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LP-935509 is an orally active, potent, selective, ATP-competitive and brain-penetrant inhibitor of adaptor protein-2 associated kinase 1 (AAK1) with an IC50 of 3.3 nM and a Ki of 0.9 nM, respectively. LP-935509 is also a potent inhibitor of BIKE (IC50=14 nM) and a modest inhibitor of GAK (IC50=320 nM). LP-935509 shows antinociceptive activity. LP-935509 can be used for neuropathic pain and SARS-CoV-2 research .
LP-184 (compound 6), an acylfulvene analog, inhibits tumor growth. LP-184 has potent anti-cancer activity in the ovarian, colon, prostate and pancreatic cell lines. (patent WO2007019308A2).
LP-284 is a potent DNA alkylating agent that kills solid tumours. LP-284 can be used in the studies of hematologic cancers with compromised DNA repair, such as mantle cell lymphoma (MCL) .
LP-922056 is an orally active, highly potent Notum Pectinacetylesterase inhibitor with EC50s of 21 nM, 55 nM in human and mouse cellular assay, respectively. LP-922056 significantly increases midshaft femur cortical bone thickness in mice and rats .
LP-922761 is a potent, selective and orally active adapter protein-2 associated kinase 1 (AAK1) inhibitor with IC50s of 4.8 nM and 7.6 nM in enzyme and cell assays, respectively. LP-922761 also inhibits BMP-2-inducible protein kinase (BIKE) with an IC50 of 24 nM. LP-922761 exhibits no significant activity at cyclin G-associated kinase (GAK), opioid, adrenergic α2 or GABAa receptors .
LP-922761 hydrate is a potent, selective and orally active adapter protein-2 associated kinase 1 (AAK1) inhibitor with IC50s of 4.8 nM and 7.6 nM in enzyme and cell assays, respectively. LP-922761 hydrate also inhibits BMP-2-inducible protein kinase (BIKE) with an IC50 of 24 nM. LP-922761 hydrate shows less activity at cyclin G-associated kinase (GAK), opioid, adrenergic α2 or GABAa receptors .
LP-261 is a potent and orally active anti-mitotic agent and shows an inhibition of in vitro tubulin polymerization with an EC50 of 3.2 μM . LP-261 inhibits growth of a human non-small-cell lung tumor (NCI-H522) in vivo and can be used for cancer research .
LP44 (hydrochloride) is a selective 5-HT7 agonist with Ki of 0.22 nM. LP44 (hydrochloride) induces hypothermic effect in a dose-dependent manner by intracerebroventricular injection. LP44 (hydrochloride) not causes considerable hypothermic response by intraperitoneal administration .
LP99, an epigenetic probe, is a potent and selective inhibitor of the BRD7 and BRD9 bromodomains with a Kd of 99 nM against BRD9. LP99 disrupts the binding of BRD7 and BRD9 to chromatin in cells .
Lp-PLA2-IN-17 (Compound 39) is an inhibitor of Lp-PLA2. Lp-PLA2-IN-17 can be used to study disorders involving the hydrolysis of oxidized lipids into two inflammatory substances with the participation of Lp-PLA2 .
LP 12 hydrochloride hydrate is a potent and selective 5-HT7 receptor agonist with a Ki of 0.13 nM. LP 12 hydrochloride hydrate displays selectivity for 5-HT7 over D2, 5-HT1A and 5-HT2A receptors (Ki values are 224 nM, 60.9 nM and >1000 nM, respectively) .
LP 12 hydrochloride (compound 21) is a potent and selective 5-HT7 receptor agonist with a Ki of 0.13 nM. LP 12 hydrochloride displays selectivity for 5-HT7 over D2, 5-HT1A and 5-HT2A receptors (Ki values are 224 nM, 60.9 nM and >1000 nM, respectively) .
Lp-PLA2-IN-2 is a potent and selective lipoprotein-associated phospholipase A2 (Lp-PLA2) inhibitor, with an IC50 0f 120 nM for recombinant human Lp-PLA2 .
LP-211 is a selective and blood−brain barrier penetrant 5-HT7 receptor agonist, with a Ki of 0.58 nM, with high selectivity over 5-HT1A receptor (Ki, 188 nM) and D2 receptor (Ki, 142 nM).
Lp-PLA2-IN-1 is a potent Lipoprotein-associated phospholipase A2 (Lp-PLA2) inhibitor. Lp-PLA2-IN-1 has the potential for atherosclerosis, Alzheimer's disease research .
Lp-PLA2-IN-3 is a potent and orally bioavailable lipoprotein-associated phospholipase A2 (Lp-PLA2) inhibitor, with an IC50 of 14 nM for recombinant human Lp-PLA2 (rhLpPLA2) .
LP23 is a non-arylmethylamine PD-1/PD-L1 inhibitor (IC50: 16.7 nM) with anti-tumor activity. LP23 restores immune cell function in HepG2/Jurkat T cells and promotes HepG2 cell death. LP23 is active in vivo in the B16-F10 tumor model (TGI=88.6% at 30 mg/kg) .
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) .
Lp-PLA2-IN-5 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-5 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 32) .
Lp-PLA2-IN-11 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-11 has the potential for the research of diseases associated with the activity of Lp-PLA2, for example atherosclerosis, Alzheimer's disease (extracted from patent WO2014114249A1, compound E145) .
Lp-PLA2-IN-6 (compound 18), a tetracyclic pyrimidinone compound, is a potent Lp-PLA2 inhibitor with a pIC50 of 10.0 for rhLp-PLA2. Lp-PLA2-IN-6 has the potential for neurodegenerative related diseases research .
Lp-PLA2-IN-9 (compound 17), a tetracyclic pyrimidinone compound, is a potent Lp-PLA2 inhibitor with a pIC50 of 10.1 for rhLp-PLA2. Lp-PLA2-IN-9 has the potential for neurodegenerative related diseases research .
Lp-PLA2-IN-12 (compound 19) is an Lp-PLA2 inhibitor. Lp-PLA2-IN-12 can be used for the study of neurodegenerative related diseases such as Alzheimer's disease (AD), glaucoma, age-related macular degeneration (AMD), or cardiovascular disease including atherosclerosis .
Lp-PLA2-IN-16 (example 1) is a lipoprotein-associated phospholipase A2 (Lp-PLA 2) inhibitor, which can be used in the research of Alzheimer's disease, etc .
Lp-PLA2-IN-15 (example 2) is a lipoprotein-associated phospholipase A2 (Lp-PLA 2) inhibitor, which can be used in the research of Alzheimer's disease, etc .
Lp-PLA2-IN-14 (Compound 19) is an Lp-PLA2 inhibitor with a pIC50 of 8.4 against rhLp-PLA2. Lp-PLA2-IN-14 can be used for the research of neurodegenerative related diseases, such as Alzheimer Disease (AD), glaucoma, age-related macular degeneration (AMD) or cardiovascular diseases including atherosclerosis and the like .
Lp-PLA2-IN-10 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-10 has the potential for the research of neurodegenerative-related diseases such as Alzheimer's disease (AD), glaucoma, age-related macular degeneration (AMD), or cardiovascular diseases including atherosclerosis (extracted from patent WO2022001881A1, compound 4) .
(2S,3R)-LP99 is a potent and selective BRD7 and BRD9 inhibitor with an KD of 99 nM for BRD9. (2S,3R)-LP99 inhibits the association of BRD7 and BRD9 to acetylated histones in vitro and in cells. (2S,3R)-LP99 demonstrates that BRD7/9 plays a role in regulating pro-inflammatory cytokine secretion .
Povorcitinib (INCB54707) is a potent and selective JAK1 inhibitor that effectively reduces abscesses and inflammatory nodules. Povorcitinib is used to study cutaneous lupus erythematosus (CLE) and lichen planus (LP) (information extracted from patent WO2021076124A1).
Pep19-2.5 is an synthetic and antitoxin peptide, blocks the intracellular endotoxin signaling cascade. Pep19-2.5 inhibits signaling of lipopeptides (LP) and lipopolysaccharides (LPS) mediated by transmembrane and cytosolic pattern recognition receptors (PRRs). The signaling cascades lead to inflammation and cell pyroptosis .
GSK2647544 is an orally available, selective inhibitor of Lp-PLA2. Lipoprotein-associated phospholipase (Lp-PLA2) is a calcium-independent phospholipase A2 with proinflammatory activities that is primarily secreted by monocyte-derived macrophages .
OH-C-Chol is a cationic liposome that serves as a siRNA delivery vehicle. OH-C-Chol (LP-C) and OH-NC-Chol (LP-NC)/siRNA complexes (lipoplexes) showed better performance than NP-C and NP-NC/siRNA complexes (nanocomplexes), respectively. ) greater gene silencing effect .
Crovalimab (SKY59; RO7112689) is a novel humanized antibody against C5 in a pH-dependent manner with KDs of 15.2 nM and 16.8 μM at pH 7.4 and 5.8, respectively. Crovalimab binds human FcRn with great affinity (KD: 17 μM at pH 6.0). Crovalimab can block cleavage of C5 by the C5 convertase and inhibite the activity of a C5 variant (p.Arg885His). Crovalimab inhibits C5b-9 formation significantly in all three complement pathways, the classical pathway (CP), lectin pathway (LP), and alternative pathway (AP). Crovalimab has the potential for paroxysmal nocturnal hemoglobinuria (PNH) and complement-mediated diseases research .
Rilapladib (SB 659032) is a selective Lp-PLA2 (lipoprotein-associated phospholipase A2) inhibitor with an IC50 of 230 pM . Rilapladib (SB 659032) is also a PAFR (Platelet Activating Factor Receptor) antagonist .
Povorcitinib (INCB54707) phosphate is a potent and selective JAK1 inhibitor that effectively reduces abscesses and inflammatory nodules. Povorcitinib phosphate can be used to study cutaneous lupus erythematosus (CLE) and lichen planus (LP) (information extracted from patent WO2021076124A1).
Darapladib (SB-480848) is an orally active, selective and reversible Lp-PLA2 inhibitor (IC50=0.25 nM). Darapladib can trigger irreversible actions on glioma cell apoptosis and induce cycle arrest. Darapladib can be used in the study of atherosclerosis and cancer .
PROTAC ERα Degrader-5 (compound LP2) consists an ADC linker and a PROTAC, whcih can be conjugated to an antibody to form PACs. PROTAC ERα Degrader-5 conjugated to an antibody is a more marked estrogen receptor-alpha (ERα) degrader compared to PROTAC (without Ab) .
PROTAC ER Degrader-3 is an intermediate for synthesis of PAC. PAC, consists the ADCs linker and PROTACs, conjugated to an antibody. PAC extracts from patent WO2017201449A1, compound LP2. PAC conjugated to an antibody is a more marked estrogen receptor-alpha (ERα) degrader compared to PROTAC (without Ab) .
PROTAC ER Degrader-2 is an intermediate for synthesis of PAC. PAC, consists the ADCs linker and PROTACs, conjugated to an antibody. PAC extracts from patent WO2017201449A1, compound LP2. PAC conjugated to an antibody is a more marked estrogen receptor-alpha (ERα) degrader compared to PROTAC (without Ab) .
DIBAC-GGFG-NH2CH2-Dxd (compound LP4), a Camptothecin (HY-16560) derivative, is a linker-payload of protein-agent conjugates . Dxd (HY-13631D) can be used as a payload for the antibody-coupling drug ADC (DS-8201a).DIBAC-GGFG-NH2CH2-Dxd is a click chemistry reagent, it contains a DBCO group that can undergo strain-promoted alkyne-azide cycloaddition (SPAAC) with molecules containing Azide groups.
Pomalidomide-NH-PEG6-amide-C2-CPI-1612 (compound 22 (dCE-1)) is a CBP/EP300 degrader, which contains a CRBN ligands Pomalidomide, a 24-atom linker with 6 PEG units and a HAT inhibitor CPI-1612. Pomalidomide-NH-PEG6-amide-C2-CPI-1612 exhibits antiproliferative effects in cells multiple myeloma cells LP1 (with a DC50 of 1.2 μM), MM1S and various cancer cell lines, especially the leukemia cells .
Pep19-2.5 is an synthetic and antitoxin peptide, blocks the intracellular endotoxin signaling cascade. Pep19-2.5 inhibits signaling of lipopeptides (LP) and lipopolysaccharides (LPS) mediated by transmembrane and cytosolic pattern recognition receptors (PRRs). The signaling cascades lead to inflammation and cell pyroptosis .
TDSRCVIGLYHPPLQVY TFA is a disordered control peptide. TDSRCVIGLYHPPLQVY TFA is a peptide containing the same amino acids as LP17 (HY-P3400) but in a different sequence order .
LQVTDSGLYRCVIYHPP (LP17) is a triggering receptor expressed on myeloid cells (TREM-1) inhibitory peptide. LQVTDSGLYRCVIYHPP substantially alleviates ischemia-induced infarction and neuronal injury. LQVTDSGLYRCVIYHPP can get access into brain and block TREM-1 .
LQVTDSGLYRCVIYHPP (LP17) TFA is a triggering receptor expressed on myeloid cells (TREM-1) inhibitory peptide. LQVTDSGLYRCVIYHPP TFA substantially alleviates ischemia-induced infarction and neuronal injury. LQVTDSGLYRCVIYHPP TFA can get access into brain and block TREM-1 .
TDSRCVIGLYHPPLQVY is a disordered control peptide. TDSRCVIGLYHPPLQVY is a peptide containing the same amino acids as LP17 (HY-P3400) but in a different sequence order .
Crovalimab (SKY59; RO7112689) is a novel humanized antibody against C5 in a pH-dependent manner with KDs of 15.2 nM and 16.8 μM at pH 7.4 and 5.8, respectively. Crovalimab binds human FcRn with great affinity (KD: 17 μM at pH 6.0). Crovalimab can block cleavage of C5 by the C5 convertase and inhibite the activity of a C5 variant (p.Arg885His). Crovalimab inhibits C5b-9 formation significantly in all three complement pathways, the classical pathway (CP), lectin pathway (LP), and alternative pathway (AP). Crovalimab has the potential for paroxysmal nocturnal hemoglobinuria (PNH) and complement-mediated diseases research .
IL-7 Protein, Mouse (CHO) is constitutively produced by stromal cells from the bone marrow and thymus, plays a crucial role in B cell lymphopoiesis and in T cell homeostasis.
AMSHLP is a zinc metalloprotease that selectively cleaves "Lys-63" linked polyubiquitin chains and acts as a positive regulator of the TORC1 signaling pathway. It specifically deubiquitinates SESN2, disrupts its interaction with the GATOR2 complex and inhibits SESN2-mediated regulation of TORC1. LP Protein, Human is the recombinant human-derived LP protein, expressed by E. coli , with tag free. The total length of LP Protein, Human is 435 a.a., .
The PLA2G7 protein is a lipoprotein-associated calcium-independent phospholipase A2 that plays a key role in phospholipid catabolism during inflammation and oxidative stress responses. It acts at the lipid-water interface and hydrolyzes the ester bond of the fatty acyl group at the sn-2 position, with particular preference for short-chain fatty acyl groups. PLA2G7 Protein, Mouse (Baculovirus, N-His, C-Myc) is the recombinant mouse-derived PLA2G7 protein, expressed by Sf9 insect cells , with C-Myc, N-10*His labeled tag. The total length of PLA2G7 Protein, Mouse (Baculovirus, N-His, C-Myc) is 419 a.a., with molecular weight of 50.7 kDa.
The PLA2G7 protein is a lipoprotein-associated calcium-independent phospholipase A2 that plays a key role in phospholipid catabolism during inflammation and oxidative stress responses. It acts at the lipid-water interface and hydrolyzes the ester bond of the fatty acyl group at the sn-2 position, with particular preference for short-chain fatty acyl groups. PLA2G7 Protein, Mouse (HEK293, N-His, C-Myc) is the recombinant mouse-derived PLA2G7 protein, expressed by HEK293 , with C-Myc, N-10*His labeled tag. The total length of PLA2G7 Protein, Mouse (HEK293, N-His, C-Myc) is 419 a.a., with molecular weight of 51.9 kDa.
DIBAC-GGFG-NH2CH2-Dxd (compound LP4), a Camptothecin (HY-16560) derivative, is a linker-payload of protein-agent conjugates . Dxd (HY-13631D) can be used as a payload for the antibody-coupling drug ADC (DS-8201a).DIBAC-GGFG-NH2CH2-Dxd is a click chemistry reagent, it contains a DBCO group that can undergo strain-promoted alkyne-azide cycloaddition (SPAAC) with molecules containing Azide groups.
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