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33

抑制剂 & 化合物

4

天然产物

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Cat. No.	Product Name	Target	Signaling Pathways
TP1432	Enfuvirtide acetate 醋酸恩夫韦地	HIV Protease	Microbiology/Virology; Proteases/Proteasome
	Enfuvirtide acetate 是一种抗HIV-1融合的抑制肽，是一种由 36 个氨基酸组成的线性合成肽。它具有乙酰化的 N 端和羧酰胺 C 端。
T8796	CAN508	CDK	Cell Cycle/Checkpoint
	CAN508 是一种有效的 ATP 竞争性 CDK9/cyclin T1 抑制剂，IC50 为 0.35 μM。它还是 Cdk2-cyclin E 对 ATP 的竞争性抑制剂，Ki 和 IC50 值分别为 13.3 和 20 µM。它对 CDK9/cyclin T 的选择性是其他 CDK/cyclin 复合物的 38 倍，有抗肿瘤活性。
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。
T36944	Ara-G	Nucleoside Antimetabolite/Analog	Cell Cycle/Checkpoint; DNA Damage/DNA Repair
	Ara-G 是一种脱氧鸟苷 (GdR) 类似物和核苷类似物，可被 T 淋巴谱系细胞迅速转化为其相应的阿拉伯糖基鸟嘌呤核苷酸三磷酸 (araGTP)，从而抑制 DNA 合成和对 T 淋巴母细胞的选择性体外毒性细胞系以及来自 T 细胞急性淋巴细胞白血病 (ALL) 患者的新鲜分离的白血病细胞。
T36696	DMBA
	7,12-Dimethylbenz[a]anthracene (DMBA) is a polycyclic aromatic hydrocarbon (PAH) that has been found in tobacco smoke and diesel exhaust and has carcinogenic activity.1,2It undergoes metabolic activation by numerous enzymes, including the cytochrome P450 (CYP450) isoform CYP1B1, as well as microsomal epoxide hydrolase (mEH), producing a variety of reactive metabolites that form DNA adductsin vivo, and it has been commonly used to induce tumor formation in various rodent models.2,3,1DMBA increase...
T35610	2,5-dimethyl Celecoxib	Apoptosis; Wnt/beta-catenin; Prostaglandin Receptor	Apoptosis; Cytoskeletal Signaling; GPCR/G Protein; Immunology/Inflammation; Stem Cells
	2,5-dimethyl Celecoxib 是塞来昔布衍生物和微粒体前列腺素 E 合酶 1 (mPGES-1) 的靶向抑制剂，mPGES-1 是炎症介质 PGE2 合成途径中的关键酶。
T83024	Antiparasitic agent-20	Parasite	Microbiology/Virology
	Antiparasitic agent-20 (Compound 1p) 是一种抗寄生虫剂，对T. brucei和T. cruzi展现出显著效力，其EC50值分别为0.09 μM和14.1 μM，表现出其广泛的抗寄生虫活性。
T32660	Leucanicidin
	Leucanicidin is a macrolide bacterial metabolite originally isolated from S. halstedii. It is toxic to L. separata fourth instar larvae when used at a concentration of 20 ppm and to H. contortus, T. colubriformis, and O. circumcincta larvae (LD50s = 0.23-
TP1515	HPV16-E711-20 epitope
	HPV16-E711-20 epitope is a well-known HLA-A*0201-restricted human cytotoxic T lymphocyte (CTL) epitope of the HPV16 E7 protein that shows high-affinity binding to HLA-A2 in vitro.
T39200	β-catenin-IN-37
	β-Catenin-IN-37 is a selective inhibitor of the protein-protein interaction between β-Catenin and T-cell factor (Tcf), known as β-catenin/Tcf PPI. It effectively inhibits canonical Wnt signaling and impedes the growth of colorectal cancer cells SW480 and HCT116, with IC50 values of 20 μM and 31 μM, respectively.
T37757	Tyvelose
	Tyvelose is an unusual 3,6-dideoxyhexose terminal sugar and the immunodominant component of glycoprotein antigens in the parasitic helminth T. spiralis, which is responsible for trichinosis in humans. It is produced in high amounts by the infective larva and is immunodominant during the muscle stage of infection. Mice immunized with tyvelose-BSA produce IgG1 antibodies to tyvelose but are not resistant to infection by T. spiralis. Tyvelose-specific antibodies (2.5 mg/20 g) administered to rat pu...
T79533	PDE5-IN-10
	PDE5-IN-10 (compound 4b)，一有效PDE5抑制剂，IC50值为20 nM。该化合物体外微粒体稳定性增强（t1/2= 44.6 分钟），在长期增强恢复方面效果显著，适用于阿尔茨海默病（AD）研究。
T83724	TPP-1 hydrochloride Targeting PD-L1 Peptide
	TPP-1是一种针对程序化细胞死亡蛋白1(PD-1)及其配体PD-1配体(PD-L1)之间蛋白-蛋白相互作用的肽抑制剂。它在无细胞实验中结合到PD-L1(Kd = 94.67 nM)。TPP-1 (20 µM)能逆转PD-L1在抗CD3激活的人类CD4+ T细胞中所引起的干扰素γ(IFN-γ)水平的下降。在使用HL-60白血病细胞与抗CD3激活的人类CD4+ T细胞共培养并在植入前预处理时，以4 mg/kg的剂量给药，可减少小鼠异种移植模型中的肿瘤体积。
T37692	Piericidin B
	Piericidin B is a bacterial metabolite that has been found inS. mobaraensisand has insecticidal and antimicrobial activities.1,2,3It inhibits NADH oxidase activity in isolated bovine heart mitochondria and inhibits respiration in isolated rat liver mitochondria and isolated cockroach (P. americana) muscle mitochondria.2,3Topical application of piericidin B (4 μg/insect) induces mortality in 87.5% of houseflies (M. domestica).1It induces 93.3, 100, and 100% mortality in rice stem borer (C. simple...
T72213	Efonidipine hydrochloride NZ-105 hydrochloride
	Efonidipine(NZ-105)盐酸盐是T 型和L 型钙离子通道双重阻断剂。
T35978	Benastatin A
	Benastatin A is a polyketide synthase-derived benastatin that has been found inStreptomycesand has diverse biological activities.1,2,3It inhibits glutathione S-transferase (GST; Ki= 5 μM for the rat liver enzyme).2Benastatin A is active against several bacteria, including methicillin-resistantS. aureus(MRSA; MIC = 3.12 μg/ml). It induces apoptosis and cell cycle arrest at the G1/G0phase in Colon 26 mouse colon cancer cells when used at concentrations of 20 and 16 μM, respectively.3 1.Xu, Z., Sch...
T37468	Siamycin I
	Siamycin I is a tricyclic peptide originally isolated from Streptomyces and has antiviral and antibacterial activities. It is active against laboratory strains and clinical isolates of HIV-1 (ED50s = 0.05-0.45 and 0.89-5.7 μM, respectively), as well as the CBL-20 strain of HIV-2 (ED50 = 0.45 μM), in vitro. Siamycin I inhibits HIV-induced fusion of C8166 T cells with HIV-1-infected CEM-SS cells with an ED50 value of 0.08 μM. It is also active against B. subtilis, M. luteus, and S. aureus (MICs = ...
T35940	Darinaparsin Dimethylarsinic glutathione,Darinaparsin
	Darinaparsin is a dimethylated arsenic linked to glutathione. It is cytotoxic to DU145, LNCaP, and PC3 prostate cancer cells (IC50s = 5-10 &#181M) and patient-derived primary prostate cancer cells (IC50s = 2.5-20 &#181M), as well as Jurkat T cell lymphoma and L540 Hodgkin lymphoma cells (IC50s = 2.7 and 1.3 &#181M, respectively). [1][2] It decreases the tumor-initiating subpopulation in DU145 and PC3 cells and halts the cell cycle in the G2/M phase. Darinaparsin decreases transcription of Gli-2,...
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,...
T36706	Bottromycin A2
	Bottromycin A2is an antibiotic originally isolated fromStreptomyces.1It blocks the binding of aminoacyl-tRNA to the A site of the 50S ribosome, inhibiting protein synthesis.2Bottromycin A2is active against clinical isolates of methicillin-resistantStaphylococcus aureus(MRSA) and vancomycin-resistantEnterococciwith MIC values of 1 and 0.5 μg/ml, respectively. 1.Nakamura, S., Yajima, T., Lin, Y., et al.Isolation and characterization of bottromycins A2, B2, C2J. Antibiot. (Tokyo)20(1)1-5(1967) 2.Go...
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。
T35892	Q134R Q134R
	Q134R, a neuroprotective hydroxyquinoline derivative that suppresses nuclear factor of activated T cell (NFAT) signaling. Q134R can across blood-brain barrier. Q134R has the potential for Alzheimer’s disease (AD) and aging-related disorders research[1]. Q134R (1-10 μM) suppresses NFAT signaling, without inhibiting calcineurin activity. Q134R partially inhibits NFAT activity in primary rat astrocytes, but does not prevent calcineurin-mediated dephosphorylation of a non-NFAT target, either in vivo...
T35428	β-Rubromycin
	β-Rubromycin is a bacterial metabolite originally isolated from Streptomyces that has diverse biological activities.1 It inhibits the growth of HMO2, KATO-III, and MCF-7 cells with GI50 values of 0.5, 0.84, and <0.1 μM, respectively. β-rubromycin inhibits HIV-1 reverse transcriptase activity by 39.7% when used at a concentration of 10 μM. It also has antibacterial activity against Gram-positive bacteria. The structure of β-rubromycin was originally described as containing an ortho-quinone group,...
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....
T36668	Geranylgeranoic Acid
	Geranylgeranoic acid (GGA) is an isoprenoid that has been found inS. chinensisand has anticancer activity.1It induces apoptosis in Huh7 and PLC/PRF/5 human hepatoma cells and MLE-10 transformed mouse hepatocytes, but not primary mouse hepatocytes, when used at concentrations ranging from 1 to 20 μM. GGA (10 μM) induces apoptosis in Huh7 cellsvialoss of the mitochondrial membrane potential and activation of interleukin-1β-converting enzyme (ICE) and cysteine protease precursor 32 (CPP32).2It also...
T35680	2-(1-(Thiophen-2-yl)ethylidene)hydrazinecarbothioamide
	2-(1-(Thiophen-2-yl)ethylidene)hydrazinecarbothioamide is an antimicrobial agent.1It is active against the Gram-negative bacteriaE. coli,P. aeruginosa, andS. marcescens(MICs = 64, 100, and 70 μg/ml, respectively), the Gram-positive bacteriaS. aureus,M. luteus, andB. cereus(MICs = 130, 100, and 50 μg/ml, respectively), and the fungiC. albicans,G. candidum,T. rubrum,F. oxysporum,A. flavus, andS. brevicaulis(MICs = 69-120 μg/ml). 2-(1-(Thiophen-2-yl)ethylidene)hydrazinecarbothioamide is also a prec...
T37431	ENPP1 Inhibitor C ENPP1 Inhibitor C
	ENPP1 inhibitor C is an inhibitor of ectonucleotide pyrophosphatase/phosphodiesterase 1 (ENPP1; IC50 = 0.26 μM in a cell-free assay).1 It is selective for ENPP1 over ENPP2-7 at 10 μM. ENPP1 inhibitor C decreases ENPP1 activity in MDA-MB-231 human breast and C6 rat glioma cancer cells when used at a concentration of 10 μM. \|1. Kawaguchi, M., Han, X., Hisada, T., et al. Development of an ENPP1 fluorescence probe for inhibitor screening, cellular imaging, and prognostic assessment of malignant brea...
T21558	MK-3207
	MK-3207是口服生物相容性的CGRP 受体拮抗剂，IC50和 Ki 分别为 0.12 nM 和 0.024 nM，对 AM1，AM2，CTR 和 AMY3 的抑制性较弱。MK-3207可用于偏头痛研究。
T36570	KUS121
	KUS121 is a valosin-containing protein (VCP) modulator that inhibits VCP ATPase activity (IC50= 330 nM).1It inhibits cell death, ATP depletion, and upregulation of C/EBP-homologous protein (CHOP) induced by tunicamycin, an inducer of ER stress, in HeLa cells when used at concentrations of 20, 50, and 50 μM, respectively. KUS121 (100 μM) inhibits ATP depletion and cell death induced by oxygen-glucose deprivation (OGD) in rat primary cortical neurons in anin vitromodel of cerebral ischemia.2It red...
T36176	AMK (hydrochloride)
	AMK is an active metabolite of the neurohormone melatonin .1,2,3,4It is formed from melatoninviathe metabolic intermediate AFMK that is then deformylated by catalase or formamidase.5,6AMK scavenges singlet oxygenin vitrowhen used at a concentration of 200 μM.1It inhibits the epinephrine- and arachidonic acid-induced production of prostaglandin E2and PGD2in ovine seminal vesicle microsomes in a concentration- and time-dependent manner, as well as LPS-induced increases in COX-2 levels in RAW 264.7...
T35789	Palmitic acid-1-13C
	Palmitic acid-13C is intended for use as an internal standard for the quantification of palmitic acid by GC- or LC-MS. Palmitic acid is a 16-carbon saturated fatty acid. It comprises approximately 25% of human total plasma lipids.1 It increases protein levels of COX-2 in RAW 264.7 cells when used at a concentration of 75 μM.2 Palmitic acid is involved in the acylation of proteins to anchor membrane-bound proteins to the lipid bilayer.2,3,4,5,6 \|1. Santos, M.J., López-Jurado, M., Llopis, J., et a...
T35791	Palmitic acid-13C
	Palmitic acid-13C is intended for use as an internal standard for the quantification of palmitic acid by GC- or LC-MS. Palmitic acid-13C contains 13C at the C2 position and has been used in the study of free fatty acid incorporation into phospholipid fatty acids in soil microbes.1 Palmitic acid is a 16-carbon saturated fatty acid. It comprises approximately 25% of human total plasma lipids.2 It increases protein levels of COX-2 in RAW 264.7 cells when used at a concentration of 75 μM.3 Palmitic ...
T35698	Octanoic Acid-13C
	Octanoic acid-13C is intended for use as an internal standard for the quantification of octanoic acid by GC- or LC-MS. Octanoic acid is a medium-chain saturated fatty acid. It has been found in Teleme cheeses made from goat, ovine, or bovine milk.1 Octanoic acid is active against the bacteria S. mutans, S. gordonii, F. nucleatum, and P. gingivalis (IC80s = <125, <125, 1,403, and 2,294 μM, respectively).2 Levels of octanoic acid are increased in the plasma of patients with medium-chain acyl-CoA d...

化合物

Enfuvirtide acetate

Cat.No: TP1432

Synonym: 醋酸恩夫韦地

Target: HIV Protease

Cat.No: T8796

Target: CDK

Cat.No: T1846

Synonym: Y320

Target: IL Receptor, Lipase, Interleukin

Cat.No: T36944

Target: Nucleoside Antimetabolite/Analog

Cat.No: T36696

2,5-dimethyl Celecoxib

Cat.No: T35610

Target: Apoptosis, Wnt/beta-catenin, Prostaglandin Receptor

Antiparasitic agent-20

Cat.No: T83024

Target: Parasite

Cat.No: T32660

HPV16-E711-20 epitope

Cat.No: TP1515

β-catenin-IN-37

Cat.No: T39200

Cat.No: T37757

Cat.No: T79533

TPP-1 hydrochloride

Cat.No: T83724

Synonym: Targeting PD-L1 Peptide

Cat.No: T37692

Efonidipine hydrochloride

Cat.No: T72213

Synonym: NZ-105 hydrochloride

Cat.No: T35978

Cat.No: T37468

Cat.No: T35940

Synonym: Dimethylarsinic glutathione,Darinaparsin

Cat.No: T38381

Cat.No: T36706

S-(N-Methylsulfinylbutylthiocarbamoyl)-L-cysteine

Cat.No: T83898

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

Cat.No: T35892

Synonym: Q134R

Cat.No: T35428

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

Cat.No: T37370

Geranylgeranoic Acid

Cat.No: T36668

2-(1-(Thiophen-2-yl)ethylidene)hydrazinecarbothioamide

Cat.No: T35680

ENPP1 Inhibitor C

Cat.No: T37431

Synonym: ENPP1 Inhibitor C

Cat.No: T21558

Cat.No: T36570

AMK (hydrochloride)

Cat.No: T36176

Palmitic acid-1-13C

Cat.No: T35789

Palmitic acid-13C

Cat.No: T35791

Octanoic Acid-13C

Cat.No: T35698

Cat. No.	Product Name	Target	Signaling Pathways
T73072	PTP1B-IN-20
	PTP1B-IN-20 是蛋白酪氨酸磷酸酶 1B (PTP1B) 的选择性抑制剂 (IC50=1.05 μM)，抑制力超出高度同源 T 细胞蛋白酪氨酸磷酸酶 (TCPTP；IC50=78.0 μM)，PTP1B 是抑制 2 型糖尿病的重要靶点。
T37609	(rel)-Asperparaline A
	Aspergillimide is a fungal metabolite originally isolated from A. japonicus.1 It reduces nicotinic acetylcholine receptor (nAChR) peak and slowly-desensitizing amplitudes induced by acetylcholine in silkworm (B. mori) larval neurons (IC50s = 20.2 and 39.6 nM, respectively) but has no effect on chicken α3β4-, α4β2-, and α7-containing nAChRs.2 Dietary administration of aspergillimide A (10 μg/g of diet) induces paralysis in silkworm fourth instar larvae.1 Aspergillimide A (10 and 20 mg/kg) reduces...
T35750	Trypacidin
	Trypacidin is a fungal metabolite originally isolated fromA. fumigatus.1It is active againstB. subtilisandM. bovis(MICs = 12.5 and 1.25 μg/ml, respectively), as well asT. cruziandT. gondii(MICs = 5-10 and 10-20 μg/ml, respectively).1,2It reduces viability and induces lysis of A549 human lung cancer cells (IC50s = 7.4 μM for both).3Trypacidin increases survival in a mouse model ofT. gondiiinfection when administered in six doses of 12.5 mg/kg each.1 1.Balan, J., Ebringer, L., Nemec, P., et al.Ant...
T36348	Cerebroside C
	Cerebroside C is a fungal metabolite and glycosphingolipid that has been found in the rice pathogenic fungusM. grisea.1It induces production of the phytoalexin momilactone A when applied to wounded rice leaves, indicating that cerebroside C is an elicitor of the hypersensitive response in rice. Cerebroside C increases germination rate and reduces germination time in wheat seeds in a concentration-dependent manner at 4°C.2It also increases root length, fresh weight, and dry weight of wheat seedli...

天然产物

Cat.No: T73072

(rel)-Asperparaline A

Cat.No: T37609

Cat.No: T35750

Cat.No: T36348

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