71
13
Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T72322 |
R 59-022 hydrochloride
DKGI-I hydrochloride,Diacylglycerol kinase inhibitor I hydrochloride,DKGI-I hydrochloride ; Diacylglycerol kinase inhibitor I hydrochloride |
5-HT Receptor; PKC | Chromatin/Epigenetic; Cytoskeletal Signaling; GPCR/G Protein; Neuroscience |
R 59-022 hydrochloride (DKGI-I hydrochloride) 是一种 5-HT Receptor 拮抗剂,可激活蛋白激酶 C (PKC)。R 59-022 hydrochloride 是一种 DGK 抑制剂 (IC50:2.8 µM),可抑制 OAG 磷酸化为 OAPA。R 59-022 增强血小板中凝血酶诱导的甘油二酯的产生,并抑制嗜中性粒细胞中磷脂酸的产生。 | |||
T11037 |
Diacylglycerol acyltransferase inhibitor-1
|
Others | Others |
Diacylglycerol Acyltransferase Inhibitor-1, a diacylglycerol acyltransferase (DGAT1) inhibitor, effectively suppresses the activity of DGAT1. | |||
T16709 |
R 59-022
Diacylglycerol kinase inhibitor I,DKGI-I |
Others | Others |
R 59-022 is a 5-HTR antagonist and activates protein kinase C (PKC). R 59-022 is a diacylglycerol kinase inhibitor (IC50=2.8 μM). R 59-022 potentiates thrombin-induced diacylglycerol production in platelets and inhibits phosphatidic acid production in neu | |||
T13373 |
YM17E
|
Acyltransferase; AChR | Metabolism; Neuroscience |
YM17E 是一种 ACAT 抑制剂,在体外兔肝微粒体中的 IC50 为 44 nM。 | |||
T8236 |
RHC 80267
U-57908 |
Others; Phospholipase; COX; Acyltransferase; AChR | Immunology/Inflammation; Metabolism; Neuroscience; Others |
RHC 80267 (U-57908) 是一种选择性二酰基甘油脂酶(DAGL)抑制剂,对犬血小板的IC50为 4 μM。它抑制COX 活性和磷脂酰胆碱的水解,还抑制胆碱酯酶活性,IC50为 4 μM,增强乙酰胆碱引起的松弛。 | |||
T9711 |
OGT-IN-2
|
Others | Others |
OGT-IN-2 是 OGT 抑制剂,抑制 sOGT 和 ncOGT 的 IC50分别为 30 μM 和 53 μM。它在关节疾病方面有研究的价值,如关节软骨疾病、骨关节炎。 | |||
T12767 |
RP 70676
|
Acyltransferase | Metabolism |
RP 70676 是ACAT 抑制剂,抑制大鼠和兔子中 ACAT 的IC50分别为 25 和 44 nM。 | |||
T15109 |
DGAT1-IN-1
|
Transferase | Metabolism |
DGAT1-IN-1是 DGAT1的高效抑制剂,在 Hep3B 细胞过表达 DGAT1裂解物中,测得IC50低于10nM。 | |||
T8314 |
RP-64477
RP64477 |
Acyltransferase | Metabolism |
RP-64477 是有效的胆固醇酯化酶酰基辅酶 A:胆固醇 O-酰基转移酶 (ACAT) 抑制剂。 | |||
T12425 |
PF-06424439 methanesulfonate
|
Acyltransferase; Transferase | Metabolism |
PF-06424439 methanesulfonate 是一种口服有效咪唑并吡啶二酰基甘油酰基转移酶 2 (DGAT2)选择性抑制剂,IC50是14 nM。PF-06424439 methanesulfonate 具有缓慢可逆,时间依赖性的特点,其相对于酰基-CoA 底物以非竞争性模式抑制 DGAT2。 | |||
T23550 |
YM-750
YM 750 |
Acyltransferase | Metabolism |
YM-750 是一种有效的酰基:胆固醇酰基转移酶(ACAT)抑制剂,IC50为0.18 μM。 | |||
T16409 |
OSMI-1
|
Others; Acyltransferase | Metabolism; Others |
OSMI-1 是一种 O-GlcNAc 转移酶 (OGT) 抑制剂 (IC50=2.7 μM),具有口服活性和细胞渗透性。OSMI-1 可以抑制蛋白质 O-GlcNA 酰化,而不会定性地改变细胞表面 N- 或 O- 连接的聚糖。 | |||
T6937 |
PF-04620110
PF04620110,PF 04620110 |
Acyltransferase; Transferase | Metabolism |
PF-04620110 是一种口服有效的甘油二酯酰基转移酶 -1(DGAT1)选择性抑制剂,IC50为 19 nM。 | |||
T26019 |
R59949
R-59949,R 59949 |
Others; PKC | Chromatin/Epigenetic; Cytoskeletal Signaling; Others |
R59949 是一种泛二酰甘油激酶(DGK)抑制剂,IC50为 300 nM。它通过提高内源性配体二酰甘油水平来激活蛋白激酶 C(PKC)。它强烈抑制 Ⅰ 型 DGKα 和 γ 的活性,中度减弱 Ⅱ 型 DGKθ 和 κ 的活性。 | |||
T11733 |
K-604 dihydrochloride
|
Acyltransferase | Metabolism |
K-604 dihydrochloride 是酰基辅酶 A:胆固醇酰基转移酶 1 的选择性抑制剂,IC50为 0.45±0.06 μM。 | |||
T10035 |
10,12-Tricosadiynoic acid
TDA,TCDA |
Acyltransferase | Metabolism |
10,12-Tricosadiynoic acid 是一种口服有效的酰基辅酶 A 氧化酶-1 (ACOX1) 抑制剂,具有高特异性,选择性,高亲和力的特点。10,12-Tricosadiynoic acid 可改善线粒体脂质和 ROS 代谢,在高脂饮食或肥胖引起的代谢性疾病中有研究的价值。 | |||
T23521 |
VULM 1457
|
Acyltransferase | Metabolism |
VULM 1457 是有效的胆固醇酰基转移酶抑制剂,具有显著的降血脂活性,并改善了整体心肌缺血再灌注损伤结果。VULM 1457 显著降低肾上腺髓质素的产生和分泌,并下调人肝母细胞上的 AM 受体。VULM 1457 具有研究糖尿病和高胆固醇血症的潜力。 | |||
T4681 |
T863
DGAT-3,DGAT-1 inhibitor |
Acyltransferase; Transferase | Metabolism |
T863 (DGAT-3) 是口服有效的二酰基甘油酰基转移酶1 选择性抑制剂。T863结合DGAT1的酰基辅酶A 结合位点,抑制三酰甘油在细胞内的合成。 | |||
T22665 |
PD 128042
CI 976 |
Acyltransferase | Metabolism |
PD 128042 (CI 976) 是口服有效的ACAT (酰基辅酶 A: 胆固醇酰基转移酶)选择性抑制剂。它也是LPAT(溶血磷脂酰基转移酶) 抑制剂。它抑制高尔基体相关 LPAT 活性 (IC50=15 μM)。它抑制多种膜运输步骤,包括在内吞和分泌途径中发现的步骤。 | |||
T22726 |
Dioctanoylglycol
2-octanoyloxyethyl octanoate,Dioctanoyl ethylene glycol,Ethylene glycol dioctanoate,ethane-1,2-diyl dioctanoate |
Others | Others |
Dioctanoylglycol (ethane-1,2-diyl dioctanoate) 是二酰基甘油类似物,也是二酰基甘油激酶 (DGK) 抑制剂,其Ki=为58 μM。 | |||
T2753 |
Avasimibe
PD-148515,阿伐麦布,CI-1011 |
P450; Acyltransferase | Metabolism |
Avasimibe (PD-148515) 是一种口服有效的酰基辅酶 A: 胆固醇酰基转移酶 (ACAT) 抑制剂,对 ACAT1和 ACAT2的 IC50分别为 24 和 9.2 µM。Avasimibe 在前列腺癌中有研究的价值。 | |||
T15247 |
ESI-05
NSC 116966 |
cAMP | GPCR/G Protein |
ESI-05 (NSC-116966) 是特异性的 cAMP 直接激活交换蛋白 2 (EPAC2) 拮抗剂(IC50:0.4 µM),能够抑制 cAMP 诱导的 EPAC2 的活化,并 EAPC2 介导的 Rap1 的活化。 | |||
T12225L |
Nevanimibe hydrochloride
PD-132301 hydrochloride,ATR101 hydrochloride |
Apoptosis; Acyltransferase | Apoptosis; Metabolism |
Nevanimibe hydrochloride (PD-132301 hydrochloride) 是一种口服有效的,选择性酰基辅酶 A:胆固醇 O-酰基转移酶 1 抑制剂,EC50为 9 nM。它抑制 ACAT2,EC50为 368 nM。它诱导细胞凋亡,具有抗肾上腺皮质癌的潜力。 | |||
T6365 |
A 922500
A922500,(1R,2R)-2-[[4-[[(苯基氨基)羰基]氨基][1,1-联苯]-4-基]甲酰基]环戊烷羧酸,DGAT-1 Inhibitor 4a |
Acyltransferase; Transferase | Metabolism |
A 922500 (DGAT-1 Inhibitor 4a) 是一种口服有效的二酰甘油酰基转移酶 1(DGAT-1)选择性抑制剂,抑制小鼠和人 DGAT-1 的IC50s 分别为9 nM,22 nM。 | |||
T12426 |
PF-06424439
|
Acyltransferase; Transferase | Metabolism |
PF-06424439 是一种口服有效的咪唑并吡啶二酰基甘油酰基转移酶 2 (DGAT2)选择性抑制剂,IC50是 14 nM。PF-06424439 具有缓慢可逆的,时间依赖性的特点,其相对于酰基-CoA 底物以非竞争性模式抑制 DGAT2。 | |||
T14375 |
AZD3988
|
Transferase | Metabolism |
AZD3988 是一种具有口服活性和高效性的二酰甘油酰基转移酶-1(DGAT-1)的抑制剂,可用于研究糖尿病和肥胖。 | |||
T73053 |
BAY 2965501
|
PERK | Apoptosis |
BAY 2965501 是一种有效且具有的选择性二酰基甘油激酶 zeta (DGKζ) 抑制剂,诱导 pERK 激活。BAY 2965501 可用于研究癌症。 | |||
T9186 |
Ervogastat
PF-06865571 |
Transferase | Metabolism |
Ervogastat (PF-06865571) 是一种有效且耐受性良好的二酰基甘油酰基转移酶 2 抑制剂。 Ervogastat 可降低非酒精性脂肪性肝炎 (NASH) 中的脂肪变性和肝脏甘油三酯水平。 | |||
T10954 |
DAGLβ-IN-1
|
Others | Others |
DAGLβ-IN-1,一种针对二酰基甘油脂肪酶 β (DAGLβ) 的抑制剂,可用作DAGL特异性活性探针的通用中间体。 | |||
T11016 |
DGAT-1 inhibitor 2
|
Transferase | Metabolism |
DGAT-1 inhibitor 2是有效的DGAT-1抑制剂,具有减肥功效。 | |||
T11827 |
Pradigastat
ANJ908,LCQ908-NXA,LCQ908A,LCQ-908 |
Transferase | Metabolism |
Pradigastat (LCQ-908) 是一种具有口服活性、有效性和选择性的二酰基甘油酰基转移酶 1 (DGAT1) 抑制剂,可用于治疗便秘,可用于研究肥胖和糖尿病。 | |||
T77761 |
BMS-502
|
Others | Others |
BMS-502 是一种二酰基甘油激酶 (DGK) α 和 ζ 的强效双重抑制剂, 诱导人和小鼠T细胞的免疫反应,阻断 T 细胞中细胞内检查点信号传导。BMS-502 以剂量依赖的方式刺激免疫反应,可用于研究与免疫相关的疾病。 | |||
T24128 |
H2-005
H2 005 |
||
H2-005 is a selective inhibitor of diacylglycerol acyltransferase 2 (DGAT2). | |||
T33814 |
OptoDArG
Opto-DArG,Opto DArG |
||
OptoDArG is a diacylglycerol (DAG) photoswitch, which enables efficient control of TRPC3 by light. | |||
T27692 |
JNJ-DGAT2-B
JNJDGAT2B,JNJ DGAT2 B |
||
JNJ-DGAT2-B is a selective inhibitor of Diacylglycerol acyltransferase 2. | |||
T71105 |
AZD2353
|
||
AZD2353 is a potent inhibitor of diacylglycerol acetyl transferase 1 (DGAT1). | |||
T40972 |
1-Oleoyl-2-acetyl-sn-glycerol
|
||
1-Oleoyl-2-acetyl-sn glycerol, a synthetic, cell-permeable diacylglycerol analog, activates calcium-dependent protein kinase C (PKC) and induces superoxide production. | |||
T33788 |
Oleoyl glutamic acid
NSC 513733,Glutamic acid, N-oleoyl-,NSC-513733,NSC513733 |
||
Oleoyl glutamic acid is a diacylglycerol analog. | |||
T24127 |
H2-003
H2003 |
||
H2-003 is a selective inhibitor of diacylglycerol acyltransferase 2 (DGAT2). | |||
T37044 |
1,2-Dioleoyl-rac-glycerol-13C3
1,2-Dioleoyl-rac-glycerol-13C3 |
||
1,2-Dioleoyl-rac-glycerol-13C3 is intended for use as an internal standard for the quantification of 1,2-dioleoyl-rac-glycerol by GC- or LC-MS. 1,2-dioleoyl-rac-glycerol is a diacylglycerol that contains oleic acid at the sn-1 and sn-2 positions. It effectively binds the C1 domain to activate conventional protein kinase C forms and serves as a substrate for diacylglycerol kinases and multisubstrate lipid kinase.1,2,3 |1. Yamaguchi, Y., Shirai, Y., Matsubara, T., et al. Phosphorylation and up-reg... | |||
T70160 | PF-06427878 | ||
PF-06427878 is an orally active, potent and selective diacylglycerol acyltransferase 2 inhibitor. | |||
T71755 |
QNN33358
|
||
QNN33358 is an alkylacylglycerol acts as a protein kinase C (PKC) inhibitor and diacylglycerol (DAG) antagonist. | |||
T27099 |
CU-3
CU 3,CU3 |
||
CU-3 is a potent and selective inhibitor of diacylglycerol kinase alpha (DGKalpha). CU-3 attenuates cancer cell proliferation and simultaneously enhances immune responses including anti-cancer immunity. | |||
T74027 | 1-Palmitoyl-2-oleoyl-sn-glycerol | ||
1-Palmitoyl-2-oleoyl-sn-glycerol是HIF (藻殖段诱导因子)-1中的主要二酰基甘油,属于内源性代谢产物。 | |||
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). | |||
T29275 |
1,3-Didecanoylglycerol
1,3-Dicaprin |
||
1,3-Didecanoylglycerol is a saturated diacylglycerol with decanoic acid (Item No. 20838) at the sn-1 and sn-3 positions. It has been used in the formation of lipid monolayers in the study of lipases. | |||
T40757 |
1-Stearoyl-2-arachidonoyl-sn-glycerol
|
||
1-Stearoyl-2-arachidonoyl-sn-glycerol, a diacylglycerol (DAG) encompassing polyunsaturated fatty acids, possesses the ability to activate PKC. Moreover, this compound has the potential to enhance nonselective cation channel (NSCC) activity. | |||
T35445 |
1-Stearoyl-3-Oleoyl-rac-glycerol
|
||
1-Stearoyl-3-oleoyl-rac-glycerol is a diacylglycerol that contains stearic acid at the sn-1 position and oleic acid at the sn-3 position. Intermittent fasting decreases skeletal muscle and hepatic levels of 1-stearoyl-3-oleoyl-rac-glycerol in New Zealand obese (NZO) mice.1 The concentration of 1-stearoyl-3-oleoyl-rac-glycerol decreases from 4.59 to 1.88% during the dry-curing process of Iberian ham.2References1. Baumeier, C., Kaiser, D., Heeren, J., et al. Caloric restriction and intermittent fa... | |||
T79826 |
DGKα-IN-6
|
||
DGKα-IN-6,一种DGKα抑制剂,其IC50值为1.377 nM,显示出可能用于癌症研究。 | |||
T72929 |
18:0-22:6 DG
1-Stearoyl-2-docosahexaenoyl-sn-glycerol |
||
18:0-22:6 DG (1-Stearoyl-2-docosahexaenoyl-sn-glycerol) 是一种二酰基甘油,可以与RasGRP 结合并调节MAP 激酶活化。 |
Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T3342 |
Xanthohumol
|
Apoptosis; Others; Influenza Virus; COX; Acyltransferase; HSV | Apoptosis; Immunology/Inflammation; Metabolism; Microbiology/Virology; Neuroscience; Others |
Xanthohumol 是从啤酒花中分离到的黄酮类化合物,可抑制 COX-1 和 COX-2 活性,具有抗肿瘤,抗血管生成的作用,还具有抗多种病毒的活性。 | |||
TN1691 |
Glabrol
光甘草酚,光甘草醇 |
P450; NF-κB; NO Synthase; Acyltransferase | Immunology/Inflammation; Metabolism; NF-κB |
Glabrol 是分离自甘草根的乙醇提取物中的一种异戊二烯类黄酮,是一种有效且非竞争性的酰基辅酶 A:胆固醇酰基转移酶(ACAT)抑制剂,抑制大鼠肝脏微粒体 ACAT 的 IC50为 24.6 μM。 | |||
T21437 |
DSPS
Phosphatidylserine(36:0),磷脂酰丝氨酸,Dioctadecanoylphosphatidylserine,Distearoyl phosphatidylserine |
Others | Others |
DSPS (Dioctadecanoylphosphatidylserine) 是一种甘油磷脂,是重要的磷脂膜成分,在细胞周期信号传导中起关键作用。DSPS 可以调节细胞活性,介导细胞凋亡。DSPS 被广泛用作营养补充剂。 | |||
T5544 |
2-Furoic acid
Furan-2-carboxylic acid,糠酸 |
Anti-infection; ATP Citrate Lyase; Endogenous Metabolite; Acyltransferase | Metabolism; Microbiology/Virology |
2-Furoic acid (Furan-2-carboxylic acid) 2-Furoic acid 能够降低血清中胆固醇和甘油三酯的水平,具有抗血脂作用。 | |||
TN5814 |
Digalactosyldiacylglycerol
DGDG,双半乳糖二酰甘油 |
||
Digalactosyldiacylglycerol 是一种天然产物,可用于生命科学领域的相关研究。其产品编号为 TN5814,CAS号为 145033-48-3。 | |||
T4950 |
1,2-Dipalmitoyl-sn-glycerol
1,2-双棕榈酸甘油酯,(S)-1,2-Dipalmitin |
Endogenous Metabolite; PKC | Chromatin/Epigenetic; Cytoskeletal Signaling; Metabolism |
1,2-Dipalmitoyl-sn-glycerol ((S)-1,2-Dipalmitin) 是内源性代谢产物的一种。 | |||
T69446 |
Cochlioquinone A
|
||
Cochlioquinone A is an inhibitor of diacylglycerol kinase (DGK) and diacylglycerol acyltransferase (DGAT). It has been shown to reduce the concentration of phosphatidic acid in T cell lymphoma and has also been shown to compete with macrophage inflammatory protein-1α for binding to human CCR5 chemokine receptors. | |||
T40347 |
Eicosapentaenoic acid methyl ester
|
||
Eicosapentaenoic acid methyl ester is a degradation product derived from monogalactosyl diacylglycerol, which is an apoptosis-inducing anticancer compound. | |||
TN1843 |
Kushenol K
|
PDE; HSV | Metabolism; Microbiology/Virology |
Kushenol K is a potent and Selective Inhibitor of cGMP Phosphodiesterase 5, it also has inhibitory effects on diacylglycerol acyltransferase (DGAT). Kushenol K shows weak antiviral activity against Herpes simplex virus types I and II. | |||
T37690 |
Phenylpyropene A
|
||
Phenylpyropene A is a fungal metabolite originally isolated from P. griseofulvum that has enzyme inhibitory and insecticidal activities.1,2,3 It inhibits acyl-coenzyme A:cholesterol acyltransferase (ACAT; IC50 = 0.8 μM).1 Phenylpyropene A inhibits diacylglycerol acyltransferase (DGAT) in rat liver microsomes (IC50 = 78.7 μM). It induces mortality in 100% of M. persicae when used at a concentration of 5 ppm.3 |1. Kwon, O.E., Rho, M.C., Song, H.Y., et al. Phenylpyropene A and B, new inhibitors of ... | |||
TN3428 |
Aphadilactone C
|
Others | Others |
Aphadilactone C shows significant antimalarial activity with the IC50 value of 170 ± 10 nM. It shows potent and selective inhibition against the diacylglycerol O-acyltransferase-1 (DGAT-1) enzyme (IC50 = 0.46 ± 0.09 uM, selectivity index > 217). | |||
TN3255 |
7beta-(3-Ethyl-cis-crotonoyloxy)-1alpha-(2-methylbutyryloxy)-3,14-dehydro-Z-notonipetranone
|
Others | Others |
7beta-(3-Ethyl-cis-crotonoyloxy)-1alpha-(2-methylbutyryloxy)-3,14-dehydro-Z-notonipetranone shows diacylglycerol acyltransferase (DGAT)1 inhibition with IC(50) values of 47.0 microM (for rat liver microsomes) and 160.7 microM (for HepG2 cell microsomes), | |||
T75697 | 1-Methyl-2-[(4Z,7Z)-4,7-tridecadienyl]-4(1H)-quinolone | ||
1-Methyl-2-[(4Z,7Z)-4,7-tridecadienyl]-4(1H)-quinolone,为喹诺酮类生物碱,作用为二酰基甘油酰基转移酶抑制剂与血管紧张素II受体阻断剂,其IC50值依次为20.1 μM与34.1 μM。此化合物亦展现对幽门螺杆菌的有效抗活性,MIC值达10 μg/mL。 |