 29 nM for human nonpancreatic secretory PLA2 isoform IIa (hnpsPLA2-IIa). sPLA2 inhibitor 1 has anti-inflammatory activity[1].

  • CAS Number: 393569-31-8
  • MF: C31H37NO4
  • MW: 487.63
  • Catalog: Phospholipase
  • Density: 1.1±0.1 g/cm3
  • Boiling Point: 720.9±60.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 389.8±32.9 °C

(±)-trans-GK563

GK563 is a selective Ca2+-independent phospholipase A2 (GVIA iPLA2) inhibitor with an IC50 value of 1 nM. GK563 is 22000 times more active against GVIA iPLA2 than GIVA cPLA2. GK563 reduces β-cell apoptosis induced by proinflammatory cytokines, raising the possibility that it can be beneficial in countering autoimmune diseases, such as type 1 diabetes[1].

  • CAS Number: 2351820-19-2
  • MF: C16H22O2
  • MW: 246.345
  • Catalog: Apoptosis
  • Density: 1.0±0.1 g/cm3
  • Boiling Point: 364.2±11.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 152.3±16.7 °C

GK187

GK187 is a potent and selective Group VIA calcium-independent phospholipase A2 (GVIA iPLA2) inhibitor with an XI(50) value of 0.0001. GK187 can be used for researching various neurological disorders[1]. [The XI(50) is the mole fraction of the inhibitor in the total substrate interface required to inhibit the enzyme by 50%.]

  • CAS Number: 1071001-50-7
  • MF: C14H15F5O2
  • MW: 310.260
  • Catalog: Phospholipase
  • Density: 1.2±0.1 g/cm3
  • Boiling Point: 330.3±42.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 148.5±22.8 °C

Lp-PLA2-IN-4

Lp-PLA2-IN-4 is a potent inhibitor of lipoprotein-associated phospholipase A2 (Lp-PLA2). Lp-PLA2 previously known as platelet- activating factor acetylhydrolase (PAF-AH), is a phospholipase A2 enzyme involved in hydrolysis of lipoprotein lipids or phospholipids. Lp-PLA2-IN-4 has the potential for the research of diseases associated with the activity of Lp-PLA2, for example atherosclerosis, Alzheimer's disease (extracted from patent WO2021228159A1, compound 38)[1].

  • CAS Number: 2738877-91-1
  • MF: C23H18F5N3O4
  • MW: 495.40
  • Catalog: Phospholipase
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

D609

D609 is a selective competitive inhibitor of phosphatidyl choline-specific phospholipase C (PC-PLC), with Ki of 6.4 μM.

  • CAS Number: 83373-60-8
  • MF: C11H15KOS2
  • MW: 266.465
  • Catalog: Phospholipase
  • Density: 1.24 g/cm3
  • Boiling Point: 303.8ºC at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 137.5ºC

Levobupivacaine hydrochloride

Levobupivacaine Hcl is a local anaesthetic compound belonging to the amino amide group; long-acting local anesthetic.

  • CAS Number: 27262-48-2
  • MF: C18H29ClN2O
  • MW: 324.889
  • Catalog: Autophagy
  • Density: N/A
  • Boiling Point: 423.4ºC at 760 mmHg
  • Melting Point: 254 °C (dec.)(lit.)
  • Flash Point: 209.9ºC

Arachidonyl trifluoromethyl ketone

AACOCF3 (Arachidonyl trifluoromethyl ketone) is a cell-permeant trifluoromethyl ketone analog of arachidonic acid. AACOCF3 is a potent and selective slow binding inhibitor of the 85-kDa cytosolic phospholipase A2 (cPLA2). AACOCF3 blocks production of arachidonate and 12-hydroxyeicosatetraenoic acid by calcium ionophore-challenged platelets. AACOCF3 inhibits glucose-induced insulin secretion from isolated rat islets. AACOCF3 has the potential for the research of cardiovascular disease[1][2][3].

  • CAS Number: 149301-79-1
  • MF: C21H31F3O
  • MW: 356.465
  • Catalog: Phospholipase
  • Density: 1.0±0.1 g/cm3
  • Boiling Point: 421.7±45.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 288.7±20.2 °C

FKGK18

FKGK18 (FKGK18) is a potent, selective inhibitor of iPLA2 (group VIA Ca2+-independent phospholipase A2) with IC50 of 50 nM; displays 195 and >455 times more potent for GVIA iPLA(2) than for GIVA cPLA(2) and GV sPLA(2); inhibits Ca2+-independent PLA2 activity in a concentration-dependent manner, similar to S-BEL, which preferentially inhibits cytosol-associated iPLA2β; FKGK18 a valuable tool to explore the role of GVIA iPLA(2) in cells and in vivo models.

  • CAS Number: 1071001-09-6
  • MF: C16H15F3O
  • MW: 280.285
  • Catalog: Apoptosis
  • Density: 1.2±0.1 g/cm3
  • Boiling Point: 382.5±42.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 202.8±19.4 °C

N-(p-amylcinnamoyl) Anthranilic Acid

N-(p-amylcinnamoyl) Anthranilic Acid (ACA) is a broad spectrum Phospholipase A2 (PLA2) inhibitor and TRP channel blocker[1][2]. N-(p-amylcinnamoyl) Anthranilic Acid (ACA) is also an effective reversible inhibitor of calcium-activated chloride channels, has potential to treat arrhythmia[3].

  • CAS Number: 110683-10-8
  • MF: C21H23NO3
  • MW: 337.41
  • Catalog: TRP Channel
  • Density: 1.2±0.1 g/cm3
  • Boiling Point: 563.1±50.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 294.4±30.1 °C

D,L-erythro-Dihydrosphingosine

DL-erythro-Dihydrosphingosine is a potent inhibitor of PKC and phospholipase A2 (PLA2)[1][2].

  • CAS Number: 3102-56-5
  • MF: C18H39NO2
  • MW: 301.50800
  • Catalog: PKC
  • Density: 0.927g/cm3
  • Boiling Point: 446.2ºC at 760 mmHg
  • Melting Point: 70-72ºC
  • Flash Point: 223.7ºC

LY 178002

LY 178002 is a potent inhibitor of 5-lipoxygenase, phospholipase A2, with IC50 of 0.6 μM for 5-1ipoxygenase, inhibits cellular production of LTB4 by human polymorphonuclear leukocytes, and shows relatively weak inhibition on cyclooxygenase.

  • CAS Number: 107889-32-7
  • MF: C18H25NO2S
  • MW: 319.46200
  • Catalog: 5-Lipoxygenase
  • Density: 1.139g/cm3
  • Boiling Point: 489.9ºC at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 250.1ºC

AA26-9

AA26-9 is a potent and broad spectrum serine hydrolase inhibitor.

  • CAS Number: 1312782-34-5
  • MF: C7H10N4O
  • MW: 166.180
  • Catalog: Phospholipase
  • Density: 1.4±0.1 g/cm3
  • Boiling Point: 306.7±25.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 139.3±23.2 °C