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Search Results for " thp-10 "

Targets Recommended: Others

20

抑制剂 & 化合物

4

重组蛋白

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Cat. No.	Product Name	Target	Signaling Pathways
T9016	AI-10-47 1H-Benzimidazole, 2-(2-pyridinyl)-6-(trifluoromethoxy)-AI-10-47	Others	Others
	AI-10-47 (1H-Benzimidazole, 2-(2-pyridinyl)-6-(trifluoromethoxy)-AI-10-47) 是 CBFβ-RUNX 结合的小分子抑制剂(IC50:3.2 μM)。
T40533	THP-PEG10-THP THP-PEG10-THP	Others	Others
	THP-PEG10-THP is a PEG-based linker for PROTACs which joins two essential ligands, crucial for forming PROTAC molecules. This linker enables selective protein degradation by leveraging the ubiquitin-proteasome system within cells.
T9552	BAZ1A-IN-1	Epigenetic Reader Domain	Chromatin/Epigenetic
	BAZ1A-IN-1 是BAZ1A（含溴结构域蛋白）抑制剂(Kd:0.52 μM)。它对低表达BAZ1A 的癌细胞表现出弱活性或无活性，但对高表达BAZ1A 的癌细胞系显示出良好的抗生存作用。
T40531	THP-PEG10-OH THP-PEG10-OH	Others	Others
	THP-PEG10-OH is a PEG-based linker for PROTACs which joins two essential ligands, crucial for forming PROTAC molecules. This linker enables selective protein degradation by leveraging the ubiquitin-proteasome system within cells.
T40532	MS-PEG10-THP MS-PEG10-THP	Others	Others
	MS-PEG10-THP is a PEG-based linker for PROTACs which joins two essential ligands, crucial for forming PROTAC molecules. This linker enables selective protein degradation by leveraging the ubiquitin-proteasome system within cells.
T72615	STING modulator-4	Others	Others
	STINGmodulator-4 是一种竞争性的 STING 调节剂，对 R232HSTING 的 Ki 为 0.0933 μM。STINGmodulator-4 在 THP-1 细胞中对 p-IRF3 的 EC50为 >10 μM。
T28072	MLN-3897 AVE9897,AVE 9897,CCR1 antagonist 10,AVE-9897	CCR	Immunology/Inflammation; Microbiology/Virology
	MLN-3897 (CCR1 antagonist 10) 是一种具有口服活性的 CCR1 拮抗剂，对于 125I-MIP-1α 与 THP-1 细胞膜的结合，Ki 为 2.3 nM。 MLN-3897 抑制 Akt 信号转导和 MM 细胞存活和增殖。
T36221	2-chloro Palmitic Acid	Others	Others
	2-chloro Palmitic acid is a monochlorinated form of palmitic acid . It is produced in a myeloperoxidase (MPO) and time-dependent manner in neutrophils stimulated by phorbol 12-myristate 13-acetate . 2-chloro Palmitic acid (10 μM) induces neutrophil extracellular trap (NET) formation (NETosis) in human neutrophils, increasing DNA release from neutrophils, colocalization of MPO with extracellular DNA (ecDNA), and trapping of E. coli. It increases COX-2 protein levels in human coronary artery endot...
T38329	CU-76	Others	Others
	CU-76 is an inhibitor of cyclic GMP-AMP synthase (cGAS; IC50= 0.24 μM).1It reduces DNA-, but not Sendai virus-, induced dimerization of IFN regulatory factor 3 in THP-1 cells, indicating selectivity for the cGAS DNA sensing pathway over the RIG-I-MAVS RNA sensing pathway. CU-76 decreases IFN-stimulatory DNA-induced production of IFN-β in THP-1 cells when used at concentrations of 10, 30, and 100 μM. 1.Padilla-Salinas, R., Sun, L., Anderson, R., et al.Discovery of small-molecule cyclic GMP-AMP sy...
T38328	CU-32	Others	Others
	CU-32 is an inhibitor of cyclic GMP-AMP (cGAMP) synthase (cGAS; IC50= 0.45 μM).1It reduces DNA-, but not Sendai virus-, induced dimerization of IFN regulatory factor 3 in THP-1 cells, indicating selectivity for the cGAS DNA sensing pathway over the RIG-I-MAVS RNA sensing pathway. It is also selective for cGAS over toll-like receptors (TLRs) at 50 μM. CU-32 decreases IFN-stimulatory DNA-induced production of IFN-β in THP-1 cells when used at concentrations of 10, 30, and 100 μM. 1.Padilla-Salinas...
T63088	NOD2 antagonist 1	Others	Others
	NOD2 antagonist 1 (compound 32) 是一种有效的、选择性的 NOD2 拮抗剂 (IC50: 5.23 μM)。NOD2 antagonist 1 在 THP-1 细胞，对 Muramyl dipeptide (MDP) 诱导的 IL-8 分泌表现出抑制作用。NOD2 antagonist 1 在 PBMCs 细胞，可以抑制 MDP 诱导的 IL-6、IL-10 和 TNF-α 的水平升高。
T38159	STING Agonist 12b	Others	Others
	STING agonist 12b is an agonist of stimulator of interferon genes (STING).1It binds to STING (Kd= 26.4 μM) and induces interferon reporter gene expression in cells expressing human or mouse STING (EC50s = 7.45 and 10.23 μM, respectively). STING agonist 12b (40 μM) induces expression of TNF-a, IL-6, IP-10, and IL-1b in THP-1 cells. 1.Hou, S., Lan, X.-j., Li, W., et al.Design, synthesis and biological evaluation of acridone analogues as novel STING receptor agonistsBioorg. Chem.95103556(2020)
T38160	STING Agonist 1a	Others	Others
	STING agonist 1a is an agonist of stimulator of interferon genes (STING).1It induces expression of an IRF-inducible SEAP reporter gene in a cell-based assay (EC50= 16.77 μM). STING agonist 1a (12.5-100 μM) induces expression of IFN-β, IL-6, and chemokine (C-X-C motif) ligand 10 (CXCL10) in THP-1 cells, an effect that can be reversed by STING knockout or the STING inhibitor H-151 . 1.Hou, H., Yang, R., Liu, X., et al.Discovery of triazoloquinoxaline as novel STING agonists via structure-based vir...
T83775	STING Agonist 12L Stimulator of Interferon Genes Agonist 12L
	STING激动剂12L是一种刺激干扰素基因(STING)的激动剂。它与野生型STING结合(IC50 = 1.15 µM)，以及STING的R232、AQ和Q变体(IC50分别为1.06、0.61和1.12 µM)，并在THP-1和RAW 264.7细胞中诱导报告基因表达(EC50分别为0.38和12.94 µM)。STING激动剂12L (5 µM)在THP-1细胞中诱导IFNB1、CXCL10和IL6 mRNA的表达。在体内，STING激动剂12L (10 mg/kg)提高了血浆IFN-β水平，并且在B16/F10小鼠黑色素瘤模型中减少了肿瘤体积和肺转移灶的数量。
T38162	STING18	Others	Others
	STING18 is a competitive ligand of stimulator of interferon genes (STING; IC50 = 0.068 μM in a radioligand binding assay).1 It inhibits cGAMP-induced IFN-β production (IC50 = 11 μM) but does not stimulate IFN-β production (EC50 = >30 μM) in THP-1 cells. \|1. Siu, T., Altman, M.D., Baltus, G.A., et al. Discovery of a novel cGAMP competitive ligand of the inactive form of STING. Med. Chem. Lett. 10(1), 92-97 (2019).
T37722	Diprovocim-1	Others	Others
	Diprovocim-1 is an agonist of the toll-like receptor 1/2 heterodimer.1It induces TNF-α release in THP-1 cells (EC50= 110 pM), an effect that can be inhibited by anti-TLR1 or anti-TLR2 antibodies. Diprovocim-1 (10 mg/kg) increases the production of ovalbumin-specific IgG1 in wild-type, but notTLR2-/-, mice sensitized to ovalbumin.2It also enhances anti-PD-L1 antibody-induced activation of cytotoxic T lymphocytes, reduction of tumor growth, and increases in survival in a B16/F10 murine melanoma mo...
T36461	CAY10748 CAY10748	Others	Others
	CAY10748 is an agonist of stimulator of interferon genes (STING; IC50= 0.3794 μM in a competition binding assay).1It activates STING in STING-expressing, but not STING knockout, THP-1 cells (EC50s = 0.287 and >100 μM, respectively, in a reporter assay). It induces phosphorylation of STING at the serine in position 366, as well as phosphorylation of TBK1 and IFN regulatory factor 3 (IRF3), indicating activation of the STING-TBK1-IRF3 signaling pathway. CAY10748 increases the secretion of IFN-β an...
T83841	STING Agonist D61 D61,Stimulator of Interferon Genes Agonist D61	Others	Others
	STING激动剂D61（D61）是干扰素基因刺激剂(STING)的激动剂。它在基于细胞的分析中诱导IFN3诱导的分泌性碱性磷酸酶(SEAP)报告基因和IFN-β诱导的报告基因的表达（EC50分别为52.9和116 nM）。D61（4, 6, 和8 µM）增加了编码IFN-β和化学因子（C-X-C基序）配体10（CXCL10）的mRNA的表达以及TANK结合激酶1（TBK1）、IRF3和STING在THP-1单核细胞中的磷酸化。在体内，D61（每隔一天0.25 mg/kg）在CT26小鼠结肠癌模型中减少肿瘤体积，而不影响体重。
T83856	AP-1	Others	Others
	AP-1是一种微型化的蛋白质水解靶向嵌合体（PROTAC），由吲哚美辛（±）连接的间变性淋巴瘤激酶（ALK）配体和E3泛素连接酶配体通过超短连接器相连。在10至300 nM浓度范围内使用时，AP-1能高效降解Karpas-299细胞中高表达的ALK融合蛋白NPM-ALK，此效应可被蛋白酶体抑制剂MG-132阻断。它还能降解在SN-N-SH和NCI H3122细胞中表达的ALK融合蛋白EML4-ALK及含有苯丙氨酸至亮氨酸替换突变（ALKF1174L）的ALK。AP-1对依赖ALK的Karpas-299细胞具有细胞毒性（IC50 = 0.1265 nM），但对非ALK依赖的THP-1细胞无细胞毒性（IC50 = 2,704 nM）。在给药剂量为25, 50, 和100 mg/kg时，能减小NCI H3122小鼠移植瘤模型中的肿瘤体积。
T36996	MSA-2 dimer	Others	Others
	MSA-2 dimer is a selective, orally active non-nucleotide STING agonist (Kd=145 μM) with long-term antitumor and immunogenic activity. MSA-2 dimer is bound to STING as a non-covalent dimer exhibiting higher permeability than cyclic dinucleotide[1]. MSA-2 dimer (60 mg/kg; p.o.; 50 days) inhibits tumor growth and prolongs overall survival[1]. MSA-2 dimer (40 mg/kg; s.c.; 25 days) induces complete tumor regression[1].MSA-2 dimer (60 mg/kg; p.o.; 4 hours) increases proinflammatory cytokine (IFN-β) le...

化合物

Cat.No: T9016

Synonym: 1H-Benzimidazole, 2-(2-pyridinyl)-6-(trifluoromethoxy)-AI-10-47

Target: Others

THP-PEG10-THP

Cat.No: T40533

Synonym: THP-PEG10-THP

Target: Others

Cat.No: T9552

Target: Epigenetic Reader Domain

Cat.No: T40531

Synonym: THP-PEG10-OH

Target: Others

Cat.No: T40532

Synonym: MS-PEG10-THP

Target: Others

STING modulator-4

Cat.No: T72615

Target: Others

Cat.No: T28072

Synonym: AVE9897,AVE 9897,CCR1 antagonist 10,AVE-9897

Target: CCR

2-chloro Palmitic Acid

Cat.No: T36221

Target: Others

Cat.No: T38329

Target: Others

Cat.No: T38328

Target: Others

NOD2 antagonist 1

Cat.No: T63088

Target: Others

STING Agonist 12b

Cat.No: T38159

Target: Others

STING Agonist 1a

Cat.No: T38160

Target: Others

STING Agonist 12L

Cat.No: T83775

Synonym: Stimulator of Interferon Genes Agonist 12L

Cat.No: T38162

Target: Others

Cat.No: T37722

Target: Others

Cat.No: T36461

Synonym: CAY10748

Target: Others

STING Agonist D61

Cat.No: T83841

Synonym: D61,Stimulator of Interferon Genes Agonist D61

Target: Others

Cat.No: T83856

Target: Others

Cat.No: T36996

Target: Others

Species：

Expression System：

Tag：

Cat. No.	Product Name	Species	Expression System
TMPY-01751	DR3/TNFRSF25 Protein, Human, Recombinant (hFc) TRAMP,TR3,WSL-1,TNFRSF12,DR3,WSL-LR,tumor necrosis factor re...	Human	HEK293 Cells
	DR3/TNFRSF25 Protein, Human, Recombinant (hFc) is expressed in HEK293 mammalian cells with hFc tag. The predicted molecular weight is 45.9 kDa and the accession number is Q93038-10.
TMPY-02300	BIN1 Protein, Human, Recombinant (His) AMPHL,bridging integrator 1,AMPH2,SH3P9	Human	E. coli
	Amphiphysin 2, also named bridging integrator-1 (BIN1) or SH3P9, Amphiphysin2/BIN1 is a crescent-shaped N-BAR protein playing a key role in forming deeply invaginated tubes in muscle T-tubules, has been recently implicated in rare and common diseases affecting different tissues and physiological functions. BIN1 downregulation is linked to cancer progression and also correlates with ventricular cardiomyopathy and arrhythmia preceding heart failure. Increased BIN1 expression is linked to increased...
TMPY-05760	DR3/TNFRSF25 Protein, Human, Recombinant (hFc), Biotinylated TRAMP,tumor necrosis factor receptor superfamily, member 25,...	Human	HEK293 Cells
	DR3/TNFRSF25 Protein, Human, Recombinant (hFc), Biotinylated is expressed in HEK293 mammalian cells with hFc tag. The predicted molecular weight is 45.9 kDa and the accession number is Q93038-10.
TMPY-00961	ADAM15 Protein, Human, Recombinant (His) MDC15,ADAM metallopeptidase domain 15	Human	HEK293 Cells
	ADAM15 Protein, Human, Recombinant (His) is expressed in HEK293 mammalian cells with His tag. The predicted molecular weight is 54 kDa and the accession number is Q13444-10.

重组蛋白

DR3/TNFRSF25 Protein, Human, Recombinant (hFc)

Cat.No: TMPY-01751

Species: Human

Expression System: HEK293 Cells

BIN1 Protein, Human, Recombinant (His)

Cat.No: TMPY-02300

Species: Human

Expression System: E. coli

DR3/TNFRSF25 Protein, Human, Recombinant (hFc), Biotinylated

Cat.No: TMPY-05760

Species: Human

Expression System: HEK293 Cells

ADAM15 Protein, Human, Recombinant (His)

Cat.No: TMPY-00961

Species: Human

Expression System: HEK293 Cells

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