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26

抑制剂 & 化合物

2

天然产物

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Cat. No.	Product Name	Target	Signaling Pathways
T38034	MAO-IN-M30 dihydrochloride M 30 dihydrochloride	Monoamine Oxidase	Neuroscience
	MAO-IN-M30 dihydrochloride (M 30 dihydrochloride) 是一种口服活性，可通过血脑屏障的，脑选择性不可逆 MAO-A (IC50=37 nM) 和 MAO-B (IC50=57 nM) 抑制剂。MAO-IN-M30 dihydrochloride 是有效的铁螯合剂、自由基清除剂。MAO-IN-M30 dihydrochloride 对 Dexamethasone 诱导的脑细胞凋亡具有神经保护作用。MAO-IN-M30 dihydrochloride 在 MPTP 和 lactacystin 帕金森病模型中也显示出神经恢复活性。
T71857	GTP-14564	FLT; Tyrosine Kinases	Angiogenesis; Tyrosine Kinase/Adaptors
	GTP-14564是一种新型酪氨酸激酶抑制剂，对 wt-FLT3和ITD-FLT3也具有抑制作用。GTP-14564 在 3μ m 处抑制表达 ITD-FLT3 的白细胞介素-3 非依赖性 Ba/F1 的生长，而需要高 30 倍的 GTP-14564 浓度来抑制表达野生型 FLT3 的 Ba/F3 的 FLT3 配体依赖性生长（wt-FLT3）。
T5818	Rigosertib sodium Rigosertib,Estybon,ON-01910	Apoptosis; PLK; PI3K	Apoptosis; Cell Cycle/Checkpoint; PI3K/Akt/mTOR signaling
	Rigosertib sodium (ON-01910) 是一种选择性的非 ATP 竞争性PLK1抑制剂，IC50值为 9 nM。它是一种多激酶抑制剂和选择性抗癌剂，通过抑制PI3K/Akt 途径诱导细胞凋亡，促进组蛋白 H2AX 的磷酸化并诱导细胞周期中的 G2/M 期停滞。
T36351	Suc-AAP-Abu-pNA
	Suc-AAP-Abu-pNA 是胰腺弹性蛋白酶的特异性底物 (Km = 100 μM; Kcat/Km = 35,300 s-1 M-1 for rat pancreatic elastase; Km = 30 μM; Kcat/Km = 351,000 s-1 M-1 for porcine pancreatic elastase)。
T80300	Aurein 2.6	Antibiotic	Microbiology/Virology
	Aurein 2.6为具有针对革兰氏阳性菌抗菌效力的抗生素肽。该化合物在抗菌活性上表现出对M. luteus、S. aureus、S. epidermis、S. mutans、B. subtilis的最小抑菌浓度（MIC）分别为25、25、30、25、30μM。
T62040	Tubulin polymerization-IN-30
	Tubulin polymerization-IN-30 (compound 6e) 是有效的微管蛋白聚合 (Tubulin polymerization) 抑制剂，可破坏细胞内微管组织，将细胞周期阻滞在 G2/M 期。Tubulin polymerization-IN-30 对 HeLa、SGC-7901和A549 等肿瘤细胞系具有良好的抗肿瘤活性，其IC50分别为 0.403、 2.16和2.21 μM。
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。
T76041	GIP (1-30) amide,human acetate
	GIP (1-30) amide, human acetate 为葡萄糖依赖性促胰岛素多肽（GIP）的片段，作为一种肠降血糖素激素，它能在10^-9至10^-6M的剂量范围内，依赖剂量地促进胰岛素的分泌，并有效减缓餐后血糖波动。
T38353	Pyrenocine A
	Pyrenocine A is a fungal metabolite that has been found inP. terrestrisand has diverse biological activities.1It inhibits the asexual spore germination of the plant pathogenic fungiF. oxysporum,F. solani,M. hiemalis, andR. stolonifer(EC50s = 14, 20, 20, and 25 μg/ml, respectively). Pyrenocine A is active againstB. subtilis,S. aureus, andE. coli(IC50s = 30, 45, and 200 μg/ml, respectively). It inhibits onion seedling elongation (EC50= 4 μg/ml). Pyrenocine A is also a phytotoxin that inhibits lett...
T35423	7-oxo Staurosporine
	7-oxo Staurosporine is an antibiotic originally isolated from S. platensis with diverse biological activites. It inhibits PKC, PKA, phosphorylase kinase, EGFR, and c-Src in vitro (IC50s = 9, 26, 5, 200, and 800 nM, respectively). 7-oxo Staurosporine induces cell cycle arrest in the G2/M phase in human leukemia K562 cells with a minimal effective dose (MED) of 30 ng/ml. It is cytotoxic to P388 mouse leukemia cells that are resistant and susceptible to doxorubicin . 7-oxo Staurosporine inhibits gr...
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...
T35671	Salazinic Acid
	Salazinic acid is a depsidone lichen metabolite that has been found in P. sulcata.1 It is active against B. cereus, B. subtilis, S. aureus, P. aeruginosa, S. typhimurium, C. albicans, and A. niger in vitro (MICs = 3.9-30.8 mM). Salazinic acid is cytotoxic to MM98, A431, and HaCaT cells in crystal violet (EC50s = 159, 2,870, and 48 μM, respectively) and neutral red uptake assays (EC50s = 1,925, 1,913, and 907 μM, respectively).2 It increases the wound closure rate in scratch-wounded HaCaT monolay...
T36291	Integrin modulator 1
	Integrin modulator 1 is a potent and selective α4β1 integrin agonist, with an IC50 of 9.8 nM for RGD-binding α4β1. Integrin modulator 1 increases cell adhesion mediated by α4β1 integrin, with an EC50 of 12.9 nM[1]. Integrin modulator 1 (2-10 μg/mL; 30 min) significantly increases Jurkat E6.1 cell adhesion[1].Integrin modulator 1 (1-100 nM; 1 h) strongly and significantly increases ERK1/2 phosphorylation in Jurkat E6.1 cells[1].Integrin modulator 1 (1 nM-10 μM; 30 min) significantly increases the...
T83898	S-(N-Methylsulfinylbutylthiocarbamoyl)-L-cysteine SFN-Cys,D,L-Sulforaphane-L-cysteine
	S-(N-Methylsulfinylbutylthiocarbamoyl)-L-cysteine (SFN-Cys) 是一种异硫氰酸酯衍生物及第一类和第二类组蛋白去乙酰化酶（HDAC）抑制剂和抗癌剂硫代硫酸烯醇醚的活性代谢产物。它通过巯基乙酸途径酶从硫代硫酸烯醇醚经DL-硫代硫酸烯醇醚谷胱甘肽和硫代硫酸烯醇醚半胱氨酸甘肽中间体形成。SFN-Cys (20 µM) 通过创伤愈合和腔室分析实验，分别减少了U87MG和U373 MG胶质母细胞瘤细胞的侵袭和迁移。在45 µM的浓度下，它降低了对紫杉醇耐药的A549肺癌细胞（A549/T）中的α-微管蛋白、βIII-微管蛋白、司他敏1和X连锁抑制剂的凋亡（XIAP）的水平，并减少了细胞密度。使用30 µM浓度的SFN-Cys诱导U87MG和U373 MG细胞凋亡和G2/M期细胞周期停滞。
T37800	PF-04449613
	PF-04449613 is a phosphodiesterase 9A (PDE9A) inhibitor (IC50= 22 nM).1It is selective for PDE9A over PDE1C (IC50= >1,000 nM), as well as over a variety of other PDEs, inhibiting PDE2-8, -10, and -11 activity by less than 30% in a panel of enzymes, ion channels, and transporters at 1 μM but does inhibit the human dopamine transporter (DAT; Ki= 293 nM). PF-04449613 (0.1-100 mg/kg, s.c.) increases cerebrospinal fluid (CSF) levels of cyclic GMP (cGMP) in rats. Subcutaneous administration of PF-0444...
T38297	Ribavirin-13C5 Ribavirin-13C5
	Ribavirin-13C5is intended for use as an internal standard for the quantification of ribavirin by GC- or LC-MS. Ribavirin is an antiviral guanosine nucleoside analog.1,2Upon entry into cells, ribavirin is metabolized to an active triphosphate form that induces viral RNA chain termination and inhibits viral polymerases. It reduces replication in a panel of seven RNA and four DNA viruses in Vero cells (EC50s = 2-95 μg/ml).3Ribavirin also reduces replication of severe acute respiratory syndrome coro...
T35772	Emestrin
	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...
T37702	Pancuronium (bromide hydrate)
	Pancuronium is an aminosteroid antagonist of muscle-type nicotinic acetylcholine receptors (nAChRs) with an IC50value of 14.8 nM using patch clamp electrophysiology in BOSC23 cells expressing mouse nAChRs.1It acts as a non-depolarizing neuromuscular blocking agent.2Pancuronium enhances anesthesia induced by isoflurane , reducing immobilization with an ED50value of 1.62 μg/kg.3 1.Liu, M., and Dilger, J.P.Site selectivity of competitive antagonists for the mouse adult muscle nicotinic acetylcholin...
T38274	Papyracillic Acid
	Papyracillic acid is a fungal metabolite and a derivative of penicillic acid originally isolated fromL. papyraceumand has antibiotic, antifungal, and phytotoxic activities.1,2It is active against the bacteriaX. campestrisandB. subtilisand the fungusC. tropicalisin a disc assay when used at a concentration of 5 μg/disc.2Papyracillic acid (1 mg/ml) induces necrotic lesion formation in a panel of 10 plants. 1.Shan, R., Anke, H., Stadler, M., et al.Papyracillic acid, a new penicillic acid analogue f...
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...
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 ...
T35893	rac-1,2-bis-Palmitoyl-3-chloropropanediol
	rac-1,2-bis-Palmitoyl-3-chloropropanediol is a 3-monochloropropane-1,2-diol (3-MCPD) ester.1It has been found as a contaminant in edible olive oils, with the lowest and highest concentrations in extra virgin and olive pomace oils, respectively.rac-1,2-bis-Palmitoyl-3-chloropropanediol has also been found in cottonseed and palm oils, as well as in shortening.2It induces renal tubular necrosis and a decrease in spermatids, but no gross pathological changes, in mice.3 1.Hung, W.-C., Peng, G.-J., Ts...
T36321	C6 Urea Ceramide
	C6 urea ceramide is an inhibitor of neutral ceramidase.1 It increases total ceramide levels in wild-type mouse embryonic fibroblasts (MEFs) and in HT-29 colon cancer cells but not in MEFs lacking neutral ceramidase. It inhibits proliferation of, and induces apoptosis and autophagy in HT-29, but not non-cancerous RIE-1, cells when used at concentrations of 5 and 10 μM. C6 urea ceramide decreases total β-catenin, increases phosphorylated β-catenin, and induces colocalization of β-catenin with the ...
T35790	Palmitic acid-1,2,3,4-13C4 Palmitic Acid-13C (C1, C2, C3, and C4 labeled)
	Palmitic acid-13C (C1, C2, C3, and C4 labeled) is intended for use as an internal standard for the quantification of palmitic acid by GC- or LC-MS. Palmitic acid is a common 16-carbon saturated fat that represents 10-20% of human dietary fat intake and comprises approximately 25 and 65% of human total plasma lipids and saturated fatty acids, respectively.1,2Acylation of palmitic acid to proteins facilitates anchoring of membrane-bound proteins to the lipid bilayer and trafficking of intracellula...
T36717	RWJ-56110 dihydrochloride
	RWJ-56110 dihydrochloride is a potent, selective, peptide-mimetic inhibitor of PAR-1 activation and internalization (binding IC50=0.44 uM) and shows no effect on PAR-2, PAR-3, or PAR-4. RWJ-56110 dihydrochloride inhibits the aggregation of human platelets induced by both SFLLRN-NH2 (IC50=0.16 μM) and thrombin (IC50=0.34 μM), quite selective relative to U46619 . RWJ-56110 dihydrochloride blocks angiogenesis and blocks the formation of new vessels in vivo. RWJ-56110 dihydrochloride induces cell ap...
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 ...

化合物

MAO-IN-M30 dihydrochloride

Cat.No: T38034

Synonym: M 30 dihydrochloride

Target: Monoamine Oxidase

Cat.No: T71857

Target: FLT, Tyrosine Kinases

Rigosertib sodium

Cat.No: T5818

Synonym: Rigosertib,Estybon,ON-01910

Target: Apoptosis, PLK, PI3K

Suc-AAP-Abu-pNA

Cat.No: T36351

Cat.No: T80300

Target: Antibiotic

Tubulin polymerization-IN-30

Cat.No: T62040

Cat.No: T36674

Target: Apoptosis, ERK

GIP (1-30) amide,human acetate

Cat.No: T76041

Cat.No: T38353

7-oxo Staurosporine

Cat.No: T35423

Cat.No: T35485

Cat.No: T35671

Integrin modulator 1

Cat.No: T36291

S-(N-Methylsulfinylbutylthiocarbamoyl)-L-cysteine

Cat.No: T83898

Synonym: SFN-Cys,D,L-Sulforaphane-L-cysteine

Cat.No: T37800

Cat.No: T38297

Synonym: Ribavirin-13C5

Cat.No: T35772

Pancuronium (bromide hydrate)

Cat.No: T37702

Papyracillic Acid

Cat.No: T38274

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

Cat.No: T35451

Cat.No: T36695

rac-1,2-bis-Palmitoyl-3-chloropropanediol

Cat.No: T35893

C6 Urea Ceramide

Cat.No: T36321

Palmitic acid-1,2,3,4-13C4

Cat.No: T35790

Synonym: Palmitic Acid-13C (C1, C2, C3, and C4 labeled)

RWJ-56110 dihydrochloride

Cat.No: T36717

Cat.No: T36084

Cat. No.	Product Name	Target	Signaling Pathways
T15277	Fervenulin	Parasite	Microbiology/Virology
	Fervenulin 具有杀灭线虫活性，抑制线虫M. incognita 卵孵化和 J2 的校正死亡率，MIC 分别为 30 μg/mL 和 120 μg/mL。
TN5639	Rocaglaol Ferrugin,Aglaiastatin A
	Rocaglaol is a potent anticancer drug that induces apoptosis of LNCaP cells through the mitochondrial pathway and its G2/M-phase cell cycle arrest is associated with the down-regulation of Cdc25C and the dephosphorylation of Cdc2. Rocaglaol can reduce tis

天然产物

Cat.No: T15277

Target: Parasite

Cat.No: TN5639

Synonym: Ferrugin,Aglaiastatin A

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