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22

抑制剂 & 化合物

8

天然产物

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Cat. No.	Product Name	Target	Signaling Pathways
T16133	MRK-560	Gamma-secretase	Neuroscience; Proteases/Proteasome; Stem Cells
	MRK-560 是高效的、口服有效的 γ- 分泌酶抑制剂抑制剂，具有大脑屏障渗透性。
T3977	Lifitegrast SHP-606,SAR 1118,立他司特,利非司特	Integrin	Cytoskeletal Signaling
	Lifitegrast (SAR 1118) 是一种整合素淋巴细胞功能相关抗原 1 拮抗剂，抑制 Jurkat T 细胞附着于ICAM-1的IC50为 2.98 nM。
T6603	Nelarabine GW 506U78,Nelzarabine,奈拉滨,506U78	Apoptosis; Nucleoside Antimetabolite/Analog; DNA/RNA Synthesis	Apoptosis; Cell Cycle/Checkpoint; DNA Damage/DNA Repair
	Nelarabine (GW 506U78) 是一种嘌呤核苷酸类似物，为DNA 合成抑制剂，对肿瘤细胞的IC50为0.067-2.15 μM，可作用于T 细胞急性淋巴细胞白血病。
T0370	Pheniramine maleate Daneral,Inhiston,Trimetose,马来酸非尼拉敏	5-HT Receptor; Histamine Receptor	GPCR/G Protein; Immunology/Inflammation; Neuroscience
	Pheniramine maleate (Trimetose) 是一种具有抗组胺和血管扩张特性的烷基胺衍生物，可与组胺 H1 受体结合，从而抑制磷脂酶 A2 和内皮源性松弛因子一氧化氮的产生。
T64387	2-Nitrobenzoic acid o-Nitrobenzoic acid	Others	Others
	2-Nitrobenzoic acid (o-Nitrobenzoic acid) 是一种抗增殖化合物，对表达 T 型钙通道α1H 或其剪接变体δ25的 jurkat 细胞系显示出8.3μM 的 IC50。
T35569	CTA 056	Apoptosis	Apoptosis
	CTA 056 是白细胞介素-2 诱导的 T 细胞激酶（ITK）抑制剂，抑制小鼠 MOLT-4 异种移植肿瘤的生长，诱导 Jurkat 细胞凋亡，可用于研究自身免疫性疾病和T细胞恶性肿瘤。
T10565	BMS-1001 hydrochloride	PD-1/PD-L1	Apoptosis; Cell Cycle/Checkpoint; Immunology/Inflammation
	BMS-1001 hydrochloride 是一种人 PD-L1/PD-1免疫检查点的抑制剂，具有口服活性且细胞毒性低。
T24816	SP-100030 SP100030,SP 100030	NF-κB	NF-κB
	SP-100030 是一种有效的 NF-κB 和激活蛋白-1 (AP-1) 双抑制剂 (IC50 分别为 50 和 50 nM)。SP-10003 抑制 Jurkat 和其他T 细胞系产生的 IL-2、IL-8 和 TNF-α 的产生。SP-100030 降低小鼠胶原性关节炎 (CIA)。
T12203L	Necrostatin 2	Others	Others
	Necrostatin 2 is an effective necroptosis inhibitor. Necrostatin 2 is also a RIPK1 inhibitor. EC50 for inhibition of necroptosis in FADD-deficient Jurkat T cells treated with TNF-α is 0.05 μM.
T80497	KTX-Sp2	Potassium Channel	Membrane transporter/Ion channel
	KTX-Sp2为钾通道毒素，能高效阻断三种外源电压门控钾通道Kv1.1、Kv1.2和Kv1.3。该化合物还能抑制内源性Kv1.3通道，降低Jurkat T细胞内Ca2+信号并抑制其活化后的IL-2分泌。
T39342	4-Maleimidosalicylic acid
	4-Maleimidosalicylic acid is a polar maleimide compound that does not exhibit suppressive effects on IL-2 production in JURKAT T cells.
TP2101	Z-VRPR-FMK trifluoroacetate salt
	Irreversible MALT1 inhibitor. Suppresses T cell activation-induced cleavage of Bcl-10 in a dose-dependent manor. Reduces Jurkat cell adhesion to fibronectin. Cell permeable.
T35906	Padanamide A
	Padanamide A is a bacterial metabolite originally isolated from a marine Streptomyces species. It is active against five strains of P. falciparum (EC50s = 160-340 nM), is not cytotoxic to HEK293 or HepG2 human cell lines, but is cytotoxic to Jurkat T lymphocytes with an IC50 value of approximately 60 μg/ml.
T36331	Z-AEVD-FMK Z-AEVD-FMK,Z-Ala-Glu-Val-Asp-Fluoromethyl Ketone
	Z-AEVD-FMK is an irreversible inhibitor of caspase-10 and related caspases.[1] At 10 &#181M, it can prevent the initiation of Fas signaling by caspase-10 in Jurkat T lymphoma cells, preventing Bid cleavage into its active form, caspase cascade activation, and apoptosis.[2]
T79705	LP23	PD-1/PD-L1	Apoptosis; Cell Cycle/Checkpoint; Immunology/Inflammation
	LP23为非芳基甲胺类PD-1/PD-L1抑制剂(IC50：16.7 nM)，展现出抗肿瘤效果。能恢复HepG2/Jurkat T细胞的免疫功能并促进HepG2细胞凋亡。在B16-F10肿瘤模型中，LP23表现出体内活性，在剂量为30 mg/kg时TGI达到88.6%。
T74843	ITK degrader 1
	ITKdegrader 1 是一种高度选择性的白细胞介素 2 诱导的 T 细胞激酶 (ITK) 降解剂 (DC50=3.6 nM)。ITKdegrader 1 快速、持久地诱导 ITK 降解，并抑制体内抗 CD3抗体刺激的 IL-2分泌 (EC50=35.2 nM，Jurkat 细胞)。ITKdegrader 1 也显示出良好的血浆暴露水平。
T79314	PD-L1-IN-3	PD-1/PD-L1	Apoptosis; Cell Cycle/Checkpoint; Immunology/Inflammation
	PD-L1-IN-3 (Compound 4a) 是一种抑制PD-1/PD-L1途径的化合物，具有高度选择性，其PD-L1的IC50值达到4.97nM，而对Jurkat T细胞的EC50为2.70μM。该化合物能够结合至PD-L1二聚体，并有效阻止PD-1与PD-L1的相互作用，从而抑制PD-1信号传导。PD-L1-IN-3主要用于肺癌和黑色素瘤等疾病的研究领域。
T36034	CAY10774
	CAY10774 is an inhibitor of the protein-protein interaction between programmed cell death 1 (PD-1) and its ligand PD-L1 (IC50= 15 nM in a homologous time-resolved fret (HTRF) assay).1It increases the activation of Jurkat cells expressing PD-1 in co-culture with artificial antigen-presenting cells (aAPCs) expressing PD-L1 (EC50= 6.6 μM in a reporter assay). CAY10774 increases surface expression of PD-1 on primary human CD4+and CD8+T cells co-cultured with aAPCs. 1.Konieczny, M., Musielak, B., Koc...
T35775	HT-2 Toxin-13C22 HT-2 Toxin-13C22
	HT-2 toxin-13C22is intended for use as an internal standard for the quantification of HT-2 toxin by GC- or LC-MS. HT-2 toxin is a type A trichothecene mycotoxin and an active, deacetylated metabolite of the trichothecene mycotoxin T-2 toxin .1,2Like T-2 toxin, HT-2 toxin inhibits protein synthesis and cell proliferation in plants.2HT-2 toxin also reduces viability of HepG2, A549, HEp-2, Caco-2, A-204, U937, Jurkat, and RPMI-8226 cancer cells with IC50values ranging from 3.1 to 23 ng/ml and human...
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,...
T69221	BMS-554417
	BMS-554417 is a novel inhibitor of IGF-IR, which inhibits IGF-IR and insulin receptor kinase activity and proliferation in vitro, and reduces tumor xenograft size in vivo. In a series of carcinoma cell lines, the IC50 for proliferation ranged from 120 nmol/L (Colo205) to >8.5 micromol/L (OV202). BMS-554417 treatment inhibited IGF-IR and insulin receptor signaling through extracellular signal-related kinase as well as the phosphoinositide 3-kinase/Akt pathway, as evidenced by decreased Akt phosph...
T83763	EPI-X4 TFA Endogenous Peptide Inhibitor of CXCR4
	EPI-X4是一种源于人血清白蛋白408-423氨基酸的内源性肽段，是趋化因子(C-X-C基序)受体4 (CXCR4)的拮抗剂。在0.8至1,000µM的浓度范围内，EPI-X4能抑制表达CXCR4的HEK293细胞中由趋化因子(C-X-C基序)配体12 (CXCL12)诱发的钙离子动员和受体内化。EPI-X4还能抑制CXCL12诱导的Jurkat T细胞和人类CD34+造血干细胞的迁移。体内实验中，EPI-X4（16µmol/kg）在急性过敏性气道高嗜酸性粒细胞疾病的小鼠模型中减少了Cxcr4依赖的炎症细胞气道浸润。慢性肾脏病患者尿液中EPI-X4的水平增高，并与肾小球滤过率(GFR)成反比。

化合物

Cat.No: T16133

Target: Gamma-secretase

Cat.No: T3977

Synonym: SHP-606,SAR 1118,立他司特,利非司特

Target: Integrin

Cat.No: T6603

Synonym: GW 506U78,Nelzarabine,奈拉滨,506U78

Target: Apoptosis, Nucleoside Antimetabolite/Analog, DNA/RNA Synthesis

Pheniramine maleate

Cat.No: T0370

Synonym: Daneral,Inhiston,Trimetose,马来酸非尼拉敏

Target: 5-HT Receptor, Histamine Receptor

2-Nitrobenzoic acid

Cat.No: T64387

Synonym: o-Nitrobenzoic acid

Target: Others

Cat.No: T35569

Target: Apoptosis

BMS-1001 hydrochloride

Cat.No: T10565

Target: PD-1/PD-L1

Cat.No: T24816

Synonym: SP100030,SP 100030

Target: NF-κB

Cat.No: T12203L

Target: Others

Cat.No: T80497

Target: Potassium Channel

4-Maleimidosalicylic acid

Cat.No: T39342

Z-VRPR-FMK trifluoroacetate salt

Cat.No: TP2101

Cat.No: T35906

Cat.No: T36331

Synonym: Z-AEVD-FMK,Z-Ala-Glu-Val-Asp-Fluoromethyl Ketone

Cat.No: T79705

Target: PD-1/PD-L1

Cat.No: T74843

Cat.No: T79314

Target: PD-1/PD-L1

Cat.No: T36034

HT-2 Toxin-13C22

Cat.No: T35775

Synonym: HT-2 Toxin-13C22

Cat.No: T35940

Synonym: Dimethylarsinic glutathione,Darinaparsin

Cat.No: T69221

Cat.No: T83763

Synonym: Endogenous Peptide Inhibitor of CXCR4

Cat. No.	Product Name	Target	Signaling Pathways
T9503	PHYTOSPHINGOSINE	Apoptosis	Apoptosis
	Phytosphingosine 是具有抗癌作用的一种磷脂。在癌细胞中，它通过 caspase 8 的激活和 Bax 转位诱导细胞凋亡。
TL0013	Heraclenin 独活内酯	Anti-infection; Immunology/Inflammation related	Immunology/Inflammation; Microbiology/Virology
	Heraclenin 是一种天然呋喃香豆素。它浓度依赖性的靶向激活的 T 细胞核因子 (NFAT) ，抑制人原代 T 细胞中 T 细胞受体介导的增殖。
T5320	Tulipalin A α-methylene-γ-butyrolactone,2-Methylenebutyrolactone,2-甲烯基丁内酯	Others; Drug Metabolite	Metabolism; Others
	Tulipalin A (α-methylene-γ-butyrolactone) 是来源于郁金香鳞茎的有毒糖苷。Tulipalin A 是引起过敏性接触皮炎的致敏性致敏物 (causative allergen)，在低剂量影响免疫细胞的功能，例如 Jurkat T 细胞。
TN3734	Cuspidiol	Others	Others
	Cuspidiol shows cytotoxicity against Jurkat T cell clone E6.1 at 7.3 ug/mL.
T14003	15-Acetoxyscirpenol	Caspase	Apoptosis; Proteases/Proteasome
	15-Acetoxyscirpenol, a member of the acetoxyscirpenol moiety mycotoxins (ASMs), potently induces apoptosis and inhibits the growth of Jurkat T cells in a dose-dependent manner. This effect is mediated through the activation of caspases independent of caspase-3[1].
T36961	Malformin C
	Malformin C is a natural fungus-derived bicyclic pentapeptide that has antibacterial properties, particularly against species of Bacillus. Malformin C potently blocks the ability of bleomycin to induce G2 arrest in human T-cell leukemia-derived Jurkat cells (IC50 = 0.9 nM). It less potently abrogates colchicine-induced M phase arrest in Jurkat cells (IC50 = 24 nM). Malformin C inhibits cell growth dose-dependently in Colon 38 and HCT 115 cancer cells (IC50s = 0.27 and 0.18 μM, respectively) but ...
TN5880	Mesuol
	Mesuol has antioxidant activity, it shows very high scavenging activity against DPPH radical; it also has immunomodulatory activity, can potentiate percentage neutrophil adhesion in neutrophil adhesion test in rats and phagocytosis in carbon clearance assay. Mesuol can suppress HIV-1 replication in Jurkat T cells, it inhibits TNFα-induced HIV-1-LTR transcriptional activity by targeting the nuclear factor-κB (NF-κB) pathway.
T35741	Gliovirin
	Gliovirin is a fungal metabolite that has been found inT. harzianumand has fungicidal, antimicrobial and anti-inflammatory activities.1It is active against the plant pathogenic fungusP. ultimum(MIC = 60 ng/ml) and the parasiteT. brucei brucei(IC50= 90 ng/ml), but has no effect on the plant pathogenic fungiR. solani,P. omnivorum,T. basicola,R. arrhizus, andV. dahliaeor the bacteriaB. thuringiensis,P. fluorescens, andX. malvacearumwhen used at concentrations up to 1,000 ng/ml.2,3Gliovirin decrease...

天然产物

PHYTOSPHINGOSINE

Cat.No: T9503

Target: Apoptosis

Cat.No: TL0013

Synonym: 独活内酯

Target: Anti-infection, Immunology/Inflammation related

Cat.No: T5320

Synonym: α-methylene-γ-butyrolactone,2-Methylenebutyrolactone,2-甲烯基丁内酯

Target: Others, Drug Metabolite

Cat.No: TN3734

Target: Others

15-Acetoxyscirpenol

Cat.No: T14003

Target: Caspase

Cat.No: T36961

Cat.No: TN5880

Cat.No: T35741

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