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20

抑制剂 & 化合物

2

天然产物

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Cat. No.	Product Name	Target	Signaling Pathways
T7119	Y15 1,2,4,5-苯四胺四盐酸盐,1,2,4,5-Benzenetetramine tetrahydrochlor,FAK Inhibitor 14	FAK	Angiogenesis; Cytoskeletal Signaling; Tyrosine Kinase/Adaptors
	Y15 (1,2,4,5-Benzenetetramine tetrahydrochlor) 是一种特异性的粘着斑激酶抑制剂，能够降低其自身磷酸化活性，抑制癌细胞的活力，阻断肿瘤生长。
T1846	Y-320 Y320	IL Receptor; Lipase; Interleukin	Immunology/Inflammation; Metabolism
	Y-320 是一种免疫调节剂，能阻碍IL-15刺激CD4 T 细胞后的IL-17的产生，IC50=20~60 nM。
T14572	BIIE-0246 AR-H 053591	Others	Others
	BIIE-0246 is a potent and highly selective non-peptide neuropeptide Y (NPY) Y2 receptor antagonist. With an IC50 of 15 nM.
T36481	BIIE 0246 hydrochloride
	Potent, selective and competitive nonpeptide antagonist for the neuropeptide Y Y2 receptor (IC50 = 15 nM). Displays > 650-fold selectivity for NPY Y2 over Y1, Y4 and Y5 receptors. Active in vivo.
TP1681	Neuropeptide Y (22-36)
	Neuropeptide Y (22-36), a 15 amino acid peptide, is a fragment of Neuropeptide Y.Neuropeptide Y (NPY) is a 36 amino-acid neuropeptide that is involved in various physiological and homeostatic processes in both the central and peripheral nervous systems. N
T38127	pNPS-DHA
	pNPS-DHA is an arylamide derivative of docosahexaenoyl ethanolamide that has anti-allergic activity.1It inhibits degranulation of RBL-2H3 mast cells (IC50= 15 μM).pNPS-DHA (1,000 mg/kg) inhibits IgE-dependent passive cutaneous anaphylaxis (PCA) in mice. 1.Kim, I.-H., Kanayama, Y., Nishiwaki, H., et al.Structure-activity relationships of fish oil derivatives with anti-allergic activity in vitro and in vivoJ. Med. Chem.62(21)9576-9592(2019)
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 ...
T35485	6-Prenylindole
	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...
T37754	Avilamycin A
	Avilamycin A is an antibiotic.1 It is active against veterinary isolates of C. perfringens (MICs = ≤0.06-0.5 mg/L) and B. hyodysenteriae (MICs = 12.5-100 μg/ml).1,2 Dietary administration of avilamycin A (15 and 30 ppm) reduces mortality in a broiler cockerel model of C. perfringens infection.3 Formulations containing avilamycin A have been used in the prevention of necrotic enteritis in livestock. \|1. Watkins, K.L., Shryock, T.R., Dearth, R.N., et al. In-vitro antimicrobial susceptibility of Cl...
T36152	14S(15R)-EET
	14S(15R)-EET is an oxylipin and a cytochrome P450 metabolite of arachidonic acid .114S(15R)-EET binds to isolated guinea pig monocytes with a Kivalue of 612.5 nM in a competitive binding assay using [3H]14(15)-EET.2It induces dilation of precontracted isolated canine epicardial arterioles (EC50= 4 pM) and denuded porcine subepicardial arterioles (EC50= 3 pM).3Unlike 14R(15S)-EET, 14S(15R)-EET does not inhibit COX in enzyme assays or isolated platelets.4 1.Daikh, B.E., Lasker, J.M., Raucy, J.L., ...
T37720	Difluorinated H2S Fluorescent Probe 1
	Difluorinated H2S probe 1 is a fluorescent probe for hydrogen sulfide (H2S).1It selectively fluoresces in the presence of H2S over Zn2+, Fe3+, S2O32-, ClO-, SO32-, H2O2, NO2-, cysteine (Cys), homocysteine (Hcy), and glutathione (GSH) when used at a concentration of 1 μM. Difluorinated H2S probe 1 displays excitation/emission maxima of 365/450 nm, respectively. 1.Zhang, J., Gao, Y., Kang, X., et al.o,o-Difluorination of aromatic azide yields a fast-response fluorescent probe for H2S detection and...
T35463	(±)14(15)-EET (±)14,15-EET,(±)14,15-EpETrE,(±)14(15)-EET
	(±)14(15)-EET is a metabolite of arachidonic acid that is formed via epoxidation of arachidonic acid by cytochrome P450.[1],[2] It prevents increases in leukotriene B4, ICAM-1, and chemokine (C-C motif) ligand 1 (CCL2) induced by oxidized LDL in primary rat pulmonary artery endothelial cells (RPAECs) when used at a concentration of 1 μM.[3] (±)14(15)-EET induces dilation of preconstricted isolated canine coronary arterioles (EC50 = 0.2 pM).[4] It reduces myocardial infarct size as a percentage o...
T38381	CAY17c
	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,...
T36722	Deltorphin II (trifluoroacetate salt)
	Deltorphin II is a peptide agonist of δ2-opioid receptors.1,2It is selective for δ-opioid receptors over μ- and κ-opioid receptors in radioligand bindings assays (Kis = 0.0033, >1, and >1 μM, respectively) and induces [35S]GTPγS binding in mouse brain membrane preparations (EC50= 0.034 μM). Deltorphin II (0.12 mg/kg) decreases the infarction zone:risk zone ratio in a rat model of myocardial ischemia-reperfusion injury induced by coronary occlusion, an effect that can be reversed by the δ2-opioid...
T36490	AZT triphosphate TEA
	AZT triphosphate TFA (3'-Azido-3'-deoxythymidine-5'-triphosphate TFA) is a active triphosphate metabolite of Zidovudine (AZT). AZT triphosphate TFA exhibits antiretroviral activity and inhibits replication of HIV. AZT triphosphate TFA also inhibits the DNA polymerase of HBV. AZT triphosphate TFA activates the mitochondria-mediated apoptosis pathway[1][2][3]. Treatment with 100 μM Zidovudine (AZT) for 48h disrupts the mitochondrial tubular network via accumulation of AZT triphosphate (AZT-TP) in ...
T35742	IKD-8344
	IKD-8344 is a macrocyclic dilactone originally isolated from an actinomycete species and has diverse biological activities, including anticancer, antimicrobial, and anthelmintic properties.1,2,3 It is cytotoxic to L5178Y murine leukemia cells (IC50 = 0.54 ng/ml).1 IKD-8344 inhibits growth of the mycelial form of C. albicans (MIC = 6.25 μg/ml) and potentiates the activity of polymyxin B against the multidrug-resistant pathogenic bacterium B. cenocepacia.2,3 It is active against T. spiralis in vit...
T36679	Rp-cAMPS sodium salt
	Rp-cAMPS sodium salt, a cAMP analog, is a potent, competitive cAMP-induced activation of cAMP-dependent PKA I and II (Kis of 12.5 μM and 4.5 μM, respectively) antagonist. Rp-cAMPS sodium salt is resistant to hydrolysis by phosphodiesterases[1][2][3][4][5][6]. A membrane-permeable competitive cAMP antagonist (Rp-cAMPS) that blocks PKA activation by binding to the regulatory subunits without dissociating the kinase holoenzyme also inhibits synaptic plasticity but has no effect on normal synaptic t...
T35536	Tpl2 Kinase Inhibitor (hydrochloride)
	Tpl2 kinase inhibitor is an inhibitor of tumor progression locus 2 (Tpl2; IC50= 0.05 μM).1It is selective for Tpl2 over MEK, p38 MAPK, Src, MK2, and PKC (IC50s = >40, 180, >400, 110, and >400 μM, respectively). Tpl2 kinase inhibitor inhibits LPS-induced TNF-α production in isolated human monocytes and whole blood (IC50s = 0.7 and 8.5 μM, respectively). It enhances differentiation induced by calcitriol in HL-60 and U937 leukemia cells when used at a concentration of 5 μM.2Tpl2 kinase inhibitor (5...
T37761	Fura-FF (potassium salt)
	Fura-FF is a difluorinated derivative of the calcium indicator fura-2. Unlike, fura-2, fura-FF has negligible magnesium sensitivity, thus reducing interference from this cation.[1] Fura-FF also has a higher calcium dissociation constant than fura-2 (Kd(calcium) = 6 and 0.14 μM, respectively).[1],[2]However, the spectral properties of fura-FF and fura-2 are similar with fura-FF displaying excitation/emission spectra of 365/514 nm in the absence of calcium, with a shift to 339/507 nm in the presen...
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...

化合物

Cat.No: T7119

Synonym: 1,2,4,5-苯四胺四盐酸盐,1,2,4,5-Benzenetetramine tetrahydrochlor,FAK Inhibitor 14

Target: FAK

Cat.No: T1846

Synonym: Y320

Target: IL Receptor, Lipase, Interleukin

Cat.No: T14572

Synonym: AR-H 053591

Target: Others

BIIE 0246 hydrochloride

Cat.No: T36481

Neuropeptide Y (22-36)

Cat.No: TP1681

Cat.No: T38127

Cat.No: T36991

Cat.No: T35485

Cat.No: T37754

Cat.No: T36152

Difluorinated H2S Fluorescent Probe 1

Cat.No: T37720

Cat.No: T35463

Synonym: (±)14,15-EET,(±)14,15-EpETrE,(±)14(15)-EET

Cat.No: T38381

Deltorphin II (trifluoroacetate salt)

Cat.No: T36722

AZT triphosphate TEA

Cat.No: T36490

Cat.No: T35742

Rp-cAMPS sodium salt

Cat.No: T36679

Tpl2 Kinase Inhibitor (hydrochloride)

Cat.No: T35536

Fura-FF (potassium salt)

Cat.No: T37761

Zonisamide-13C2,15N

Cat.No: T37847

Synonym: Zonisamide-13C2,15N

Cat. No.	Product Name	Target	Signaling Pathways
T3030	L-Sophoridine L-槐定碱,Sophoridine,Matridin-15-one	Others	Others
	L-Sophoridine (Matridin-15-one) 一种从药用植物中提取的天然产物，具有多种药理作用，包括抗Y 作用，可在体外和体内选择性诱导多种人体Y 细胞凋亡；然而，其作用机制需要进一步阐述。
T36000	3-Hydroxyterphenyllin
	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: T3030

Synonym: L-槐定碱,Sophoridine,Matridin-15-one

Target: Others

3-Hydroxyterphenyllin

Cat.No: T36000

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