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21

抑制剂 & 化合物

2

天然产物

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Cat. No.	Product Name	Target	Signaling Pathways
TP1992L	M40 acetate(143896-17-7 free base)	Neuropeptide Y Receptor	GPCR/G Protein; Neuroscience
	M40 acetate(143896-17-7 free base) 是一种有效的、非选择性的甘丙肽受体拮抗剂（GAL1 和 GAL2 的 Ki 值分别为 1.82 和 5.1 nM），在体外抑制大鼠脑中甘丙肽 (1-29) 的结合 (IC50 = 3 - 15 nM)。减弱氟西汀的抗抑郁作用并阻止甘丙肽诱导的体内食物摄入。在剂量 > 100 nM 时，对外周 GAL2 受体也表现出较弱的部分激动剂活性。
TP1992	M40
	Potent, non-selective galanin receptor antagonist (Ki values are 1.82 and 5.1 nM at GAL1 and GAL2 respectively) that inhibits galanin (1-29) binding in rat brain in vitro (IC50 = 3 - 15 nM). Attenuates the antidepressant effects of fluoxetine and blocks galanin-induced food intake in vivo. Also exhibits weak partial agonist activity at peripheral GAL2 receptors at doses > 100 nM.
T20073	Asulam MB 9057,Asulox 40,M and B 9057
	Asulam is a wild oat herbicide.
T8107	GLX351322	NADPH-oxidase; NADPH	Immunology/Inflammation; Metabolism
	GLX351322 抑制 NADPH 氧化酶 4 (Nox4) 。在 NOX4 过表达的细胞中，抑制过氧化氢的产生，IC50值为 5 μM。
T72169	Tubulin polymerization-IN-40
	Tubulin polymerization-IN-40为基于吖啶的微管蛋白聚合抑制剂，IC50值为1.5 μM，能在G2/M期阻滞癌细胞并诱导细胞凋亡，同时显示出抗癌活性与免疫增强作用。
T36674	DMU-212	Apoptosis; ERK	Apoptosis; MAPK
	DMU-212 是具有口服活性的白藜芦醇的甲基化衍生物，表现出抗分裂、抗增殖、抗氧化和促进细胞凋亡的活性。它通过诱导凋亡和激活ERK1/2蛋白阻止有丝分裂。
T37531	Glycerophosphorylethanolamine (sodium salt)
	Glycerophosphorylethanolamine is an active phosphodiester metabolite of phosphatidylethanolamine.1,2It promotes aggregation of amyloid-β (1-40) (Aβ40)in vitro, and levels of glycerophosphorylethanolamine are elevated in postmortem brains isolated from patients with Alzheimer’s disease. 1.Klunk, W.E., Xu, C.J., McClure, R.J., et al.Aggregation of β-amyloid peptide is promoted by membrane phospholipid metabolites elevated in Alzheimer’s disease brainJ. Neurochem.69(1)266-272(1997) 2.Blusztajn, J.K...
T36991	Monascuspiloin
	Monascuspiloin is a fungal metabolite that has been found inM. pilosusM93-fermented rice.1It induces endoplasmic reticulum stress and autophagy in PC3 prostate cancer cells. Monascuspiloin (15-45 μM) decreases viability of PC3 cells and has an additive effect on the reduction in viability of PC3 cells induced by irradiation when used at a concentration of 25 μM. It induces intratumor apoptosis and autophagy and reduces tumor growth in a PC3 mouse xenograft model when administered at doses of 40 ...
T37594	Pericosine A
	Pericosine A is a fungal metabolite that has been found inP. byssoidesand has anticancer activity.1It inhibits the growth of a variety of cancer cells, including breast, colon, lung, ovary, stomach, and prostate cell lines (GI50s = 0.05-24.55 μM) and increases survival in a P388 mouse xenograft model when administered at a dose of 25 mg/kg. Pericosine A inhibits EGFR by 40 to 70% when used at a concentration of 100 μg/ml. It also reacts with organosulfur compounds in skunk spray to form stable t...
T35504	(±)10-HDHA
	(±)10-HDHA is an autoxidation product of docosahexaenoic acid (DHA) in vitro.[1][2] It is also produced from incubations of DHA in rat liver, brain, and intestinal microsomes.[3][4][5] (±)10-HDHA is a potential marker of oxidative stress in brain and retina where DHA is an abundant polyunsaturated fatty acid. Reference：[1]. VanRollins, M., and Murphy, R.C. Autooxidation of docosahexaenoic acid: Analysis of ten isomers of hydroxydocosahexaenoate. J. Lipid Res. 25(5), 507-517 (1984).[2]. Reynaud, ...
T36521	Alaproclate (hydrochloride)
	Alaproclate is a selective serotonin reuptake inhibitor (SSRI).1,2 It inhibits depletion of serotonin (5-HT) induced by 4-methyl-α-ethyl-m-tyramine in rat cerebral cortex, hippocampus, hypothalamus, and striatum (EC50s = 18, 4, 8, and 12 mg/kg, respectively).1 Alaproclate inhibits NMDA-evoked currents and depolarization-induced voltage-dependent potassium currents in rat hippocampal neurons (IC50s = 1.1 and 6.9 μM, respectively) and does not inhibit GABA-evoked currents when used at concentratio...
T35762	MC1742
	MC1742 is an inhibitor of class I histone deacetylases (HDACs; IC50s = 0.1, 0.11, 0.02, and 0.61 μM for HDAC1, -2, -3, and -8, respectively) and class IIb HDACs (IC50s = 7 and 40 nM for HDAC6 and HDAC10, respectively).1 It is selective for class I and class IIb over class IIa HDACs (IC50s = >50 μM for HDAC4, -5, -7, and -9). MC1742 reduces proliferation of HOS, MG-63, RD, A204, SK-ES-1, and A673 sarcoma cancer stem cells (CSCs). It increases levels of acetylated histone H3 and acetylated tubulin...
T35814	Urocortin III (human) (trifluoroacetate salt)
	Urocortin III is a neuropeptide hormone and member of the corticotropin-releasing factor (CRF) family which includes mammalian CRF , urocortin , urocortin II , frog sauvagine, and piscine urotensin I.1 Human urocortin III shares 90, 40, 37, and 21% identity to mouse urocortin III , mouse urocortin II , human urocortin , and mouse urocortin, respectively. Urocortin III selectively binds to type 2 CRF receptors (Kis = 21.7, 13.5, and >100 nM for rat CRF2α, rat CRF2β, and human CRF1, respectively)....
T37537	Carbazomycin D
	Carbazomycin D is a bacterial metabolite that has been found inStreptomycesand has diverse biological activities.1,2It is active against the fungiT. asteroidesandT. mentagrophytes(MIC = 100 μg/ml for both) and the bacteriumM. tuberculosis(IC50= 25 μg/ml). Carbazomycin D is cytotoxic to MCF-7, KB, NCI H187, and Vero cells (IC50s = 21.3, 33.2, 12.9, and 34.3 μg/ml, respectively).2 1.Naid, T., Kitahara, T., Kaneda, M., et al.Carbazomycins C, D, E and F, minor components of the carbazomycin complexJ...
T37847	Zonisamide-13C2,15N Zonisamide-13C2,15N
	Zonisamide-13C2,15N is intended for use as an internal standard for the quantification of zonisamide by GC- or LC-MS. Zonisamide is an antiepileptic agent.1 It selectively inhibits the repeated firing of sodium channels (IC50 = 2 μg/ml) in mouse embryo spinal cord neurons and inhibits spontaneous channel firing when used at concentrations greater than 10 μg/ml.2 In rat cerebral cortex neurons, zonisamide (1-1,000 μM) inhibits T-type calcium channels with a maximum reduction of 60% of the calcium...
T36695	TAS-103
	TAS-103 is a dual inhibitor of DNA topoisomerase I/II, used for cancer research. TAS-103 is a dual inhibitor of DNA topoisomerase I/II. TAS-103 (0.1-10 μM) is active on CCRF-CEM cells, with an IC50 value of 5 nM. TAS-103 (0.1 μM) significantly increases levels of topo IIα FITC immunofluorescence in individual CCRF-CEM cells[1]. TAS-103 (0.01-1 μM) is highly cytotoxic to Lewis lung carcinoma (LLC) cells, and Liposomal TAS-103 is almost as active as free TAS-103[2]. TAS-103 inhibits the viability ...
T38280	C22 dihydro 1-Deoxyceramide (m18:0/22:0) C22 dihydro 1-Deoxyceramide (m18:0/22:0)
	C22 dihydro 1-Deoxyceramide (m18:0/22:0) is a very long-chain atypical ceramide containing a 1-deoxysphinganine backbone. 1-Deoxysphingolipids are formed when serine palmitoyltransferase condenses palmitoyl-CoA with alanine instead of serine during sphingolipid synthesis.1,2 C22 dihydro 1-Deoxyceramide (m18:0/22:0) has been found in mouse embryonic fibroblasts (MEFs) following application of 1-deoxysphinganine alkyne or 1-deoxysphinganine-d3.3 It has also been found as the most prevalent dihydro...
T35451	β-Defensin-2 (human) (trifluoroacetate salt)
	β-Defensin-2 is a peptide with antimicrobial properties that protects the skin and mucosal membranes of the respiratory, genitourinary, and gastrointestinal tracts.1It inhibits the growth of periodontopathogenic and cariogenic bacteria, includingP. gingivalisandS. salivarius.2β-Defensin-2 (30 μg/ml) stimulates gene expression and production of IL-6, IL-10, CXCL10, CCL2, MIP-3α, and RANTES by keratinocytes.3It also stimulates calcium mobilization, migration, and proliferation of keratinocytes whe...
T38284	C24 dihydro 1-Deoxyceramide (m18:0/24:0) C24 dihydro 1-Deoxyceramide (m18:0/24:0)
	C24 dihydro 1-Deoxyceramide (m18:0/24:0) is a very long-chain atypical ceramide containing a 1-deoxysphinganine backbone. 1-Deoxysphingolipids are formed when serine palmitoyltransferase condenses palmitoyl-CoA with alanine instead of serine during sphingolipid synthesis.1,2 C24 dihydro 1-Deoxyceramide (m18:0/24:0) has been found in mouse embryonic fibroblasts (MEFs) following application of 1-deoxysphinganine alkyne or 1-deoxysphinganine-d3.3 It has also been found in mouse brain, spinal cord, ...
T36084	PKI-179
	PKI-179 is a potent and orally active dual PI3K/mTOR inhibitor, with IC50s of 8 nM, 24 nM, 74 nM, 77 nM, and 0.42 nM for PI3K-α, PI3K-β, PI3K-γ, PI3K-δ and mTOR, respectively. PKI-179 also exhibits activity over E545K and H1047R, with IC50s of 14 nM and 11 nM, respectively. PKI-179 shows anti-tumor activity in vivo[1][2]. PKI-179 inhibits the cell proliferation, with IC50s of 22 nM and 29 nM for MDA361 and PC3 cells, respectively[1].PKI-179 shows inhibitory activity against a panel of 361 other ...
T37582	Ganglioside GM1 Mixture (ovine) (ammonium salt)
	Ganglioside GM1is a monosialylated ganglioside and the prototypic ganglioside for those containing one sialic acid residue.1,2It is found in a large variety of cells, including immune cells and neurons, and is enriched in lipid rafts in the cell membrane.3It associates with growth factor receptors, including TrkA, TrkB, and the GDNF receptor complex containing Ret and GFRα, and is required for TrkA expression on the cell surface. Ganglioside GM1interacts with other proteins to increase calcium i...

化合物

M40 acetate(143896-17-7 free base)

Cat.No: TP1992L

Target: Neuropeptide Y Receptor

Cat.No: TP1992

Cat.No: T20073

Synonym: MB 9057,Asulox 40,M and B 9057

Cat.No: T8107

Target: NADPH-oxidase, NADPH

Tubulin polymerization-IN-40

Cat.No: T72169

Cat.No: T36674

Target: Apoptosis, ERK

Glycerophosphorylethanolamine (sodium salt)

Cat.No: T37531

Cat.No: T36991

Cat.No: T37594

Cat.No: T35504

Alaproclate (hydrochloride)

Cat.No: T36521

Cat.No: T35762

Urocortin III (human) (trifluoroacetate salt)

Cat.No: T35814

Cat.No: T37537

Zonisamide-13C2,15N

Cat.No: T37847

Synonym: Zonisamide-13C2,15N

Cat.No: T36695

C22 dihydro 1-Deoxyceramide (m18:0/22:0)

Cat.No: T38280

Synonym: C22 dihydro 1-Deoxyceramide (m18:0/22:0)

β-Defensin-2 (human) (trifluoroacetate salt)

Cat.No: T35451

C24 dihydro 1-Deoxyceramide (m18:0/24:0)

Cat.No: T38284

Synonym: C24 dihydro 1-Deoxyceramide (m18:0/24:0)

Cat.No: T36084

Ganglioside GM1 Mixture (ovine) (ammonium salt)

Cat.No: T37582

Cat. No.	Product Name	Target	Signaling Pathways
TN1950	Moracin M	PDE	Metabolism
	Moracin M 是桑白皮中的一种酚类成分，有效的磷酸二酯酶 4 (PDE4) 抑制剂，对于 PDE4D2，PDE4B2，PDE5A1 和 PDE9A2 的 IC50 分别为 2.9 μM，4.5 μM，> 40 μM 和 > 100 μM。Moracin M 具有抗炎活性。
T37272	9(S),12(S),13(S)-TriHOME
	9(S),12(S),13(S)-TriHOME is a linoleic acid-derived oxylipin that has diverse biological activities.1,2,3,4It has been found in various plants and is produced in human eosinophils in a 15-lipoxygenase-dependent, soluble epoxide hydrolase-independent manner.1,59(S),12(S)13(S)-TriHOME inhibits antigen-induced β-hexosaminidase release from RBL-2H3 mast cells (IC50= 28.7 μg/ml).2It inhibits LPS-induced nitric oxide (NO) production in BV-2 microglia (IC50= 40.95 μM).3In vivo, 9(S),12(S),13(S)-TriHOME...

天然产物

Cat.No: TN1950

Target: PDE

9(S),12(S),13(S)-TriHOME

Cat.No: T37272

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