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Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T81181 |
sEH/FLAP-IN-1
|
FLAP | Immunology/Inflammation |
sEH/FLAP-IN-1(Compound 46A)是一sEH/FLAP抑制剂,具有阻断SACM刺激PBMC中5-LOX产物形成的活性(EC50: 11 nM),并能抑制sEH活性(EC50: 18 nM)及血栓素产生。该化合物适用于炎症性疾病研究领域。 | |||
T8844 |
Diflapolin
|
Others; FLAP; Epoxide Hydrolase | Immunology/Inflammation; Metabolism; Others |
Diflapolin 是高活性的双 5-脂氧合酶激活蛋白(FLAP)/可溶性环氧化物水解酶抑制剂,具有显著的抗炎作用和较高的靶向选择性。它抑制分离的 sEH 的活性,IC50为20 nM。它还抑制完整人单核细胞和中性粒细胞中 5-LOX 产物的形成,IC50分别为 30 和 170 nM。 | |||
T16087 |
Quiflapon
喹夫拉朋,MK-591 |
Apoptosis; FLAP | Apoptosis; Immunology/Inflammation |
Quiflapon (MK-591) 是一种选择性和特异性的FLAP 抑制剂,可诱导细胞凋亡。它也是口服白三烯生物合成抑制剂,在完整的人和诱导的大鼠多形核白细胞 PMNLs 中,其IC50值分别为 3.1 nM 和 6.1 nM。 | |||
T9023 |
Atuliflapon
AZD5718 |
FLAP | Immunology/Inflammation |
Atuliflapon (AZD5718) 是可口服的FLAP(5 -脂氧合酶激活蛋白)的抑制剂,IC50值为 2 nM,可用于冠状动脉疾病的研究。 | |||
T8545 |
FEN1-IN-4
FEN1 Inhibitor C2 |
Others | Others |
FEN1-IN-4 (FEN1 Inhibitor C2) 是人类皮瓣内切核酸酶-1 (hFEN1) 抑制剂。 | |||
T6893 |
MK-886
MK886,L 663536 |
Apoptosis; Leukotriene Receptor; COX; PPAR; FLAP | Apoptosis; DNA Damage/DNA Repair; GPCR/G Protein; Immunology/Inflammation; Metabolism; Neuroscience |
MK-886 (L 663536)是一种细胞可渗透的,具有口服活性的 FLAP (IC50为 30 nM) 和白三烯生物合成 (完整白细胞和人全血中的IC50分别为 3 nM 和 1.1μM) 的抑制剂。它也是一种非竞争性PPARα拮抗剂,可以诱导细胞凋亡。 | |||
T11487 |
Fiboflapon
GSK2190915,AM-803 |
FLAP | Immunology/Inflammation |
Fiboflapon (GSK2190915) 是一种可口服且具有有效性 5-脂氧合酶激活蛋白 (FLAP) 抑制剂,结合 FLAP 的效价为 2.9 nM,对人血中 LTB4 有抑制作用, IC50 值为 76 nM。 | |||
T11487L |
Fiboflapon sodium
GSK2190915 sodium salt,AM-803 sodium |
LTR | Immunology/Inflammation |
Fiboflapon sodium (GSK2190915) is an orally bioavailable 5-lipoxygenase-activating protein (FLAP) inhibitor with a potency of 2.9 nM in FLAP binding, an IC50 of 76 nM for inhibition of LTB4 in human blood. | |||
TQ0098 |
Quiflapon sodium
喹夫拉朋钠,MK591 |
FLAP | Immunology/Inflammation |
Quiflapon sodium (MK591) is a selective inhibitor of 5-Lipoxygenase-activating protein (FLAP). | |||
T13295 |
Veliflapon
DG-031,BAY X 1005 |
LTR | Immunology/Inflammation |
Veliflapon is an orally active and selective inhibitor of 5-lipoxygenase activating protein (FLAP). Veliflapon inhibits the synthesis of the leukotrienes B4 and C4. | |||
T77172 | Eflapegrastim | ||
Eflapegrastim 是一种人源化IgG4单抗 ,也是一种粒细胞集落刺激因子 (G-CSF)。Eflapegrastim 靶向G-CSF 受体 (c-Fms)。Eflapegrastim 刺激中性粒细胞祖细胞的增殖和分化,维持成熟和功能性中性粒细胞数目稳定。Eflapegrastim 还缩短中性粒细胞减少的持续时间。 | |||
T10314 |
AM103
AM 103 |
FLAP | Immunology/Inflammation |
AM103 是一种有效的特异性 FLAP 抑制剂 (IC50 = 4.2 nM)。 | |||
T9147 |
FEN1-IN-3
|
||
FEN1-IN-3 是一种人类皮瓣内切核酸酶-1 (hFEN1) 抑制剂,可使 hFEN1 稳定化,EC50为 6.8 μM。 | |||
T15274 |
FEN1-IN-1
LNT-1 |
Others | Others |
FEN1-IN-1 (LNT-1) 是一种FEN1的抑制剂,可绑定 FEN1 的活性位点,也可通过协调 Mg2+,进而表现出部分抑制作用。 | |||
T12793 |
(S)-BI 665915
|
Others | Others |
(S)-BI 665915 is an orally active inhibitor of oxadiazole-containing 5-lipoxygenase-activating protein (FLAP)(IC50 of 1.7 nM for FLAP binding).. | |||
T68449 |
JFD00950
|
||
JFD00950 is a human flap endonuclease 1 (FEN1) inhibitor with in vitro inhibition of flap cleavage activity as well as cytotoxic activity against a colon cancer cell line, DLD-1. | |||
T14205 |
AM679
|
Others | Others |
AM679 is a potent and selective FLAP inhibitor with IC50s of 2.2 nM/0.6 nM/154 nM for FLAP binding/hLA/hWB respectively. IC50 value: 2.2 nM/0.6 nM/154 nM(FLAP binding/hLA/hWB) [1] AM679 showed an improved CYP inhibition profile (IC50 3A4 = 16.7 lM, 2C9 = | |||
T69418 |
AM-679
|
||
AM-679 is a 5-lipoxygenase-activating protein (FLAP) inhibitor. | |||
T69128 |
NSC-13755
|
||
NSC-13755 is a human flap endonuclease 1 (FEN1) inhibitor. | |||
T78192 |
FEN1-IN-5
|
FLAP | Immunology/Inflammation |
FEN1-IN-5(化合物12A),一种Flap内切酶1(FEN1,IC50=12 nM)的高效抑制剂,作用于DNA损伤修复过程。 | |||
T79389 |
LTB4-IN-2
|
FLAP | Immunology/Inflammation |
LTB4-IN-2(Compound 6x)是一种选择性的5-脂氧合酶激活蛋白(FLAP)抑制剂,旨在抑制白三烯B4(LTB4)的形成(IC50:1.15 μM),适用于抗炎研究。 | |||
T70316 |
AZD6642
|
||
AZD6642 is a potential and selective 5-Lipoxygenase activating Protein (FLAP) inhibitor. AZD6642 shows high specific potency and low lipophilicity resulting in a selective and metabolically stable profile. Based on initial PK/PD relations a low dose to human was predicted. | |||
T79134 |
FEN1-IN-6
|
FLAP | Immunology/Inflammation |
FEN1-IN-6(化合物9)是一种高效的Flap内切酶1(FEN1,IC50=10 nM)抑制剂,对哺乳动物细胞DNA损伤修复有关键作用。同时,FEN1-IN-6也针对相关酶,如XPG,表现出较强的抑制活性(IC50为23 nM)。 | |||
T69970 |
AZD5718
|
||
AZD5718 is a potent and selective FLAP inhibitor (IC50 = 2.0 nM) for Treatment of Coronary Artery Disease. AZD5718 demonstrated a dose dependent and greater than 90% suppression of leukotriene production over 24 h. Preclinical toxicology studies in rat and dog did not show any serious adverse events of clinical significance. Currently, AZD5718 is evaluated in a phase 2a study for treatment of coronary artery disease. | |||
T40931 | FEN1-IN-2 | Others | Others |
FEN1-IN-2 是一种具有选择性和有效性的瓣内切酶 1 (FEN1) 的抑制剂,抑制 FEN1 和 XPG,具有潜在的抗癌活性,可用于研究DNA损伤修复。 | |||
T37649 |
5(S),12(S)-DiHETE
|
||
5(S),12(S)-DiHETE is a natural bioactive lipid derived from arachidonic acid . It is synthesized by glycogen-induced rabbit peritoneal polymorphonuclear leukocytes (PMNLs) incubated with AA. 5(S),12(S)-DiHETE can be produced by successive oxygenation of AA by 5-lipoxygenase (5-LO) in platelets and 12-LO in leukocytes. It can also be synthesized from 12(S)-HETE by 5-LO, in the presence of 5-LO activating protein (FLAP), activated with calcium ionophore. 5(S),12(S)-DiHETE is an epimer of leukotrie... | |||
T79135 |
FEN1-IN-7
|
FLAP | Immunology/Inflammation |
FEN1-IN-7(化合物16)是一款选择性Flap内切酶1(FEN1,IC50=18 nM)抑制剂,它在哺乳动物细胞的DNA损伤修复过程中发挥作用。此外,FEN1-IN-7对相关内切酶如着色性干皮病G蛋白(XPG,IC50=3.04 μM)也有靶向性。它能提高癌细胞对DNA烷基化剂或甲基化试剂的敏感性。 |
Cat. No. | Product Name | Species | Expression System |
---|---|---|---|
TMPY-01481 |
FLAP Protein, Human, Recombinant (His)
FLAP,arachidonate 5-lipoxygenase-activating protein |
Human | Baculovirus Insect Cells |
Arachidonate 5-Lipoxygenase-Activating Protein (ALOX5AP), also known as FLAP, belongs to the MAPEG family. ALOX5AP/FLAP is an essential partner of 5-LO for this process. The FLAP (ALOX5AP) gene has been linked to risk for myocardial infarction, stroke and restenosis, reigniting pharmaceutical interest in this target. It had been found that ALOX5AP/FLAP is a key enzyme in leukotriene formation, in both human pulmonary microvascular endothelial cells and a transformed human brain endothelial cell ... | |||
TMPH-01344 |
Flap endonuclease 1/FEN-1 Protein, Human, Recombinant (His & Myc)
|
Human | E. coli |
Flap endonuclease 1/FEN-1 Protein, Human, Recombinant (His & Myc) is expressed in E. coli expression system with N-10xHis and C-Myc tag. The predicted molecular weight is 50.0 kDa and the accession number is P39748. | |||
TMPH-02649 |
FAN1 Protein, Mouse, Recombinant (His & Myc)
|
Mouse | E. coli |
Nuclease required for the repair of DNA interstrand cross-links (ICL) recruited at sites of DNA damage by monoubiquitinated FANCD2. Specifically involved in repair of ICL-induced DNA breaks by being required for efficient homologous recombination, probably in the resolution of homologous recombination intermediates. Not involved in DNA double-strand breaks resection. Acts as a 5'-3' exonuclease that anchors at a cut end of DNA and cleaves DNA successively at every third nucleotide, allowing to e... | |||
TMPY-01480 |
LTC4S Protein, Human, Recombinant (His)
LTC4S,MGC33147,leukotriene C4 synthase |
Human | Baculovirus Insect Cells |
Leukotriene C4 synthase, also known as LTC4 synthase, Leukotriene-C(4) synthase, and LTC4S, is a multi-pass membrane protein that belongs to the MAPEG family. LTC4S is detected in the lung, platelets, and the myelogenous leukemia cell line KG-1 (at protein level). LTC4S activity is present in eosinophils, basophils, mast cells, certain phagocytic mononuclear cells, endothelial cells, vascular smooth muscle cells, and platelets. LTC4S is essential for the production of cysteinyl leukotrienes (Cys... |