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14

抑制剂 & 化合物

2

天然产物

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Cat. No.	Product Name	Target	Signaling Pathways
T23539	Y 11	Others	Others
	focal adhesion kinase (FAK) inhibitor
T23349	SF 11	Others	Others
	SF 11是一种有效的脑渗透神经肽 Y Y2 受体拮抗剂 (IC50=199 nM)。具有抗抑郁药样活性。
T1768	7ACC2	Mitochondrial Metabolism; Monocarboxylate transporter	Membrane transporter/Ion channel; Metabolism
	7ACC2 是单羧酸盐转运蛋白抑制剂，IC50为 11 nM。它还是线粒体丙酮酸转运的有效抑制剂，可抑制乳酸涌入，通过抑制乳酸通量来发挥抗癌作用。
T26855	BMS-665053 BMS665053	Others	Others
	BMS-665053 is a corticotropin-releasing factor-1 (CRF1) receptor antagonist (IC50 = 1.0 nM). BMS-665053)11 is a potent inhibitor of CRF-stimulated cyclic adenosine monophosphate (cAMP) production in human Y-79 retinoblastoma cells (IC50 = 4.9 nM). In addi
T35547	YW1128	Others	Others
	YW1128 is an inhibitor of Wnt/β-catenin signaling with an IC50 value of 4.1 nM in a reporter assay.1 It decreases protein levels of β-catenin in the presence of the GSK3β inhibitor lithium chloride and increases protein levels of Axin1 in HEK293 cells. YW1128 decreases lipid accumulation and the expression of gluconeogenic and lipogenic genes in Huh7 cells. It decreases the hepatic expression of Wnt target genes, improves glucose tolerance, and prevents body weight increases and hepatic lipid ac...
T35909	Penicinoline	Others	Others
	Penicinoline is an alkaloid that has been found in Penicillium and has antimalarial, insecticidal, and anticancer activities.1,2 It is active against chloroquine-sensitive and -resistant strains of P. falciparum (IC50 = 25 μM for both).1 Penicinoline (1,000 ppm) is also active against the aphid A. gossypii.2 It inhibits proliferation of 95-D and HepG2 cancer cells (IC50s = 0.57 and 6.5 μg/ml, respectively) but not HeLa, KB, KBv200, or Hep-2 cells (IC50s = >100 μg/ml). \|1. Naveen, B., Ommi, N.B.,...
T35854	9(Z),11(E)-Conjugated Linoleic Acid (sodium salt)	Others	Others
	9(Z),11(E)-Conjugated linoleic acid is an isomer of linoleic acid that has been found in beef and milk fat.1It binds to peroxisome proliferator-activated receptor α (PPARα; IC50= 140 nM) and activates the receptor in a reporter assay using COS-1 cells expressing mouse PPARα when used at a concentration of 100 μM.29(Z),11(E)-Conjugated linoleic acid inhibits TNF-α-inducedGLUT4expression and increases insulin-stimulated glucose transport in 3T3-L1 adipocytes.3Dietary administration of 9(Z)11(E)-co...
T37370	Amyloid-β (25-35) Peptide (human) (trifluoroacetate salt)
	Amyloid-β (25-35) (Aβ (25-35)) is an 11-residue fragment of the Aβ protein that retains the physical and biological characteristics of the full length peptide. It forms fibrils that react to thioflavin T and Congo red and are organized in a cross-β arrangement of β-strands similar to Aβ (1-40) and Aβ (1-42) fibrils. Aggregated Aβ (25-35) decreases the viability of rat adrenal PC12 cells. It also decreases the viability of primary rat cortical neurons at concentrations ranging from 1 nM to 30 μM....
T37837	2-Methylhexacosane	Others	Others
	2-Methylhexacosane is a saturated hydrocarbon and an insect pheromone.1,2It has been found in the cuticle ofM. dasystomusfemales, but not males, where it contributes to the mating behavior of males, as well as inD. melanogasterfemales where it modulates aggression of males towards females. 2-methylhexacosane has also been found in yellow jacket (V. vulgaris) trail extracts.3 1.Spikes, A.E., Pashen, M.A., Millar, J.G., et al.First contact pheromone identified for a longhorned beetle (Coleoptera: ...
T35485	6-Prenylindole	Others	Others
	6-Prenylindole is a bacterial metabolite that has been found in Streptomyces and has antifungal and antimalarial properties.1 It is active against A. brassicicola strain TP-F0423 and F. oxysporum f. sp. tulipae TU-4-2 (15 and 30 μg/disc in the paper disc assay), and also drug-resistant P. falciparum strain K1 (IC50 = 21 μg/ml).2 \|1. Sasaki, T., Igarashi, Y., Ogawa, M., et al. Identification of 6-prenylindole as an antifungal metabolite of Streptomyces sp. TP-A0595 and synthesis and bioactivity o...
T38381	CAY17c	Others	Others
	CAY17c is an inhibitor of bromodomain-containing protein 4 (BRD4; IC50= 0.71 μM), as well as class I histone deacetylases (HDACs; IC50s = 0.046, 0.058, 0.075, and 0.167 μM for HDAC1, -2, -3, and -8, respectively) and class IIb HDACs (IC50s = 0.073 and 0.923 μM for HDAC6 and HDAC10, respectively).1It is selective for these enzymes over BRD2, -3, and -T (IC50s = >20 μM for all), as well as over HDAC4, -5, -7, -9, and -11 (IC50s = >10 μM for all). CAY17c inhibits the proliferation of HCT116, SW620,...
T35929	O-Demethyl Apremilast	Others	Others
	O-Demethyl apremilast is an active metabolite of the phosphodiesterase 4 (PDE4) inhibitor apremilast .1It inhibits the activity of PDE4 isolated from U937 cells and LPS-induced TNF-α production in isolated human peripheral blood mononuclear cells (PBMCs; IC50s = 8.3 and 5.6 μM, respectively). O-Demethyl apremilast is also an oxidative degradation product of apremilast.2,3 1.Hoffmann, M., Kumar, G., Schafer, P., et al.Disposition, metabolism and mass balance of [14C]apremilast following oral admi...
T35772	Emestrin	Others	Others
	Emestrin is a mycotoxin originally isolated from E. striata that has antimicrobial, immunomodulatory, and cytotoxic activities.1,2,3,4,5 It is active against the fungi C. albicans and C. neoformans, as well as the bacteria E. coli, S. aureus, and methicillin-resistant S. aureus (MRSA; IC50s = 3.94, 0.6, 2.21, 4.55, and 2.21 μg/ml, respectively).2 Emestrin is a chemokine (C-C motif) receptor 2 (CCR2) antagonist (IC50 = 5.4 μM in a radioligand binding assay using isolated human monocytes).3 Emestr...
T35406	α-MSH TFA
	α-Melanocyte-stimulating hormone (α-MSH) is a 13-amino acid peptide hormone produced by post-translational processing of proopiomelanocortin (POMC) in the pituitary gland, as well as in keratinocytes, astrocytes, monocytes, and gastrointestinal cells.1It is an agonist of melanocortin receptor 3 (MC3R) and MC4R that induces cAMP production in Hepa cells expressing the human receptors (EC50s = 0.16 and 56 nM, respectively).2α-MSH (100 pM) reducesS. aureuscolony formation andC. albicansgerm tube fo...

化合物

Cat.No: T23539

Target: Others

Cat.No: T23349

Target: Others

Cat.No: T1768

Target: Mitochondrial Metabolism, Monocarboxylate transporter

Cat.No: T26855

Synonym: BMS665053

Target: Others

Cat.No: T35547

Target: Others

Cat.No: T35909

Target: Others

9(Z),11(E)-Conjugated Linoleic Acid (sodium salt)

Cat.No: T35854

Target: Others

Amyloid-β (25-35) Peptide (human) (trifluoroacetate salt)

Cat.No: T37370

2-Methylhexacosane

Cat.No: T37837

Target: Others

Cat.No: T35485

Target: Others

Cat.No: T38381

Target: Others

O-Demethyl Apremilast

Cat.No: T35929

Target: Others

Cat.No: T35772

Target: Others

Cat.No: T35406

Cat. No.	Product Name	Target	Signaling Pathways
T38069	Aquastatin A	Others	Others
	Aquastatin A is a fungal metabolite originally isolated fromF. aquaeductuumthat has diverse biological activities.1It is active againstS. aureus(MIC = 32 μg/ml) and inhibits enoyl-acyl carrier protein reductase (Fabl; IC50= 3.2 μM) andS. aureusfatty acid synthesis (IC50= 3.5 μM).2Aquastatin A also inhibits the Na+/K+-ATPase and H+/K+-ATPase (IC50s = 7.1 and 6.2 μM, respectively), as well as protein tyrosine phosphatase 1B (PTP1B; IC50= 0.19 μM).1,3 1.Hamano, K., Kinoshita-Okami, M., Minagawa, K....
T36000	3-Hydroxyterphenyllin	Others	Others
	3-Hydroxyterphenyllin is a p-terphenyl fungal metabolite originally isolated from A. candidus that has diverse biological activities, including antioxidant, antiproliferative, antibacterial, and antiviral properties.1,2,3,4 It has a 96% scavenging effect on 2,2-diphenyl-1-picrylhydrazyl radicals when used at a concentration of 100 μg/ml.2 3-Hydroxyterphenyllin inhibits the growth of HeLa cervical, A549 lung, and HepG2 liver cancer cells (IC50s = 23, 36, and 32 μM, respectively), as well as methi...

天然产物

Cat.No: T38069

Target: Others

3-Hydroxyterphenyllin

Cat.No: T36000

Target: Others

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