Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T4694 |
AG-1557 hydrochloride (189290-58-2(free base))
|
EGFR; HER | Angiogenesis; JAK/STAT signaling; Tyrosine Kinase/Adaptors |
AG-1557 hydrochloride (189290-58-2(free base)) 是一种表皮生长因子受体 (EGFR) 酪氨酸激酶抑制剂 (pIC50: 8.194)。 | |||
T7493 |
AG-13958
AG-013958,N-[2-氟-5-[[3-[(1E)-2-(2-吡啶基)乙烯基]-1H-吲唑-6-基]氨基]苯基]-1,3-二甲基-1H-吡唑-5-甲酰胺 |
VEGFR | Angiogenesis; Tyrosine Kinase/Adaptors |
AG-13958 (AG-013958) 是 VEGFR 酪氨酸激酶抑制剂,可用于年龄相关性黄斑变性 (AMD) 的脉络膜新生血管形成的研究。 | |||
T6266 |
PP2
AGL 1879,AG 1879,AGL 1879 |
EGFR; Tyrosine Kinases; JAK; Src | Angiogenesis; Chromatin/Epigenetic; JAK/STAT signaling; Stem Cells; Tyrosine Kinase/Adaptors |
PP2 (AG 1879,AGL 1879) 是 Lck/Fyn 抑制剂 (IC50:4/5 nM),对 EGFR 的效力降低约 100 倍,对 ZAP-70、PKA 和 JAK2 无活性。 | |||
T1088 |
Repaglinide
AG-EE 388 ZW,AG-EE 623ZW,瑞格列奈 |
Potassium Channel; PPAR | DNA Damage/DNA Repair; Membrane transporter/Ion channel; Metabolism |
Repaglinide (AG-EE 623ZW) 是一种能够用于2 型糖尿病的胰岛素促分泌剂。 | |||
T13238 |
Tyrphostin AG1433
SU1433,AG1433 |
VEGFR; PDGFR | Angiogenesis; Tyrosine Kinase/Adaptors |
Tyrphostin AG1433 (AG1433) 是选择性的PDGFRβ和VEGFR-2 (Flk-1/KDR)抑制剂,IC50分别为 5.0 μM 和 9.3 μM。Tyrphostin AG1433有防止血管形成的活性。 | |||
T22253 |
AG-120 (racemic)
1-(4-氰基-2-吡啶基)-5-氧代-L-脯氨酰-2-(2-氯苯基)-N-(3,3-二氟环丁基)-N2-(5-氟-3-吡啶基)甘氨酰胺 |
Dehydrogenase | Metabolism |
AG-120 (racemic) 是 AG-120 的外消旋混合物,是一种可口服的异柠檬酸脱氢酶 1 型 (IDH1) 抑制剂,具有潜在的抗肿瘤活性。 | |||
T4052 |
KML29
|
Lipase | Metabolism |
KML29 是一种口服具有活性的、高度选择性的不可逆 MAGL 抑制剂,其对小鼠、大鼠和人的 IC50值分别为15 nM、43 nM 和 5.9 nM。它对 FAAH 在内的其他中心和外周丝氨酸水解酶的交叉反应极小。 | |||
T29372 |
2-Pyridineacetamide, 5-ethylthio-
AG-41,AG 41,AG41 |
||
2-Pyridineacetamide, 5-ethylthio- is a biochemical. | |||
T29373 |
2-Pyridineacetamide, 5-methylthio-
AG 42,AG-42 AG42 |
||
2-Pyridineacetamide, 5-methylthio- is a biochemical. | |||
T22456 |
Voreloxin hydrochloride
SNS-595 hydrochloride,Vosaroxin,(3S-反式)-1,4-二氢-7-[3-甲氧基-4-(甲基氨基)-1-吡咯烷基]-4-氧代-1-(2-噻唑基)-1,8-萘啶-3-羧酸单盐酸盐 |
Apoptosis; Topoisomerase | Apoptosis; DNA Damage/DNA Repair |
Voreloxin hydrochloride (SNS-595 hydrochloride) 是一种新型拓扑异构酶 II 抑制剂,能够诱导 DNA 双链断裂,阻滞 G2 期,引起细胞凋亡。 | |||
T4554 |
AG 1406
|
VEGFR | Angiogenesis; Tyrosine Kinase/Adaptors |
AG 1406 是受体酪氨酸激酶 VEGF 受体 2 的选择性抑制剂。 | |||
T1452 |
Axitinib
AG-013736,阿昔替尼,阿西替尼 |
VEGFR; PDGFR; c-Kit | Angiogenesis; Tyrosine Kinase/Adaptors |
Axitinib (AG-013736) 是一种多靶点酪氨酸激酶抑制剂,能够抑制 VEGFR1 (IC50:4 nM),VEGFR2 (IC50:20 nM),VEGFR3 (IC50:0.4 nM),PDGFRβ (IC50:2 nM)。 | |||
T11724 |
JNJ-42226314
|
Lipase | Metabolism |
JNJ-42226314 是一种具有高选择性的非共价单酰基甘油脂肪酶 (MAGL) 抑制剂,具有抗伤害作用。JNJ-42226314 通过内源性大麻素-2-丙烯酰甘油(2-AG)在神经病理性疼痛和炎症性疼痛模型中显示出疗效。 | |||
T2346 |
Enasidenib
恩西地平,AG-221 |
Dehydrogenase; Isocitrate Dehydrogenase (IDH) | Metabolism |
Enasidenib (AG-221) 是口服具有活力的、可逆的、选择性IDH2突变酶抑制剂,抑制IDH2R140Q 和 IDH2R172K 的IC50分别为100 和 400 nM。 | |||
T14137 |
AG 1295
|
PDGFR | Angiogenesis; Tyrosine Kinase/Adaptors |
AG 1295 是选择性血小板衍生生长因子受体酪氨酸激酶抑制剂。它能抑制 PDGFR 的自磷酸化,对 EGF 受体的自磷酸化无影响。 | |||
T4205 |
AG-494
Tyrphostin AG-494,AG 494,Tyrphostin B48 |
EGFR; CDK | Angiogenesis; Cell Cycle/Checkpoint; JAK/STAT signaling; Tyrosine Kinase/Adaptors |
AG-494 (Tyrphostin B48) 是一种高效、选择性的 EGFR 酪氨酸激酶抑制剂,IC50为0.7 μM。它阻断 Cdk2 的激活并抑制 EGF 依赖的 DNA 合成。它抑制 EGFR、ErbB2、HER1-2 和 PDGF-R 的自磷酸化,IC50为 1.1、39、45 和 6 μM。 | |||
T3617 |
Ivosidenib
艾伏尼布,AG-120 |
Dehydrogenase; Isocitrate Dehydrogenase (IDH) | Metabolism |
Ivosidenib (AG-120) 是一种口服具有活力的异柠檬酸脱氢酶 1 的突变体酶 (mIDH1 enzyme) 抑制剂,能够使 d-2- hydroxyglutatrate (2-HG) 在体内降低。它具有良好的的安全性和临床活性,具有研究 AML 的潜力。 | |||
T4092 |
AG126
Tyrphostin AG126,AG 126 |
ERK; COX | Immunology/Inflammation; MAPK; Neuroscience |
AG126 (Tyrphostin AG126) 是一种酪氨酸激酶抑制剂,可阻止丝裂原活化蛋白激酶 p42MAPK(ERK2) 的激活。 | |||
T6554 |
JZL 184
JZL184 |
Lipase | Metabolism |
JZL 184 是不可逆的、选择性的MAGL 抑制剂,对MAGL 的选择性比 FAAH 高 300 倍以上。它可阻断脑膜中的 2-花生四烯酸甘油酯 (2-AG) 的水解 (IC50为 8 nM)。 | |||
T5815 |
MJN110
Cravatt Reagent |
Lipase | Metabolism |
MJN110 (Cravatt Reagent) 是选择性的、口服具有活性的单酰基甘油脂肪酶 (MAGL) 抑制剂,对 hMAGL 和 2-花生四烯酸甘油酯 (2-AG) 的IC50分别为 9.1 nM 和 2.1 nM。它具有阿片类药物保护作用,具有显著的抗痛觉过敏活性。 | |||
T27811 |
LEI-106
|
||
LEI-106, a novel potent sn-1 DAGLalpha inhibitor, blocks the hydrolysis of sn-1-oleoyl-2-AG, inhibits the hydrolysis of 2-AG by the monoacylglycerol lipase ABHD6. | |||
T34521 |
SAR629
SAR 629,SAR-629 |
||
SAR-629 is an MGL inhibitor or 2-AG degradation inhibitor. | |||
T28235 |
OMDM169
OMDM 169,OMDM-169 |
||
OMDM169 is a potent and selective MAGL inhibitor. OMDM169 could enhances 2-AG levels and of exerts analgesic activity via indirect activation of cannabinoid receptors. OMDM169 exhibited 0.13 microM<IC(50)<0.41 microM towards 2-AG hydrolysing activities in | |||
T68451 |
AG-28262 besylate
|
||
AG-28262 besylate is a VEGFR-2 Inhibitorwhich may affect alanine aminotransferase gene expression and enzymatic activity in the liver. | |||
T11070L | DO34 | Others | Others |
DO34 is a highly potent and centrally active inhibitor of diacylglycerol lipase (IC50: 6 nM for DAGLα conversion of SAG to 2-AG). | |||
T38115 |
Fluprostenol serinol amide
|
||
2-arachidonyl glycerol (2-AG) exhibits cannabinoid (CB) agonist activity at the CB1 receptor, is an important endogenous monoglyceride species, and is thus considered to be the natural ligand for the CB1 receptor. 2-AG can also be metabolized by cyclooxygenase-2 and specific prostaglandin H2 (PGH2) isomerases to form PG 2-glyceryl esters. Fluprostenol serinol amide (Flu-SA) is a stable analog of PGF2α 2-glyceryl ester that has much greater stability. The biological activity of Flu-SA has not yet... | |||
T37629 |
IDFP
|
||
The endocannabinoids, 2-arachidonoyl glycerol (2-AG) and arachidonoyl ethanolamide (AEA), are biologically active lipids that regulate diverse neurological and metabolic functions by activating the cannabinoid receptors, central cannabinoid (CB1) and peripheral cannabinoid (CB2). Monoacylglycerol lipase (MAGL) and fatty acid amide hydrolase (FAAH) hydrolyze 2-AG and AEA, respectively, thus terminating their biological function. IDFP is an organophosphorus compound that dually inhibits MAGL and F... | |||
T35786 |
O-7460
|
||
In humans, two forms of diacylglycerol lipase, DAGLα and DAGLβ, generate the endocannabinoid 2-arachidonoyl glycerol by attacking DAG at the sn-1 position. O-7460 is a selective inhibitor of 2-AG biosynthesis via DAGLα (IC50 = 690 nM). It demonstrates much weaker inhibition towards human monoacylglycerol lipase and rat brain fatty acid amide hydrolase (IC50s > 10 μM) and does not bind to CB1 or CB2 cannabinoid receptors (Kis > 10 μM). At 0-12 mg/kg, i.p. in mice, O-7460 was reported to dose-depe... | |||
T37374 |
URB754
|
||
URB754 is a potent and noncompetitive inhibitor of monoacylglycerol lipase (MAGL), exhibiting an IC50 value of 200 nM for the recombinant rat brain enzyme. However, it does not inhibit human recombinant, rat brain, or mouse brain MAGL at concentrations up to 100 μM. There is evidence that the MAGL inhibitory activity of URB754 may be attributed to the impurity bis(methylthio)mercurane (IC50 = 11.9 nM for rat recombinant MAGL) that is found in commercial preparations. URB754 inhibits rat brain fa... | |||
T75834 |
Antagonist G TFA
|
||
Antagonist G TFA 作为后叶加压素(vasopressin)的有效拮抗剂,同时对GRP和缓激肽具有弱拮抗作用。此外,Antagonist G 能够诱导AG-1转录,增强癌细胞对化疗的敏感性。 | |||
T70882 |
Orlistat-d3
|
||
Orlistat-d3 is intended for use as an internal standard for the quantification of orlistat by GC- or LC-MS. Orlistat is a digestive lipase inhibitor. It inhibits diacylglycerol lipase α (DAGLα), DAGLβ, α/β-hydrolase domain-containing protein 12 (ABHD12), ABHD16A, and platelet-activating factor acetylhydrolase (PAF-AH; IC50s = 0.06, 0.1, 0.08, 0.03, and 0.05 µM, respectively), as well as pancreatic lipase and hormone-sensitive lipase (IC50s = 0.65 and 2.1 µg/ml, respectively) but does not inhibit... |